Search Result
Results for "
KI mice
" in MedChemExpress (MCE) Product Catalog:
1358
Inhibitors & Agonists
17
Biochemical Assay Reagents
34
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13283
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MF63
1 Publications Verification
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PGE synthase
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Inflammation/Immunology
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MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1 .
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- HY-N1503
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6α-Hydroxygeniposide; Deacetylasperulosidic acid methyl ester
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Others
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Metabolic Disease
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Methyl deacetylasperulosidate is an iridoid and shows purgative effects in mice and lowers the blood glucose level in normal mice .
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- HY-124617
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Others
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Inflammation/Immunology
Cancer
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AMXT1501 is a novel inhibitor of the polyamine transport system. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells .
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- HY-120872
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Others
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Metabolic Disease
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AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice[1].
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- HY-116193
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- HY-RS08425
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Small Interfering RNA (siRNA)
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Others
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MICAL1 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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MICAL1 Human Pre-designed siRNA Set A
MICAL1 Human Pre-designed siRNA Set A
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- HY-RS08426
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Small Interfering RNA (siRNA)
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Others
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MICAL2 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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MICAL2 Human Pre-designed siRNA Set A
MICAL2 Human Pre-designed siRNA Set A
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- HY-RS08427
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Small Interfering RNA (siRNA)
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Others
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MICAL3 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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MICAL3 Human Pre-designed siRNA Set A
MICAL3 Human Pre-designed siRNA Set A
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- HY-N1503R
-
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Others
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Metabolic Disease
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Methyl deacetylasperulosidate (Standard) is the analytical standard of Methyl deacetylasperulosidate. This product is intended for research and analytical applications. Methyl deacetylasperulosidate is an iridoid and shows purgative effects in mice and lowers the blood glucose level in normal mice .
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- HY-130581
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Bacterial
Antibiotic
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Infection
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Lipid X is a novel monosaccharide precursor of Lipid A (the active moiety of gram-negative endotoxin). Lipid X is protective against endotoxin administered to mice and sheep and against life-threatening gram-negative infections in mice .
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- HY-119261
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Antibiotic
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Cancer
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Ruboxyl is an anthracycline antibiotic with antitumor activity. Ruboxyl inhibits colorectal cancer (CRC) liver metastasis in mice by 84%, suppresses B16 melanoma growth, and increases the survival rate of mice with L1210 or L5178Y leukemia .
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- HY-131508
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-
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- HY-101699A
-
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MCHR1 (GPR24)
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Metabolic Disease
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AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
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- HY-106925
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E 4868
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Antibiotic
Bacterial
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Infection
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Cetefloxacin (E 4868) is a board-spectrum antibacterial antibiotic, MIC of 0.007-8 µg/ml. Cetefloxacin exhibits good pharmacokinetic characters in mice. Cetefloxacin exhibits protective effects against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae in mice .
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- HY-N0260
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- HY-125850
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- HY-122398
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- HY-109506S1
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129Y83-d9
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Endogenous Metabolite
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Others
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DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
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- HY-109506S
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129Y83-d62
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Isotope-Labeled Compounds
Endogenous Metabolite
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Others
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DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
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- HY-P1438A
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Neuropeptide Y Receptor
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Neurological Disease
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Neuropeptide S(Rat) TFA is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) TFA also reduces anxiety-like behavior in mice.
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- HY-124112
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Parasite
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Infection
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PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
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- HY-N10279
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Others
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Infection
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Gymconopin C shows an antiallergic effect on ear passive cutaneous anaphylaxis reactions in mice.
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- HY-N6857C
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Others
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Inflammation/Immunology
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(±)-Armepavine hydrochloride is a compound that has demonstrated immunosuppressive effects on T lymphocytes and in lupus nephritic mice.
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- HY-126910
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Opioid Receptor
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Metabolic Disease
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Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
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- HY-109506S3
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129Y83-d9-1
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Isotope-Labeled Compounds
Endogenous Metabolite
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Others
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DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
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- HY-101699
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MCHR1 (GPR24)
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Metabolic Disease
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AMG-076 free base is an orally bioavailable and selective MCHR1 antagonist. AMG-076 free base results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
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- HY-153392
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Oxidative Phosphorylation
HDAC
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Cardiovascular Disease
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TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation .
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- HY-P10110
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Autophagy
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Neurological Disease
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retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice .
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- HY-W040276
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Others
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Cancer
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Diafen NN is an antioxidant. Diafen NN induces leukoses and local sarcomas in mice .
.
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- HY-119218
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- HY-124617A
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Apoptosis
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Inflammation/Immunology
Cancer
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AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells . Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
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- HY-B1198
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ENT-14250
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Parasite
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Infection
Cancer
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Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice .
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- HY-B0448S1
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Sodium Channel
Virus Protease
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Neurological Disease
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Phenytoin- 15N2, 13C is the 13C and 15N labeled Phenytoin[1]. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[2][3].
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- HY-100751
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Fungal
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Others
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N-563 is an analogue of deoxyspergualin with an immunostimulating activity,it promotes resistance to Candida albicans infection in mice.
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- HY-W011890A
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Others
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Infection
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Cridanimod sodium is an antiviral agent that induces interferon production in mice. Cridanimod can be utilized in antiviral research .
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- HY-110197
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6bK TFA
1 Publications Verification
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Others
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Metabolic Disease
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6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice .
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- HY-153617
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FOXO
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Metabolic Disease
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FOXO1-IN-3 is a highly-selective and orally active FOXO1 inhibitor. FOXO1-IN-3 reduces hepatic glucose production in mice. FOXO1-IN-3 improves insulin sensitivity and glucose control in db/db mice without causing weight gain .
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- HY-129762
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NSC-102627
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DNA/RNA Synthesis
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Cancer
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Yoshi-864 is an alkylsulfonate DNA crosslinker with anticancer activity. Yoshi-864 extends markedly the survival times of mice bearing L1210 leukemia or Ehrlich ascites carcinoma. Yoshi-864 also has a persistent reduction in ability to synthesize DNA in tumor cells from mice bearing the Ehrlich tumor .
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- HY-100617A
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(RS)-4-Carboxyphenylglycine
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Others
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Others
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(RS)-4CPG ((RS)-4-Carboxyphenylglycine) is a type I metabotropic glutamate receptor antagonist with activity in blocking LTP induction. In mice lacking IP3R1, (RS)-4CPG (500μM) nearly blocked long-term potentiation (LTP) induced by type I metabotropic glutamate receptor activation, with LTP of 117.6±1.7% (n = 8) in IP3R1(-/-) mice and 116.9±1.8% (n = 5) in IP3R1(+/+) mice.
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- HY-U00008
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CP 28888-27
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IFNAR
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Infection
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CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.
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- HY-N9794
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Others
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Inflammation/Immunology
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Isoboldine is a pyridine alkaloid. Isoboldine effectively alleviates inflammation and joint destruction in collagen-induced arthritis in mice .
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- HY-N3098
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Others
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Others
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Pelirine is an alkaloid isolated from R. perakensis and causes death in mice at concentrations of 100 mg/kg and above .
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- HY-156193
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- HY-12242
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Dopamine Transporter
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Neurological Disease
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GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice .
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- HY-12242A
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Dopamine Transporter
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Neurological Disease
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GBR 12935 is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice .
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- HY-P1437A
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Neuropeptide Y Receptor
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Neurological Disease
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Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
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- HY-139973
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Amyloid-β
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Neurological Disease
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OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice .
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- HY-128530
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Cuproptosis
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Tetrathiomolybdate, an orally active anti-copper agent, reduces copper levels in the body. Tetrathiomolybdate has a protective effect on collagen-induced arthritis in mice. Tetrathiomolybdate also reduces blood sugar, but has no effect on mice with hereditary diabetes (db/db). Tetrathiomolybdate inhibit angiogenesis, also shows antiangiogenic effects in malignant pleural mesothelioma .
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- HY-153322
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PROTACs
Itk
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Cancer
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ITK degrader 2 (compound 30) is an orally active, PROTAC-based ITK-targeted degrader (DC50<10 nM). ITK degrader 2 exhibits Cmax and Tmax in mice (po; 90 mg/kg) of 0.87 μM and 2 h, respectively. At this dose, ITK degrader 2 degrades ITK by 20% (6 h) in mice .
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- HY-P5724
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Bacterial
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Infection
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Nv-CATH is an antibacterial peptide of frog origin. Nv-CATH has broad-spectrum antibacterial activity against gram-positive and gram-negative bacteria. Nv-CATH significantly protects mice from fatal infections caused by Staphylococcus aureus. Nv-CATH protects mice from bacterial infection through antimicrobial immunoregulatory duality .
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- HY-118113
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Others
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Others
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BVT-116429 is an 11βHSD1 inhibitor with the activity of increasing adiponectin concentration and improving glucose homeostasis in diabetic mice. BVT-116429 can increase plasma adiponectin levels in diabetic KKAy mice, reduce basal insulin levels, and reduce fasting blood glucose levels after 10 days of inhibition, similar to the effect of rosiglitazone.
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- HY-12242B
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Dopamine Transporter
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Neurological Disease
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GBR 12935 fumarate is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 fumarate stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 fumarate also prevents the d-Fenfluramine-induced head-twitch response in mice .
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- HY-N0700
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α-Asarone; trans-Asarone
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GABA Receptor
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Neurological Disease
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alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.
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- HY-N0204
-
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Anemoside A3
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iGluR
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Others
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Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
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- HY-131102
-
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Bacterial
DNA/RNA Synthesis
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Infection
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Mequindox is an antimicrobial agent . Mequindox acts as an inhibitor of DNA synthesis. Mequindox induces genotoxicity and carcinogenicity in mice .
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- HY-139703
-
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Others
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Inflammation/Immunology
|
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Se-DMC attenuates complete Freund’s adjuvant (CFA)-induced inflammatory response, nociception, and neurobehavioral deficits in mice.
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- HY-N10196
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- HY-N10424
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Apoptosis
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Inflammation/Immunology
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Brazilein is an important immunosuppressive component isolated from Caesalpinia sappan L. Brazilein induces apoptosis in mice spleen lymphocytes .
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- HY-100922
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Others
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Neurological Disease
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N-Acetylglycyl-D-glutamic acid is a peptide with excitatory effect. N-Acetylglycyl-D-glutamic acid induces seizures in mice .
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- HY-126152
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Others
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Others
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Chlorthiamid is a broad-spectrum herbicide. Chlorthiamid is an olfactory toxicant with a high in vivo covalent binding in the olfactory mucosa of mice .
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- HY-B1002S
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Bacterial
Antibiotic
DNA/RNA Synthesis
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Infection
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Oxolinic acid-d5 is the deuterium labeled Oxolinic acid. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice[1][2][3].
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- HY-113354S
-
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Endogenous Metabolite
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Neurological Disease
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Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
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- HY-124499
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Integrin
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Cardiovascular Disease
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RUC-1 (Compound 1) is an inhibitor for αIIbβ3 integrin. RUC-1 inhibits fibrin deposition and platelet aggregation in hybrid hαIIb/mβ3 receptors expressing mice. RUC-1 exhibits antithrombotic effect in hαIIb/mβ3 receptor expressing mice .
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- HY-122916
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- HY-139994
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- HY-101139
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- HY-101139A
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XAC hydrochloride
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Adenosine Receptor
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Neurological Disease
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Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice .
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- HY-148548
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Amyloid-β
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Neurological Disease
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p-HTAA is a pentamer hydrogen thiophene acetic acid. p-HTAA specifically labels Aβ deposits in the mice living brain .
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- HY-131334
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AMPK
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Metabolic Disease
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AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect .
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- HY-124609
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Monoamine Oxidase
Dopamine Transporter
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Neurological Disease
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CAD031 is a derivative of the Alzheimer's disease (AD) targeting agent J147 (HY-13779) with neuroprotective and memory-enhancing properties. CAD031 enhances memory in mice, improves dendritic structure, and stimulates cell division in the germinal zone of the brain in aged mice. CAD031 is more active than J147 in human neural stem cell assays .
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- HY-15041
-
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Bradykinin Receptor
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Inflammation/Immunology
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NVP-SAA164 is an orally active nonpeptide kinin B1 receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .
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- HY-D0195
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- HY-W009688
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Others
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Inflammation/Immunology
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Dibutyl maleate, the diester of the Maleic Acid, can be used as an intermediate of pharmaceutical synthesis. Dibutyl maleate can enhance contact sensitization to Fluorescein isothiocyanate in mice .
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- HY-W550739
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- HY-D2203
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Fluorescent Dye
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Cancer
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BODIPY BDP4 has ssuperb sonosensitivity and high SDT efficiency against cancer cells and tumors in tumor-bearing mice .
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- HY-163087
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- HY-12610
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Parasite
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Cancer
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Carbonic anhydrase inhibitor 27 (compund 5g) is an antitrypanosomal agent that reduces parasites in the bloodstream and improves survival of infected mice .
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- HY-12752A
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Trimeprazine hemitartrate
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Histamine Receptor
Influenza Virus
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Neurological Disease
Inflammation/Immunology
Cancer
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Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice .
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- HY-B1198S
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ENT-14250-d9
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Isotope-Labeled Compounds
Parasite
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Infection
Cancer
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Piperonyl butoxide-d9 is the deuterium labeled Piperonyl butoxide.Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice .
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- HY-111792
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CRX-601
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Toll-like Receptor (TLR)
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Inflammation/Immunology
Cancer
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GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. Not only, GSK1795091 inhibits tumor growth and increases the survival in mice model, but results in long term survival in influenza challenge model in mice .
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- HY-W747072
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3-Sulfocholyl Taurine; TCA3S
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Others
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Metabolic Disease
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3-Sulfo-taurocholic Acid Disodium Salt (3-Sulfocholyl Taurine; TCA3S) is a metabolite of the conjugated bile acid taurocholic acid. Plasma levels of 3-Sulfo-taurocholic Acid Disodium Salt are elevated in wild-type and Sortilin 1 (Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated in Sort1 knockout mice at 24 hours post-BDL.
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- HY-105110
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SM-8668
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Fungal
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Infection
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SM-8668 is an effective orally active antifungal agent, with median effective doses (ED50) of 0.18, 3.7, and 5.9 mg/kg for systemic candidiasis, aspergillosis, and cryptococcosis in mice, respectively. Pharmacokinetic studies in mice and rats indicate that SM-8668 has a long half-life and a high total exposure. SM-8668 can be used in anti-infective research .
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- HY-115889
-
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NO Synthase
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Neurological Disease
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L-NAPNA is a nitric oxide synthase (NOS) inhibitor with an IC50 of 1.4 μM. L-NAPNA exhibits analgesic effects by inhibiting formalin-induced paw licking behavior in mice (ED50 of 57.2 mg/kg) and suppressing acetic acid-induced abdominal writhing in mice (ED50 of 25 mg/kg). L-NAPNA can be used in research related to central nervous system diseases .
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- HY-120783
-
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Endogenous Metabolite
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Neurological Disease
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Lu AF58801 is a potent, orally available, brain-penetrant positive allosteric modulator of α7 nicotinic acetylcholine receptors with efficacy in a novel object recognition task in mice. Lu AF58801 was shown to selectively enhance the activity of α7 nicotinic acetylcholine receptors. Lu AF58801 was able to improve cognitive function in mice treated with subchronic fluchlorothiazol (PCP) .
|
-
- HY-119955
-
|
LY-141894
|
Xanthine Oxidase
|
Others
|
|
Amflutizole (LY-141894) is an inhibitor of xanthine oxidase. Amflutizole abolishes free radical formation and release in cerebral ischemia/reperfusion mice .
|
-
- HY-B1429
-
-
- HY-109044
-
-
- HY-N5126
-
|
|
Others
|
Neurological Disease
|
Juncusol, a phenanthrenoid found in Juncus setchuenensis, possesses anxiolytic effect. Juncusol is associated with metabolic changes in cortical serotonin/dopamine levels in Mice .
|
-
- HY-N10359
-
-
- HY-N1149
-
|
(-)-Tilifodiolide
|
Others
|
Others
|
|
Tilifodiolide ((-)-Tilifodiolide) is a lactone, which can be isolated from the roots of Salvia tiliaefolia. Tilifodiolide has anti-inflammatory activity in mice model .
|
-
- HY-163346
-
|
|
Others
|
Metabolic Disease
|
|
TPEG-P is an enzyme-activated intramolecular hydrogen bond (IMHB) enhanced probe, developed for ALP detection in cells and mice models of DILI .
|
-
- HY-129318
-
|
|
Bacterial
|
Infection
|
|
MBX 1066 is a potent antibacterial agent. MBX 1066 shows inhibition for Mycobacterium tuberculosis. MBX 1066 shows antibacterial activity in mice .
|
-
- HY-B1198R
-
|
ENT-142521 (Standard)
|
Parasite
|
Infection
Cancer
|
|
Piperonyl butoxide (Standard) is the analytical standard of Piperonyl butoxide. This product is intended for research and analytical applications. Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice .
|
-
- HY-P10746
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
EB1002 is a selective NK2R agonist. EB1002 significantly raises the expression levels of mitochondrial biosynthesis-related genes (like PGC-1α) in obese mice, indicating that it promotes energy expenditure by boosting mitochondrial activity. EB1002 also increases the insulin sensitivity and improves glycolipid metabolism of the mice. EB1002 is promising for research of obesity and type 2 diabetes .
|
-
- HY-124557
-
-
- HY-137207
-
MK-28
5 Publications Verification
|
PERK
|
Neurological Disease
|
|
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .
|
-
- HY-11053
-
|
|
nAChR
|
Neurological Disease
|
|
S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the research of aging-related memory disturbances .
|
-
- HY-106471
-
|
Propyldazine
|
Others
|
Cardiovascular Disease
|
|
Pildralazine (Propyldazine) is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally active, has no significant carcinogenicity in mice model .
|
-
- HY-113889
-
|
|
Progesterone Receptor
|
Cancer
|
|
ZK112993 is a potent progesterone receptor (PR) antagonist. ZK112993 significantly inhibits the growth of T61 human tumors in nude mice .
|
-
- HY-145454A
-
|
(-)-3-PPP
|
Dopamine Receptor
|
Neurological Disease
|
|
Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. Preclamol inhibits the locomotor activity of mice and rats in low doses .
|
-
- HY-W721596
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Pentadecanoyl ethanolamide is derivate of endougenous lipid amides, the N-acylethanolamines. Pentadecanoyl ethanolamide exhibits anticonvulsant efficacy in electroshocked mice without significant toxicity .
|
-
- HY-107567B
-
|
β-Alanylhistamine dihydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Carcinine (β-Alanylhistamine) dihydrochloride is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice .
|
-
- HY-126185
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Nibroxane is an orally active antibacterial agent. Nibroxane can be metabolized to 2-methyl-5-nitro-m-dioxane in mice .
|
-
- HY-159737
-
|
HOE 602
|
HCV
CMV
|
Infection
|
|
Rociclovir (HOE 602) is an acyclic nucleoside derivative. Rociclovir protects mice against HSV and MCMV infections, but lacks antiviral activity in cell cultures .
|
-
- HY-P1823
-
|
|
Akt
mTOR
Caspase
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
C-Reactive Protein (CRP) is an anti-pneumococcal plasma protein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma .
|
-
- HY-P1726A
-
|
|
Melanocortin Receptor
|
Cancer
|
|
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
|
-
- HY-N1428S3
-
|
|
Apoptosis
Endogenous Metabolite
Antibiotic
|
Cancer
|
|
Citric acid- 13C3 is the 13C labeled Citric acid[1]. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[2][3][4].
|
-
- HY-P99797
-
|
JR-141
|
Transferrin Receptor
|
Neurological Disease
|
|
Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice .
|
-
- HY-107567
-
|
β-Alanylhistamine
|
Histamine Receptor
|
Neurological Disease
|
|
Alistin (Carcinine; β-Alanylhistamine) is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice .
|
-
- HY-N8522
-
|
|
Others
|
Metabolic Disease
|
|
9,10-Dihydroxystearic acid is an oxidation product of oleic acid. 9,10-Dihydroxystearic acid can improve glucose tolerance and insulin sensitivity in KKAy mice .
|
-
- HY-106887
-
|
|
Neprilysin
Others
|
Neurological Disease
|
|
SCH 32615 is an enkephalinase (the enzymes responsible for the degradation of endogenous enkephalins) inhibitor. SCH 32615 can enhance surgery- and pregnancy-induced analgesia in mice .
|
-
- HY-141896
-
|
|
RET
|
Cancer
|
|
RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
|
-
- HY-114651
-
|
|
Others
|
Cancer
|
|
Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitory activity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice .
|
-
- HY-163039
-
|
|
Others
|
Inflammation/Immunology
|
DOTA-biotin is a DOTA-based small molecule hapten. DOTA-biotin has low tissue and whole-body retention in mice 4 h postinjection .
|
-
- HY-157492
-
|
|
Bacterial
|
Infection
|
|
RO7075573 (compound 3) is an antibiotics that targets the lipopolysaccharide (LPS) transport machine in Acinetobacter. RO7075573 protects mice from A. baumannii infections .
|
-
- HY-113878
-
-
- HY-W100403
-
|
Choline p-toluenesulfonate
|
Phospholipase
|
Cancer
|
|
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) .
|
-
- HY-125850R
-
|
|
Drug Metabolite
|
Inflammation/Immunology
|
|
Berberrubine (chloride) (Standard) is the analytical standard of Berberrubine (chloride). This product is intended for research and analytical applications. Berberrubine chloride is an active metabolite of berberine, attenuates ulcerative colitis in mice model .
|
-
- HY-163965
-
|
|
Others
|
Cancer
|
|
Antitumor agent-185 (compound 3) shows antitumor activity that could effectively reduce the growth of tumors and prolong the survival time of mice in vivo .
|
-
- HY-116799
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
NSC 145669 is an inhibitor for tubulin polymerization with IC50 of 1.7 μM. NSC 145669 exhibits cytotoxicity in cancer cells and reveals antileukemic efficacy in mice .
|
-
- HY-123367
-
|
|
Others
|
Others
|
|
Rubraxanthone is a compound with multiple biological activities. Its pharmacokinetic parameters were determined in mice and it showed a certain concentration variation pattern in plasma after oral administration.
|
-
- HY-122323
-
|
Leucylarginine
|
Others
|
Others
|
|
L-Leucyl-L-arginine (Leucylarginine) is a compound that inhibits the analgesic effect of systemically administered L-arginine in a carrageenan-induced hyperalgesia model in mice when administered intracerebroventricularly.
|
-
- HY-159972
-
-
- HY-161618
-
|
|
JAK
EGFR
PI3K
IGF-1R
GSK-3
|
Inflammation/Immunology
Endocrinology
|
|
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
|
-
- HY-120597
-
|
|
Calcium Channel
|
Neurological Disease
|
|
SAK3 is a potent T-type voltage-gated Ca 2+ channels (T-VGCCs) enhancer. SAK3 enhances Cav3.1 and Cav3.3 T-type Ca 2+ channel currents. Acute SAK3 administration improves memory deficits in olfactory-bulbectomized mice . SAK3 inhibits amyloid β plaque formation in APP-KI mice by activating the proteasome activity .
|
-
- HY-147548
-
|
|
Others
|
Others
|
|
Keap1-Nrf2-IN-10 (compound 15) is a potent NQO1 inducer. Keap1-Nrf2-IN-10 inhibits oxidative stress by decreasing the levels of MDA, ROS, NQO1 in the liver for gamma-irradiated mice. Keap1-Nrf2-IN-10 improves the survival of gamma-irradiated mice .
|
-
- HY-106720C
-
|
(+)-YM 09538
|
Others
|
Others
|
|
(+)-Amosulalol ((+)-YM 09538) is an α,β-blocker with pharmacokinetic and metabolic activities in mice. In mice, the plasma concentration of (+)-Amosulalol decreased in a biphasic manner after intravenous injection. The time to reach the maximum plasma concentration after oral administration was 0.25h, and then decreased. The systemic bioavailability was 38.7%, and it was mainly excreted through urine. Multiple metabolites were detected in urine, and a new metabolite amosulalol carbamoyl glucuronide was found in bile samples.
|
-
- HY-106720B
-
|
(-)-YM 09538
|
Others
|
Others
|
|
(-)-Amosulalol ((-)-YM 09538) is an α,β-blocker with pharmacokinetic and metabolic activities in mice. In mice, the plasma concentration of (-)-Amosulalol decreased in a biphasic manner after intravenous injection. The time to reach the maximum plasma concentration after oral administration was 0.25h, and then decreased. The systemic bioavailability was 38.7%, and it was mainly excreted through urine. Multiple metabolites were detected in urine, and a new metabolite amosulalol carbamoyl glucuronide was found in bile samples.
|
-
- HY-121365
-
|
|
Others
|
Infection
|
|
Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
|
-
- HY-113412A
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
3-Methylhistamine dihydrochloride is a degradation product of histamine. 3-Methylhistamine dihydrochloride, a methylated product of histamine, is associated with immune response and shows upregulation in the vaccinated mice .
|
-
- HY-N0546
-
|
Nuezhenoside
|
CaSR
|
Metabolic Disease
|
|
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice .
|
-
- HY-N3506
-
|
|
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Wilfortrine is a bioactive sesquiterpene alkaloid. Wilfortrine exhibits immunosuppresive effects. Wilfortrine also can inhibit leukaemia cell growth in mice and shows anti-HIV activity .
|
-
- HY-139844
-
|
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 7 inhibits proinflammatory cytokines by blocking the NF-κB/MAPK signaling pathway in LPS-treated RAW 264.7 cells as well as mice.
|
-
- HY-121565
-
|
|
Others
|
Metabolic Disease
Endocrinology
|
|
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice .
|
-
- HY-145454
-
|
(+)-3-PPP
|
Dopamine Receptor
|
Neurological Disease
|
|
(R)-Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. (R)-Preclamol inhibits the locomotor activity of mice and rats in low doses .
|
-
- HY-W248594
-
|
|
Fluorescent Dye
|
Others
|
|
IR 813 tosylate is a near-infrared (NIR) fluorescent dye (λex=815 nm, λem=840 nm) and can be used for visualizing regional lymph nodes in mice .
|
-
- HY-N11021
-
|
|
Others
|
Others
|
|
Feruloyl tyramine, an amide compound, can be isolated from ethanol extract of hemp seed. Feruloyl tyramine injected into the lateral ventricle caused hypothermia and dyskinesia in mice .
|
-
- HY-105052
-
|
Enisoprost
|
Prostaglandin Receptor
|
Endocrinology
|
|
SC 34301 (Enisoprost) is a potent and orally active PGE1 analog. SC 34301 significantly reduces bacterial translocation and improves survival for burned mice .
|
-
- HY-155236
-
-
- HY-100967
-
|
Homodimaprit dihydrochloride
|
Histone Methyltransferase
|
Neurological Disease
|
|
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice .
|
-
- HY-117774
-
|
|
Others
|
Neurological Disease
|
|
AHR-2244 hydrochloride is a bioactive agent that acts against psychosis and anxiety. It selectively blocks CAR in mice, rats, and cats, and can reduce the lethality associated with amphetamine .
|
-
- HY-105969
-
|
NSC-29630; 3',5'-Dichloromethotrexate
|
Others
|
Cancer
|
|
Dichloromethotrexate (NSC-29630), an orally active antitumor agent, shows antitumor effect against L1210 leukemia and C3H lymphosarcoma in mice .
|
-
- HY-105589
-
|
HL 707
|
Parasite
|
Infection
|
|
Liroldine (Compound 10) is an anti-amebic agent that exhibits effective anti-amebic activity in both the intestines and livers of mice. Liroldine can be utilized for the research of amebiasis .
|
-
- HY-125047
-
|
UK 3557
|
Monoamine Oxidase
|
Neurological Disease
|
|
Daledalin tosylate (UK 3557) has mono-amine oxidase inhibitory activity in vitro, probably by acting as a substrate. Daledalin tosylate also has antidepressant effects. Daledalin tosylate potentiates amphetamine-induced excitation in rats, antagonises Reserpine (HY-N0480)-hypothermia in mice, tetrabenazine-sedation in rats and Reserpine (HY-N0480)- and Tetrabenazine (HY-B0590)-induced ptosis in mice with . Daledalin tosylate is proming for rasearch of depressive illness .
|
-
- HY-162866
-
|
|
Autophagy
|
Metabolic Disease
|
CXM102 is an autophagy activator. CXM102 can induce autophagy in aged BMSCs, leading to the rejuvenation of BMSCs and preferential differentiation into osteoblasts. CXM102 promotes the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. CXM102 can stimulate bone synthesis metabolism in middle-aged male mice, reduce bone marrow adipocytes, delay bone loss, lower serum inflammation levels, decrease organ fibrosis, and extend the lifespan of the mice .
|
-
- HY-103496
-
|
|
GABA Receptor
|
Others
|
|
U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent .
|
-
- HY-126426
-
|
|
DNA Methyltransferase
|
Cardiovascular Disease
|
|
CBHcy is an inhibitor for betaine-homocysteine S-methyltransferase (BGMT), with an IC50 of 0.09 μM. CBHcy upregulates the plasma total homocysteine and causes transient hyperhomocysteinemia in mice model .
|
-
- HY-149955
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%) .
|
-
- HY-106947
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SY-640 is an Acetamide derivative and has potent hepatoprotective effect. SY-640 reduces Propionibacterium acnes and Lipopolysaccharide-induced liver injury in mice .
|
-
- HY-N3204
-
|
|
Apoptosis
|
Neurological Disease
|
|
Neoechinulin A is an isoprenyl indole alkaloid that exhibits scavenging, neurotrophic factor-like, and anti-apoptotic activities. Neoechinulin A induces memory improvements and antidepressant-like effects in mice .
|
-
- HY-103357
-
-
- HY-146297
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidoreductase-IN-2 (Compound IVa) is a xanthine oxidoreductase (XOR) inhibitor with the IC50 of 7.2 nM. Xanthine oxidoreductase-IN-2 shows hypouricemic effects in mice .
|
-
- HY-D1535
-
|
|
Fluorescent Dye
|
Others
|
|
IR 813 perchlorate is a near-infrared (NIR) fluorescent dye (Ex=815 nm, Em=840 nm) and can be used for visualizing regional lymph nodes in mice .
|
-
- HY-N3960
-
|
|
PPAR
Bacterial
|
Infection
Metabolic Disease
|
|
Glycyrin is a PPAR-γ ligand of licorice. Glycyrin can decrease the blood glucose levels of genetically diabetic mice. Glycyrin also shows antibacterial activity .
|
-
- HY-103290
-
|
|
Bradykinin Receptor
|
Others
|
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- HY-W275039
-
|
2-Phenylbenzoquinone
|
Others
|
Neurological Disease
|
|
Phenylquinone (2-Phenylbenzoquinone) causes pain and induces writhing in mice, and is often used in experiments to test the effectiveness of analgesics or agent that can suppress or relieve pain .
|
-
- HY-124412S
-
-
- HY-145525
-
|
CAR 18:2; C18:2 Carnitine; L-Carnitine linoleoyl ester
|
Others
|
Others
|
|
Linoleoyl-L-carnitine is a naturally occurring long-chain acylcarnitine. Hepatic levels of linoleoyl-L-carnitine are increased following high-dose (200 mg/kg) administration of Isoniazid (Item No. 20378) in mice.
|
-
- HY-163618
-
|
|
Fluorescent Dye
Monoamine Oxidase
|
Cancer
|
|
DHMQ is a NIR fluorescent probe that binds to the propylamino group of monoamine oxidase A (MAO-A). DHMQ tracks MAO-A activity in real-time by using fluorescence imaging on mice and cells .
|
-
- HY-161728
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 223 (compound D8-03) is an inhibitor of Francisella tularensis. Antibacterial agent 223 can inhibit intracellular growth of Francisella tularensis in mice .
|
-
- HY-P10721
-
|
|
Antibiotic
Bacterial
|
Infection
|
Plectasin is a peptide antibiotic derived from saprophytic fungi. Plectasin can kill pneumococcus in vitro. Plectasin can alleviate experimental peritonitis and pneumonia caused by pneumococcus in mice .
|
-
- HY-118803
-
|
|
Factor Xa
|
Others
|
|
AS1468240 is an orally active inhibitor for anticoagulant factor Xa (fXa), that inhibits human fXa with IC50 of 8.7 nM. AS1468240 prolongs the coagulation time in mice .
|
-
- HY-158272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Penicillin/OVA is a conjugate of penicillin and Ovalbumins (HY-W250978), that is utilized as an antigen in immunological research. Penicillin/OVA causes IgE-dependent anaphylactic response to penicillin in mice .
|
-
- HY-P10312
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models .
|
-
- HY-N0541
-
|
Ginsenoside A1
|
Endogenous Metabolite
|
Others
|
|
Pseudoginsenoside F11 (Ginsenoside A1), a component of Panax quinquefolium (American ginseng), has been demonstrated to antagonize the learning and memory deficits induced by scopolamine, morphine and methamphetamine in mice.
|
-
- HY-D0211
-
|
|
Fluorescent Dye
|
Cancer
|
|
Phenolphthalein is an acid-base indicator that is colorless in an acidic environment and pink in an alkaline environment. Phenolphthalein is genotoxic and potentially carcinogenic to mice. In addition, phenolphthalein is also a blood indicator .
|
-
- HY-128578
-
|
|
PDHK
|
Metabolic Disease
Inflammation/Immunology
|
|
KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice .
|
-
- HY-N6774
-
|
|
Others
|
Infection
|
|
Cytochalasin C is a cell-permeable fungal toxin and induces the formation of nuclear rodlets. Cytochalasin C is 10 times less toxic in mice than is cytochalasin D .
|
-
- HY-N1109
-
Uvaol
1 Publications Verification
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice .
|
-
- HY-119981
-
|
|
Chloride Channel
|
Neurological Disease
Cancer
|
|
Ani9 is an ANO1 inhibitor, with an IC50 of 77 nM. Ani9 can inhibit smooth muscle contractions in mice and is applicable in research related to diseases such as tumors .
|
-
- HY-P5890
-
-
- HY-N8317
-
|
|
Others
|
Cancer
|
|
Rubicordifolin is a natural product that can be isolated from Rubia cordifolia. Rubicordifolin inhibits the growth of sarcoma ascites in mice. Rubicordifolin has significant cytotoxic activity both in vitro and in vivo .
|
-
- HY-N9685
-
|
D-(+)-Digitoxose
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Digitoxose (D-(+)-Digitoxose), a natural product, specifically and competitively inhibits glucose-stimulated insulin release from islets in lean and obese mice. Digitoxose can be used in diabetes research .
|
-
- HY-114918
-
|
|
TSH Receptor
|
Endocrinology
|
|
MS438 is a potent thyrotropin receptor (TSHR) agonist with an EC50 of 53 nM. MS438 binds to the serpentine portion of the TSHR. MS438 induces T4 secretion in mice .
|
-
- HY-N10171
-
|
|
Others
|
Inflammation/Immunology
|
|
GB-2a is a bioflavonoids that can be isolated from Rheedia gardneriana. GB-2a has significant analgesic activity in mice with 58.9% inhibition .
|
-
- HY-N12719
-
|
|
Others
|
Others
|
|
Isocampneoside I is an acylated phenethyl oligosaccharide that can be isolated from Cistanche deserticola (Orobanchaceae). Isocampneoside I inhibits D-galactose-induced cytotoxicity and protects primary hepatocytes in mice .
|
-
- HY-138100
-
|
(+)-Hyalodendrin
|
Fungal
|
Infection
|
|
Hyalodendrin ((+)-Hyalodendrin) is a fungal growth inhibitor with inhibitory activity against wood decay fungi. Hyalodendrin has low phytotoxicity, with an acute toxicity (LD50) of 75 mg/kg in mice .
|
-
- HY-163906
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 16 (Compound 4) is an inhibitor of methicillin-resistant Staphylococcus aureus (MRSA). Anti-MRSA agent 16 is effective in combination with oxacillin or meropenem in infected mice .
|
-
- HY-116597
-
|
F3MethylAA
|
PPAR
|
Inflammation/Immunology
|
|
L-783483 (F3MethylAA) is an agonist for PPARδ. L-783483 ameliorates Carrageenan (HY-125474)-induced paw edema in mice .
|
-
- HY-118537
-
|
|
Parasite
|
Infection
|
|
ICI 56780 is an antimalarial agent, that exhibits etiological prevention and blood schizonticidal activity in rodent malaria models. ICI 56780 develops parasite resistance in P. berghei infected mice .
|
-
- HY-126720
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
N-Lignoceroyl Taurine is an arachidonoyl amino acid and taurine conjugate with a fatty acid that can be isolated from bovine brain. N-Lignoceroyl Taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of the brain and spinal cord of wild-type and fatty acid amide hydrolase (FAAH) knockout mice. N-Lignoceroyl Taurine levels were 23-26-fold higher in FAAH -/- mice compared to wild-type mice, suggesting that FAAH utilizes N-Lignoceroyl Taurine as a substrate. However, in vitro experiments with purified FAAH showed that N-Lignoceroyl Taurine was hydrolyzed 2,000-fold slower in FAAH compared to oleoylethanolamide. N-Acyl Taurines with polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) calcium channel family, including TRPV1 and TRPV4.
|
-
- HY-143312C
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
(S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
|
-
- HY-143312E
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
|
-
- HY-120462
-
|
|
Dihydroorotate Dehydrogenase
Parasite
|
Infection
|
|
Genz-669178 is an inhibitor for dihydroorotate dehydrogenase (DHODH) with IC50 of 0.015-0.05 μM in Plasmodium spp.. Genz-669178 inhibits P. berghei, P. falciparum strains 3D7 and Dd2 with IC50 of 0.068, 0.008 and 0.01 μM, respectively. Genz-669178 exhibits anti-malarial efficacy in P. berghei-infected mice with ED50 of 13-21 mg/kg/day. Genz-669178 exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-161926
-
|
|
PPAR
|
Metabolic Disease
|
|
YGT-31 is a modulator for PPARγ with an IC50 of 1.72 μM, and a Ki of 0.62 μM. YGT-31 reduces blood glucose levels and improves insulin resistance in db/db mice type 2 diabetes models, through inhibition of CDK5-mediated PPARγ-Ser273 phosphorylation. YGT-31 exhibits anti-hepatic steatosis effect in mice non-alcoholic fatty liver disease (NAFLD) model .
|
-
- HY-B0448
-
-
- HY-12246
-
XEN445
1 Publications Verification
|
Others
|
Cardiovascular Disease
|
|
XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
|
-
- HY-N0901A
-
-
- HY-B0448A
-
|
5,5-Diphenylhydantoin sodium salt
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-N4243
-
|
|
Others
|
Metabolic Disease
|
|
Neocurdione is a hepatoprotective sesquiterpene isolated from Curcuma zedoaria rhizome. Neocurdione exerts potent effect on D-galactosamine- (D-Gain) and lipopolysaccharide- (LPS) induced acute liver injury in mice .
|
-
- HY-101325
-
-
- HY-100782
-
|
2-APH; 2-Amino-7-phosphonoheptanoic acid
|
iGluR
|
Neurological Disease
|
|
DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice .
|
-
- HY-P0107
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-100784
-
|
|
EAAT
|
Neurological Disease
|
|
Dihydrokainic acid (DHK) is a glutamate transporter GLT1 (EAAT2) inhibitor. Dihydrokainic acid impairs novel object recognition (NOR) memory performance in mice. Dihydrokainic acid also shows epileptogenic effects .
|
-
- HY-110020
-
-
- HY-112636
-
|
|
Amyloid-β
|
Others
|
|
Astrophloxine is a fluorescent imaging probe capable of targeting antiparallel dimers. Astrophloxine can be used to detect aggregated Aβ in brain tissue and cerebrospinal fluid samples of Alzheimer's disease (AD) mice .
|
-
- HY-148617
-
-
- HY-106997
-
|
BAY 10-8888; PLD 118
|
Fungal
|
Infection
|
|
Icofungipen is an orally active antifungal agent. Icofungipen is the representative of beta amino acids, is toxic against Candida species. Icofungipen protects infected mice survival from C. albicans infection .
|
-
- HY-P5003
-
|
|
MMP
|
Inflammation/Immunology
|
|
Collagen Type II Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen Type II Fragment can be used for research on inflammation and immunity .
|
-
- HY-103163
-
-
- HY-119899
-
|
|
Others
|
Cancer
|
|
BO-0742, a derivative of AHMA and N-mustard, is a potent anti-cancer agent. BO-0742 significantly suppresses the growth of xenografts of human breast and ovarian cancers in mice .
|
-
- HY-P6053
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
|
-
- HY-W040276R
-
|
|
Others
|
Cancer
|
|
Diafen NN (Standard) is the analytical standard of Diafen NN. This product is intended for research and analytical applications. Diafen NN is an antioxidant. Diafen NN induces leukoses and local sarcomas in mice .
.
|
-
- HY-105098B
-
|
(±)-BMS-180194; SQ 33054
|
Others
|
Others
|
|
(±)-Lobucavir ((±)-BMS-180194) is a nucleoside analog with carcinogenic activity. In mice, chronic administration of (±)-Lobucavir resulted in tumor formation with a tumor spectrum similar to that observed after chronic administration of zidovudine or ganciclovir.
|
-
- HY-24238
-
|
|
Others
|
Others
|
|
DLCI-1 is a potent and selective oral inhibitor of cytochrome P450 2A6 (CYP2A6) that markedly reduces nicotine self-administration in both male and female mice.
|
-
- HY-133171A
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
(S)-Norfluoxetine, a S enantiomer of Norfluoxetine (HY-135556), is a selective serotonin reuptake inhibitor. (S)-Norfluoxetine can increase allopregnanolone levels and reduce aggression in socially isolated mice .
|
-
- HY-163482
-
|
|
Parasite
|
Infection
|
|
ELQ-596 is a quinolone derivative, that exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-596 attenuates babesiosis in immunosuppressed mice .
|
-
- HY-163484
-
|
|
Parasite
|
Infection
|
|
ELQ-650 is a quinolone derivative, that exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-650 attenuates babesiosis in immunosuppressed mice .
|
-
- HY-B0401
-
|
|
Na+/K+ ATPase
|
Metabolic Disease
Cancer
|
|
Tolbutamide is an orally active KATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete .
|
-
- HY-101404A
-
|
|
Others
|
Cardiovascular Disease
Inflammation/Immunology
|
|
L-Homocysteine thiolactone hydrochloride is an intramolecular thioester of Homocysteine. Homocysteine thiolactone hydrochloride prevents translational incorporation of homocysteine into proteins. L-Homocysteine thiolactone hydrochloride can induce elevated HHcy (hyperhomocysteinemia) in mice .
|
-
- HY-12459
-
|
|
Bacterial
|
Infection
|
|
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both agent-sensitive and resistant cells of P388 leukemia in mice .
|
-
- HY-131181
-
LEI-401
2 Publications Verification
|
Phospholipase
|
Neurological Disease
|
|
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice .
|
-
- HY-139798
-
|
|
Bacterial
|
Infection
|
|
Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice .
|
-
- HY-150036
-
|
|
Antibiotic
Cholecystokinin Receptor
|
Cancer
|
|
Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice .
|
-
- HY-105790
-
|
Pipethanate
|
Cholinesterase (ChE)
|
Cardiovascular Disease
|
|
Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates .
|
-
- HY-122672
-
|
|
FAK
|
Neurological Disease
|
|
Adhesamine, dumbbell-shaped molecule, activates MAPK/FAK pathway. Adhesamine promotes adhesion and growth of mammalian cells. Adhesamine accelerates the differentiation and improves the survival of mice hippocampal neurons in primary culture .
|
-
- HY-118992
-
|
X 5108; Goldinomycin
|
Antibiotic
Bacterial
|
Infection
|
|
Aurodox (X 5108) is an antibiotic obtained from a streptomyces variant, Aurodox can against a number of gram-positive bacteria. Aurodox shows a very low toxicity in mice and promoted poultry growth .
|
-
- HY-N1546
-
|
|
Others
|
Inflammation/Immunology
|
|
Protoplumericin A is a bioactive ingredient of Plumeria obtusa L. attenuates. Protoplumericin A mitigated lipopolysaccharide (LPS) -induced acute lung injury in mice. Protoplumericin A can be used to study the LPS-induced anti-inflammatory effect .
|
-
- HY-106902
-
|
|
Acyltransferase
|
Cardiovascular Disease
|
|
F-1394 is an orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that inhibits dietary cholesterol absorption in mice. F-1394 can be used in cardiovascular disease research .
|
-
- HY-156856
-
|
|
ADC Cytotoxin
|
Cancer
|
|
FL118-14-Propanol is a FL118 derivative. FL118-14-Propanol synthesized ADC molecule has good anti-tumor effect in mice .
|
-
- HY-117630
-
|
|
Others
|
Cancer
|
|
RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice .
|
-
- HY-W679796
-
|
4-Phenylbutyl isothiocyanate
|
Others
|
Cancer
|
|
PBITC (4-Phenylbutyl isothiocyanate) is an orally active antitumor agent, and inhibits NNK (HY-126477) induced lung tumors in mice. PBITC is a sulfur analog of ISC-4 .
|
-
- HY-119519
-
|
|
Others
|
Neurological Disease
|
|
OB-2 is a STOML3 oligomerization blocker. OB-2 reverses pathological mechanical hypersensitivity. OB-2 can be used for research of painful diabetic neuropathy in mice .
|
-
- HY-126152R
-
|
|
Others
|
Others
|
|
Chlorthiamid (Standard) is the analytical standard of Chlorthiamid. This product is intended for research and analytical applications. Chlorthiamid is a broad-spectrum herbicide. Chlorthiamid is an olfactory toxicant with a high in vivo covalent binding in the olfactory mucosa of mice .
|
-
- HY-131102R
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Mequindox (Standard) is the analytical standard of Mequindox. This product is intended for research and analytical applications. Mequindox is an antimicrobial agent . Mequindox acts as an inhibitor of DNA synthesis. Mequindox induces genotoxicity and carcinogenicity in mice .
|
-
- HY-105790A
-
|
|
Cholinesterase (ChE)
|
Cardiovascular Disease
|
|
Piperilate (Pipethanate) hydrochloride is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate hydrochloride also causes hypotension and rescues mice poisoned by the organophosphates .
|
-
- HY-156126
-
|
|
Others
|
Others
|
|
Lentztrehalose C (compound LTC) is a trehalose analogue with high stability in microbial and mammalian cells. It can be detected in the blood of mice and is ultimately excreted in feces and urine. It can induce autophagy in human cancer cells.
|
-
- HY-149208
-
|
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
|
-
- HY-114969
-
|
NSC 233846; SYD 230; Tremerad
|
Parasite
|
Infection
|
|
Clioxanide is a potential anti-liver fluke (Fasciola hepatica) agent. The results showed that Clioxanide showed no efficacy against 4-week-old or 19-week-old flukes at doses of 135 mg/kg or 200 mg/kg. In contrast, hexachloroethane was very effective against older flukes, reaching 100% efficacy at lower doses. The study pointed out that laboratory mice may not be suitable for screening potential compounds against liver fluke infections in ruminants such as cattle and sheep. In addition, no obvious toxic reactions were observed in mice with Clioxanide .
|
-
- HY-N2189
-
-
- HY-B0860
-
|
|
ATP Synthase
Others
|
Cancer
|
|
Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male and female mice by 73 and 27%, respectively.
|
-
- HY-145265
-
|
|
Bacterial
|
Infection
|
|
Antimicrobial photosensitizer-1 is a promising candidate as the antimicrobial photosensitizer for combating pathogenic microorganism infections. Antimicrobial photosensitizer-1 exhibits an impressive antimicrobial efficacy in S. aureus-infected mice wounds .
|
-
- HY-108623
-
|
CP-80,633
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice .
|
-
- HY-P0009
-
|
SB-75
|
GnRH Receptor
|
Endocrinology
|
|
Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist. Cetrorelix inhibits the endogenous luteinizing hormone surge during ovarian stimulation. Cetrorelix reduces cyclophosphamide induced ovarian follicular destruction in mice .
|
-
- HY-118388
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour .
|
-
- HY-153262
-
|
|
Ras
|
Cancer
|
|
KRASG12C IN-2 (compound 17) is an orally active KRAS G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice .
|
-
- HY-149227
-
-
- HY-120769
-
-
- HY-N11972
-
|
|
Others
|
Neurological Disease
|
|
β-Maaliene can be isolated from the fresh leaves of Vitex densiflora (Maaliene) and is the main component in the isolate. β-Maaliene can significantly reduce the exercise capacity of mice at certain doses .
|
-
- HY-116046
-
|
|
Melatonin Receptor
|
Others
|
|
GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR 196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice .
|
-
- HY-119105
-
|
|
Others
|
Neurological Disease
|
|
LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites .
|
-
- HY-160025
-
-
- HY-101325A
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BRL-37344 (Fosigotifator (THAM sodium)) is a specific β3-adrenergic receptor agonist. BRL-37344 treatment significantly lowers the body weight of obese mice .
|
-
- HY-163782
-
|
|
Autophagy
Phosphatase
|
Infection
|
|
SMIP-031 is a potent and orally active PPM1A inhibitor with an IC50 value of 180 nM. SMIP-031 induces autophagy. SMIP-031 inhibits Mycobacterium tuberculosis infect in mice .
|
-
- HY-14866
-
|
ADX-10059
|
mGluR
|
Neurological Disease
|
|
Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice .
|
-
- HY-162498
-
|
|
Parasite
|
Infection
|
|
Antileishmanial agent-29 (Compound 110) is an orally active antileishmanial agent. Antileishmanial agent-29 (p.o., 40, 60 mg/kg, 10 days) protects mice from leishmania infection .
|
-
- HY-N7912
-
|
(2S)-Pterosin A
|
Others
|
Metabolic Disease
|
|
Pterosin A is an orally active anti-diabetic agent. Pterosin A promotes glucose uptake, increases serum insulin, and improves hyperglycemia and glucose intolerance in diabetic mice. Pterosin A can be isolated from Pteridium aquilinum .
|
-
- HY-B0534
-
|
Ro111163
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-112726
-
|
BI-1467335
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-4728A (BI-1467335) is a selective, orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO). PXS-4728A ameliorates chronic obstructive pulmonary disease in mice .
|
-
- HY-P2203
-
SAHM1
1 Publications Verification
|
Notch
|
Inflammation/Immunology
|
|
SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice .
|
-
- HY-12124
-
|
|
NO Synthase
|
Cardiovascular Disease
|
|
BBS-4 is a potent and selective inducible nitric oxide synthase (NOS2) dimerization inhibitor, with an IC50 of 0.49 nM. BBS-4 can protect mice from the cardiovascular dysfunction of sepsis .
|
-
- HY-P0107A
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-143228
-
-
- HY-147323
-
-
- HY-148163
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Polystyrene sulfonic acid is a potentially toxic hazardous substance. Polystyrene-derived microplastics (PS-MPs) are harmful to zebrafish hearts and induce male reproductive toxicity in mice. MCE offers Polystyrene products in solution packaging .
|
-
- HY-P9960
-
|
|
CD20
|
Inflammation/Immunology
|
|
Ocrelizumab (Ocrevus) is a humanized anti-CD20 monoclonal antibody. Ocrelizumab can induce B cell depletion and inhibit multiple sclerosis lesions in mice through antibody dependent cytotoxicity (ADCC) .
|
-
- HY-156936
-
|
|
Liposome
|
Others
|
|
RCB-02-4-8 is an ionizable cationic lipid that is used to form lipid nanoparticles (LNPs) to deliver mRNA. RCB-02-4-8 can improve the efficiency of lung transfection in mice .
|
-
- HY-106755
-
|
BWA589C
|
HIV
|
Infection
Cancer
|
|
Tucaresol is an orally bioavailable immunopotentiatory drug that show to enhance T-helper-cell activity, with the induction of increased IL-2 and IFN-γ levels in mice and humans. Tucaresol has anti-HIV effect .
|
-
- HY-105236
-
|
(Rac)-CI-977 free base
|
Others
|
Neurological Disease
|
|
(Rac)-Enadoline ((Rac)-CI-977 free base) is a selective K-opioid receptor agonist that stereoselectively antagonizes clonic seizures induced by slow intravenous injection of N-methyl-DL-aspartate in mice .
|
-
- HY-N12169
-
|
11,12-Epoxyjanthitrem B
|
Others
|
Neurological Disease
|
|
Janthitrem A (11,12-Epoxyjanthitrem B) is a natural product that can be isolated from Penicillium janthinellum. Janthitrem A induces tremors in mice and reduces weight gain and food consumption of porina (Wiseana cervinata) larvae .
|
-
- HY-129347
-
|
T-2636E
|
Antibiotic
Bacterial
|
Infection
|
|
Lankacyclinol A is an orally active antibiotic isolated from Streptomyces rochei. Lankacyclinol A has broad-spectrum antimicrobial activity against both Gram-positive and Gram-negative bacteria. Lankacyclinol A exhibits low toxicity in mice .
|
-
- HY-120450
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
CL-55 is an inhibitor for type three secretion system of Chlamydia trachomatis, that blocks the effector molecules delivery of bacteria into host cells. CL-55 ameliorates the C. trachomatis infection and inflammation in mice .
|
-
- HY-122604
-
|
|
Others
|
Neurological Disease
|
|
PF-DcpSi is a mRNA decapping scavenger enzyme (DcpS) inhibitor (IC50: 0.11 nM). PF-DcpSi (30 mg/kg,i.p.) ameliorates the disease phenotype in a mice model of spinal muscular atrophy (SMA) .
|
-
- HY-122655
-
|
|
P-selectin
|
Cardiovascular Disease
Inflammation/Immunology
|
|
HMCEF is an orally active P-selectin inhibitor and inhibits P-selectin expression. HMCEF blocks the interaction between P-selectin and natural ligands, such as PSGL-1. HMCEF inhibits thrombosis and inflammation in mice .
|
-
- HY-D0195R
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
Metabolic Disease
|
|
Acesulfame (potassium) (Standard) is the analytical standard of Acesulfame (potassium). This product is intended for research and analytical applications. Acesulfame potassium is an artificial sweetener. Acesulfame potassium (long-term) affects cognitive functions, potentially via altering neuro-metabolic functions in mice .
|
-
- HY-W062702
-
|
|
nAChR
|
Neurological Disease
|
|
BMS-933043 is a potent and selective α7 nACh receptor partial agonist. BMS-933043 attenuates the cognitive impairment in mice and can be utilized in research related to cognitive dysfunction in schizophrenia .
|
-
- HY-114853
-
|
|
PPAR
|
Metabolic Disease
|
|
BVT.13 is an orally active and selective PPARγ agonist with a maximal efficacy similar to that of Rosiglitazone (HY-17386). In addition, BVT.13 exhibits antidiabetic activity in ob/ob mice .
|
-
- HY-114542
-
|
|
Others
|
Others
|
|
LY 201409 is a compound with anticonvulsant activity that can antagonize maximal electroconvulsive-induced epileptic seizures, has mixed effects on epileptic seizures induced by a variety of chemical convulsants, and can also affect the behavior and sleep of mice.
|
-
- HY-P1624
-
|
ALX-0600
|
Nuclear Hormone Receptor 4A/NR4A
FXR
|
Inflammation/Immunology
|
|
Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
|
-
- HY-150725
-
|
|
IFNAR
TNF Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
|
-
- HY-P1624A
-
|
ALX-0600 TFA
|
Nuclear Hormone Receptor 4A/NR4A
FXR
|
Inflammation/Immunology
|
|
Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
|
-
- HY-150725C
-
|
|
TNF Receptor
IFNAR
|
Cancer
|
|
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
|
-
- HY-118285
-
|
|
mGluR
|
Neurological Disease
|
|
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
|
-
- HY-168214
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
|
-
- HY-19015
-
|
AT-2153
|
Others
|
Cancer
|
|
Probimane (AT-2153) is a potent anticancer agent. Probimane is effective against mouse tumors S37, S180, Lewis lung carcinoma, L1210 and human pulmonary adenocarcinoma heterotransplanted into nude mice .
|
-
- HY-109044R
-
|
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
Tapinarof (Standard) is the analytical standard of Tapinarof. This product is intended for research and analytical applications. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice .
|
-
- HY-N0840
-
|
(-)-Bruceantin; NCI165563; NSC165563
|
Others
|
Cancer
|
|
Bruceantin(NSC165563) is first isolated from Brucea javanica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
|
-
- HY-N1570
-
|
|
Salt-inducible Kinase (SIK)
|
Inflammation/Immunology
|
|
Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3 .
|
-
- HY-101194
-
|
Tin-protoporphyrin IX; Sn-Protoporphyrin; SnPPIX
|
Reactive Oxygen Species
|
Cancer
|
|
Tin protoporphyrin IX dichloride (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin protoporphyrin IX dichloride sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model .
|
-
- HY-N0031
-
|
|
Others
|
Inflammation/Immunology
|
|
Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation .
|
-
- HY-103017
-
|
|
IRAK
|
Infection
|
|
JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice .
|
-
- HY-P1241
-
-
- HY-133887
-
|
|
Antifolate
DNA/RNA Synthesis
|
Cancer
|
|
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent .
|
-
- HY-141866
-
|
|
Ceramidase
|
Neurological Disease
|
|
Acid Ceramidase-IN-1 is a potent and oral bioavailable acid ceramidase (AC, ASAH-1) inhibitor (hAC IC50=0.166 μM). Acid Ceramidase-IN-1 has excellent brain penetration in mice .
|
-
- HY-N3312
-
|
|
Endogenous Metabolite
|
Infection
|
|
Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-P99199
-
|
NI-0401
|
CD3
|
Inflammation/Immunology
|
|
Foralumab (NI-0401) is a potent, orally active human monoclonal antibody targeting the CD3. Foralumab modulates immune responses by human cells in NSG mice that were reconstituted with human hematopoietic stem cells .
|
-
- HY-N7944
-
|
|
Others
|
Cancer
|
|
Eucommiol is a natural product that can be isolated from the roasted leaves of E. ulmoides. Eucommiol inhibits growth of Molt 4B cells. Eucommiol reduces spontaneous activity and increases the sleep ratio in mice .
|
-
- HY-141638
-
|
Methyl-IQ
|
Others
|
Cancer
|
|
Me-IQ (Methyl-IQ), an orally active heterocyclic amine, is carcinogenic and mutagenic. Me-IQ is several hundred-fold more mutagenic in liver than in lung microsomal preparations from uninduced mice and rabbits .
|
-
- HY-133800
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Volvaltrate B is an anticancer agent, iridoid, can be obtained from the root of valerian (Valeriana officinalis). Volvaltrate B is effective against ovarian tumors in female mice. Volvaltrate B has the potential to study cancer .
|
-
- HY-P5437
-
|
|
PKC
|
Others
|
|
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
|
-
- HY-P10032
-
-
- HY-122518
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
8-Deazafolic acid is an antimicrobial drug for the folate-dependent bacteria, Streptococcus faecium (ATCC 8043) and Lactobacillus casei (ATCC 74691). 8-Deazafolic acid has activity against lymphoid leukemia L1210 in mice .
|
-
- HY-116392B
-
|
|
Glucosylceramide Synthase (GCS)
|
Cancer
|
|
DL-threo-PDMP hydrochloride is the hydrochloride form of DL-threo-PDMP that is a competitive glucosylceramide synthase (GCS) inhibitor. DL-threo-PDMP resensitizes refractory testicular germ cell tumors and epithelial ovarian cancer orthoxenografts to cisplatin in mice .
|
-
- HY-162396
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .
|
-
- HY-119206
-
|
|
Others
|
Others
|
|
Sulbenicillin is an antibiotic that, in a study of its activity against Pseudomonas aeruginosa infection in mice, showed differences in activity against certain strains compared to other antibiotics, and activity against gentamicin-resistant strains was affected by the strain's own resistance.
|
-
- HY-121007
-
|
Web2170
|
Others
|
Others
|
|
Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guinea pigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
|
-
- HY-W099437
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Diethylene glycol monobutyl ether acetate is an orally available high molecular weight glycol ether solvent that can be used as a coalescing agent for polyvinyl acetate (latex) coatings, the acute oral LD in mice and rats is about 7 g/kg .
|
-
- HY-155551
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 46 (compound 7h) is an anti-inflammatory agent with nitric oxide (NO) inhibitory effect. Anti-inflammatory agent 46 binds to iNOS with low energies, inhibits swelling in mice (at dose of 10 mg/kg) .
|
-
- HY-133898
-
|
TAK-925
|
Orexin Receptor (OX Receptor)
|
Others
|
|
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
|
-
- HY-N5106
-
|
|
Apoptosis
|
Cancer
|
|
(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice .
|
-
- HY-111320
-
|
|
Bacterial
Antibiotic
|
Cancer
|
|
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
|
-
- HY-P1241A
-
-
- HY-121271
-
|
|
Others
|
Inflammation/Immunology
|
|
Kadsurin, a natural compound from the stems of Kadsura heteroclita (Schizandraceae), results in significant decreases of CCL4- induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice .
|
-
- HY-144232
-
|
|
Others
|
Cancer
|
|
Anticancer agent 28 showed good antitumor activity in H22 allogeneic mice in vivo. Its potency in K562 cells was 50 times that of oridonin, and its < b > IC < sub > 50 < / sub > < / b > value was 0.09 μ M。
|
-
- HY-B0430B
-
|
(±)-Pantothenate; (±)-Vitamin B5
|
Others
|
Neurological Disease
Metabolic Disease
|
|
(±)-Pantothenic acid ((±)-Pantothenate), a B-vitamin, is an essential vitamin required for the biosynthesis of coenzyme A (CoA) in mammalian cells. Pantothenic acid has protective activity against valproic acid (VPA)-induced neural tube defects (NTD) in CD-1 mice .
|
-
- HY-P3707
-
|
|
Apoptosis
|
Cancer
|
|
Tumor targeted pro-apoptotic peptide (CNGRC-GG-D(KLAKLAK)2) is an anti-tumor peptide. Tumor targeted pro-apoptotic peptide disrupts mitochondrial membranes and promotes apoptosis, showing anticancer activity in mice .
|
-
- HY-148232
-
|
|
CCR
|
Inflammation/Immunology
|
|
BAY-3153 is a selective CCR1 (C-C motif chemokine receptor 1) antagonist (human IC50=3 nM; rat IC50=11 nM; mice IC50=81 nM) .
|
-
- HY-N2867
-
|
|
Others
|
Cancer
|
|
Andrographiside is a labdane diterpenoid glucoside that can be isolated from the leaves of Andrographis paniculata Nees. Andrographiside has antihepatotoxic and antioxidative effects. Andrographiside shows protective effects on mice with hepatotoxicity induced by carbon tetrachloride or tert-butylhydroperoxide (tBHP) .
|
-
- HY-D0195S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Acesulfame-d4 potassiumis the deuterium labeledAcesulfame (potassium)(HY-D0195) . Acesulfame potassium is an artificial sweetener. Acesulfame potassium (long-term) affects cognitive functions, potentially via altering neuro-metabolic functions in mice .
|
-
- HY-149403
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Others
|
|
J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway .
|
-
- HY-155966
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-19 (Compound 32) is a selective and orally active CDK2 inhibitor (Ki: 0.18 nM). CDK2-IN-19 shows anticancer activity in mice bearing OVCAR3 tumors .
|
-
- HY-103567
-
|
|
mGluR
|
Neurological Disease
|
|
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-107527
-
|
|
GlyT
|
Neurological Disease
|
|
Org 25543 hydrochloride is a selective and irreversible GlyT2 inhibitor (IC50: 16 nM). Org 25543 hydrochloride has analgesia effect. Org 25543 hydrochloride ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice .
|
-
- HY-114992
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
2-Propyl-2-pentenoic acid is a metabolite of Valproic acid (HY-10585). 2-Propyl-2-pentenoic acid has a facilitating action on the acquisition of conditioned behavior with negative reinforcement in mice .
|
-
- HY-D2095
-
|
|
Fluorescent Dye
|
Cancer
|
|
Medical fluorophore 33 is a novel quinoline-isoquinoline salt. Medical fluorophore 33 exhibits a strong fluorescent signal, good microsomal stability and high biocompatibility in vivo. Medical fluorophore 33 has antitumor activity in colorectal cancer mice .
|
-
- HY-156842
-
|
|
Amyloid-β
|
Neurological Disease
|
|
MCAAD-3 is a near-infrared Aβ imaging probe with blood-brain barrier penetrability. MCAAD-3 has a strong affinity for Aβ polymers (Ki >106 nM) and can label Aβ plaques in the brains of transgenic mice .
|
-
- HY-122309
-
|
|
Antibiotic
|
Infection
|
|
A-71497 is the 3-formyl derivative of the antibiotic Tosufloxacin (HY-B1802). A-71497 can produce high plasma levels of tosufloxacin upon both oral and subcutaneous administration to mice .
|
-
- HY-P10102
-
|
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury .
|
-
- HY-157430
-
|
|
Epigenetic Reader Domain
|
Neurological Disease
|
|
BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the Ki of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice .
|
-
- HY-163300
-
-
- HY-114784
-
|
Ingamine
|
Influenza Virus
|
Infection
|
|
Ingavirin (Ingamine) exhibits broad spectrum antiviral activities against human respiratory viruses, such as influenza virus A (IVA), human parainfluenza virus (hPIV) and human adenovirus (AdV). Ingavirin exhibits no toxixcity to mice at the dose of 3000 mg/kg .
|
-
- HY-B2085
-
|
Arsthinol; Balarsen
|
Others
|
Cancer
|
|
Arsthinenol is an orally active antitumor agent, that exhibits cytotoxicity in U87MG cells with an IC50 of 31.6 μM. Arsthinenol forms complex with cyclodextrin, inhibits the tumor growth and improves the survival rates of U87MG xenograft mice .
|
-
- HY-103567A
-
|
|
mGluR
|
Neurological Disease
|
|
Desmethyl-YM-298198 is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-126645
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
Atelopidtoxin (zetekitoxin) is a toxin (LD50=0.016 mg/kg for mice), which can be isolated from Panamanian frog Atelopus zeteki. Atelopidtoxin causes hypotension and ventricular fibrillation in rabbits. Atelopidtoxin an inhibitor for sodium channel .
|
-
- HY-117231
-
|
|
Others
|
Cancer
|
|
RM 06 is an immunomodulator with a peptidyl hypoxanthine structure that significantly reduces the number of lung metastases of B16 melanoma cells in mice after lethal irradiation and bone marrow reconstitution by stimulating the activity of natural killer (NK) cells .
|
-
- HY-158649
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
Fasnall benzenesulfonate is the benzenesulfonate salt form of Fasnall (HY-121250). Fasnall benzenesulfonate is the inhibitor for fatty acid synthase (FASN) with IC50 of 3.7 μM. Fasnall benzenesulfonate inhibits the proliferation and induces apoptosis in breast cancer cells. Fasnall benzenesulfonate exhibits antitumor efficacy in mice .
|
-
- HY-N0700R
-
|
|
GABA Receptor
|
Neurological Disease
|
|
alpha-Asarone (Standard) is the analytical standard of alpha-Asarone. This product is intended for research and analytical applications. alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.
|
-
- HY-10845
-
|
|
Others
|
Others
|
|
CGI-17341 is a 5-nitroimidazole antibacterial agent that has the activity of inhibiting sensitive and multidrug-resistant strains of Mycobacterium tuberculosis in vitro and prolonging the survival time of mice infected with Mycobacterium tuberculosis in vivo in a dose-dependent manner.
|
-
- HY-W018791
-
|
DDB
|
HBV
Autophagy
Cytochrome P450
Atg8/LC3
p62
P-glycoprotein
|
Infection
Cardiovascular Disease
Cancer
|
|
Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR) .
|
-
- HY-160887
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
|
-
- HY-156991
-
|
NODA-GA-NHS ester
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
|
Cancer
|
|
NODAGA-NHS (NODA-GA-NHS ester) is a [64]Cu chelator and the dissociated form of DOTA-trastuzumab in vivo. NODAGA-NHS was added in 0.1 M borate buffer at a ratio of 5/20/100 and was able to effectively bind trastuzumab (10 mg/mL) (4°C, 20 h). The copper content of the [64]Cu-NODAGA-trastuzumab was up to 80%. After blood was drawn from the caudal vein of mice, [64]Cu-NODAGA-trastuzumab was injected and showed good tumor uptake in mice expressing HER2 tumors, showing good PET imaging tracking ability.
|
-
- HY-101317A
-
|
SB-205607
|
Opioid Receptor
|
Metabolic Disease
|
|
TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
|
-
- HY-14447
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system .
|
-
- HY-103316A
-
Ned 19
2 Publications Verification
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM . Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .
|
-
- HY-110303
-
|
XAC dihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-P1290A
-
|
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice .
|
-
- HY-120083
-
-
- HY-122365
-
|
Inositol niacinate; Hexanicit
|
Others
|
Cardiovascular Disease
|
|
Inositol nicotinate (Hexanicit) has vasodilating effects and can be used in research on peripheral arterial disease, showing efficacy when taken orally. Inositol nicotinate does not significantly improve triglyceride levels in mice induced by biphenyl esters .
|
-
- HY-P9944
-
|
MEDI 493
|
RSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Palivizumab (MEDI 493) is a humanized monoclonal antibody against respiratory syncytial virus (RSV). Palivizumab can bind to RSV F protein with a Kd value of 1.4 nM. Palivizumab can prevent respiratory syncytial virus infection in cotton mice .
|
-
- HY-100426A
-
|
MKC242
|
5-HT Receptor
|
Neurological Disease
|
|
Osemozotan hydrochloride (MKC242) is a selective 5-HT1A receptor agonist. Osemozotan hydrochloride decreases the number of c-Fos-positive cells caused by MAMP in mice. Osemozotan hydrochloride can be used for the research of depressive disorder .
|
-
- HY-12095
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
|
-
- HY-N9173
-
|
|
Others
|
Inflammation/Immunology
|
|
Cupressuflavone is a natural product that can be found in Cupressus macrocarpa. Cupressuflavone exhibits anti-inflammatory and antiulcerogenic activities. Cupressuflavone also show protective effects against CCl4-induced hepato- and nephrotoxicity in mice .
|
-
- HY-114683
-
|
|
Others
|
Cardiovascular Disease
|
|
KS370G is an orally active hypoglycemic and cardiovascular protective agent. KS370G improves left ventricular hypertrophy and function in pressure-overload mice heart. KS370G reduces renal obstructive nephropathy .
|
-
- HY-155653
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) .
|
-
- HY-N12127
-
|
|
Others
|
Others
|
|
Gymnoside I (compound 1) is a glycosidoxybenzyl 2-isobutylmalic acid. Gymnoside I shows antiallergic activity in passive cutaneous allergic reaction (PCA) in mice. Gymnoside I can be used in research to treat asthma, neurasthenia and chronic hepatitis .
|
-
- HY-P5883
-
|
tatM2NX
|
TRP Channel
|
Neurological Disease
|
|
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. TAT-M2NX can be used to study ischemic neuronal damage .
|
-
- HY-P4885
-
|
AβpE3-40
|
Amyloid-β
|
Neurological Disease
|
|
Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice .
|
-
- HY-P5762
-
|
PNX-14
|
GnRH Receptor
|
Neurological Disease
|
|
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia .
|
-
- HY-138291
-
|
|
Others
|
Inflammation/Immunology
|
|
Ethoxyquin dimer is a dimer of Ethoxyquin (HY-B1425). Ethoxyquin dimer is an antioxidant. Ethoxyquin dimer can more readily accumulate in liver and adipose tissue compared with Ethoxyquin. Ethoxyquin above 10?mg/kg shows hepatotoxicity in mice .
|
-
- HY-N2953
-
|
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
|
Borapetoside E can be isolated from T. crispa. Borapetoside E improves hyperglycemia, insulin resistance, hepatic steatosis, hyperlipidemia, and oxygen consumption in obese mice. Borapetoside E also inhibits SREBPs expression in the liver and adipose tissue .
|
-
- HY-156276
-
|
|
PPAR
|
Metabolic Disease
|
|
SP4e is an activator of PPAR-γ, with the EC50 of 739 nM in HK-2 cells. SP4e reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice .
|
-
- HY-156277
-
|
|
PPAR
|
Metabolic Disease
|
|
SP4f is an activator ofPPAR-γ, with the EC50 of 826 nM in HK-2 cells. SP4f reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice .
|
-
- HY-40156
-
|
|
Bacterial
|
Infection
|
|
5-Fluoroindole is an antibacterial agent, that inhibits Mycobacterium tuberculosis with a MIC of 4.7 μM. 5-Fluoroindole exhibits metabolic stability in rat liver microsomes. 5-Fluoroindole exhibits anti-tuberculosis efficacy in mice .
|
-
- HY-W590683
-
|
|
Liposome
CRISPR/Cas9
|
Others
|
|
9A1P9 is a multi-tail ionizable cationic phospholipid. 9A1P9 induces membrane destabilization. 9A1P9 can be used for CRISPR-Cas9 gene editing in mice .
|
-
- HY-121582
-
|
(E)-EPH 116
|
Others
|
Cancer
|
|
(E)-SI-2 is an isomer of SI-2, an inhibitor of the steroid receptor coactivator SRC-3. SI-2 has anticancer activity and increases the number of cytotoxic immune cells in mice with breast cancer .
|
-
- HY-110262
-
|
|
MAP3K
p38 MAPK
|
Inflammation/Immunology
|
|
MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation .
|
-
- HY-121182
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Chalcomycin is a macrolide antibiotic, which exhibits antimicrobial activities against gram-positive Staphylococcus aureus and Streptococcus pyogenes. Chalcomycin protects mice from infection with a variety of staphylococci and streptococc, without significant toxicity (LD50 >2500 mg/kg) .
|
-
- HY-113086
-
|
16:1(9Z) CE; 16:1(9Z) Cholesterol ester; Cholesterol Palmitoleate
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Cholesteryl palmitoleate is a cholesterol ester. Plasma levels of cholesteryl palmitoleate are increased in ApoE-/- mice exposed to cigarette smoke and in pediatric patients with biliary atresia. Cholesteryl palmitoleate has been used as a standard for the identification of cholesterol esters in human meibomian gland secretions.
|
-
- HY-101139B
-
|
XAC trihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener trihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-165677
-
|
|
Others
|
Neurological Disease
|
|
C22 Galactosylceramide is a sphingolipid present in the central nervous system, exhibiting elevated levels in the spinal cord of mice on a methionine-restricted diet, while not affecting the brain or liver; furthermore, it has been identified in the postmortem hippocampus of Alzheimer's disease patients.
|
-
- HY-167856
-
|
|
GPR88
|
Neurological Disease
|
|
RTI-122 is a brain-penetrant and potent GPR88 agonist with good metabolic stability (half-life of 5.8 h in mice) and a cAMP EC50 of 11 nM. RTI-122 can be utilized in research on excessive drinking .
|
-
- HY-108352
-
|
VCE 004
|
Topoisomerase
|
Cancer
|
|
HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo .
|
-
- HY-114221
-
|
UR13870
|
p38 MAPK
|
Inflammation/Immunology
|
|
Org 48762-0 is a potent, orally active and selective p38 inhibitor with EC50 of 0.1 μM. Org 48762-0 reduces LPS-induced TNFα release and prevents bone damage in collagen-induced arthritis in mice .
|
-
- HY-B0892
-
|
Benzenemethanol
|
Cytochrome P450
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice .
|
-
- HY-109120
-
|
A4250
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
|
Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
|
-
- HY-120813
-
|
URB913
|
Others
|
Inflammation/Immunology
|
|
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA . ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats .
|
-
- HY-127039
-
|
|
Ser/Thr Protease
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
|
Antipain is a protease inhibitor isolated from Actinomycetes. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain restricts uterine DNA synthesis and function in mice .
|
-
- HY-127034
-
|
|
Ser/Thr Protease
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
|
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice .
|
-
- HY-P1290
-
|
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice .
|
-
- HY-10080
-
|
GMX1777; EB-1627
|
NAMPT
|
Cancer
|
|
Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis .
|
-
- HY-P1149
-
|
Epithalon; Epithalamin
|
Telomerase
|
Neurological Disease
Cancer
|
|
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-129087
-
|
|
Apoptosis
|
Cancer
|
|
BC-1258, an F-box/LRR-repeat protein 2 (FBXL2) activator, can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells, and profoundly inhibits tumor formation in mice .
|
-
- HY-135042
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model .
|
-
- HY-147013
-
|
|
Influenza Virus
Orthopoxvirus
|
Infection
|
|
Caprochlorone has antiviral activity against orthopoxvirus. Caprochlorone can inhibit cell penetration by virus, also delays release of newly formed virus from the cell. Caprochlorone decreases the titers of influenza virus in infected-mice lungs .
|
-
- HY-147335
-
|
|
Others
|
Cardiovascular Disease
|
|
6,9,12,15-Hexadecatetraenoic acid-ethyl ester is an orally active n-1PUFA. 6,9,12,15-Hexadecatetraenoic acid-ethyl ester intake can reduce plasma triglyceride content in mice .
|
-
- HY-P99354
-
|
Anti-Human CTLA4xLAG3
|
LAG-3
|
Inflammation/Immunology
Cancer
|
|
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activates T cells in NSG mice. Bavunalimab can be used for the research of cancer .
|
-
- HY-N4063
-
|
|
FXR
|
Inflammation/Immunology
|
|
Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation .
|
-
- HY-145721A
-
|
GED-0301 sodium
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
|
-
- HY-162683
-
|
|
CDK
|
Neurological Disease
Cancer
|
|
(S)-PHA533533 is a cyclin-dependent kinase 2 (CDK2) inhibitor. (S)-PHA533533 shows anti-tumor activity and can induce widespread neuronal UBE3A expression in angelman syndrome model mice .
|
-
- HY-134579
-
|
|
Farnesyl Transferase
|
Inflammation/Immunology
|
|
Chaetomellic acid A can be isolated from Chaetomella acutiseta. Chaetomellic acid A is a specific inhibitor of farnesyl-protein transferase. Chaetomellic acid A decreases oxidative stress-induced apoptosis in cells. Chaetomellic acid A reduces renal damage after unilateral ureteral obstruction (UUO) in mice .
|
-
- HY-N0546R
-
|
|
CaSR
|
Metabolic Disease
|
|
Ligustroflavone (Standard) is the analytical standard of Ligustroflavone. This product is intended for research and analytical applications. Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice .
|
-
- HY-164478
-
|
|
PARP
|
Cancer
|
|
G-631 is a selective inhibitor for tankyrase. G-631 inhibits tankyrase auto-PARsylation (poly ADP ribosylation) with an IC50 of 7 nM, and inhibits Wnt signaling pathway. G-631 exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-115826
-
|
|
Others
|
Cancer
|
|
AB-163 is an alkylating agent with anti-tumor activity. AB-163 exerts LD50s of 198 (p.o.) and 159 (i.p.) mg/kg in ICR/Ha male mice and can be utilized in cancer research .
|
-
- HY-100935
-
|
CL 263780; (±)-2-Amino-5-[1-hydroxy-2-[(1-methylethyl)amino]ethyl]benzonitrile
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Cimaterol (CL 263780) is a β-adrenergic agonist on energy metabolism in ob/ob mice . The Kd for Cimaterol binding to the L6 β-receptor is 26 nM which is compatible with its EC50 for the stimulation of protein synthesis (approx 5 nM) .
|
-
- HY-106591A
-
|
Vinylcyclohexene diepoxide
|
Apoptosis
|
Cardiovascular Disease
|
|
4-Vinylcyclohexene dioxide is a metabolite of 4-vinylcyclohexene that can specifically destroy oocytes in primordial and primary follicles of rats and mice. 4-Vinylcyclohexene dioxide induces apoptosis in rat cells is associated with activation of a caspase-mediated cascade .
|
-
- HY-124322
-
|
|
Beta-secretase
|
Neurological Disease
Inflammation/Immunology
|
|
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
|
-
- HY-14393S
-
|
Frangula emodin-d4
|
Isotope-Labeled Compounds
SARS-CoV
Casein Kinase
Autophagy
11β-HSD
|
Cancer
|
|
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
|
-
- HY-155998
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-11 (Compound 3i) is a NF-κB inhibitor. NF-κB-IN-11 inhibits TNF-α induced activation of NF-κB pathway, and inhibits nuclear translocation of NF-κB. NF-κB-IN-11 down-regulates the expression levels of phosphor-IKK, IκBα, and NF-κB p65. NF-κB-IN-11 has anti-inflammatory activity, and alleviates dextran sulfate sodium-induced colitis in mice. NF-κB-IN-11 (p.o.) shows a MTD more than 1852 mg/kg in mice acute toxicity assay .
|
-
- HY-12191
-
|
|
Histamine Receptor
|
Metabolic Disease
|
|
A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation .
|
-
- HY-120912
-
-
- HY-131954
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT3 antagonist 4 is a 5-HT3 receptor (5HT3R) antagonist. 5-HT3 antagonist 4 prevents diabetes-induced depressive phenotypes in mice .
|
-
- HY-10367A
-
|
CI-1033 dihydrochloride; PD-183805 dihydrochloride
|
EGFR
Orthopoxvirus
|
Infection
Cancer
|
|
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice .
|
-
- HY-B2194
-
|
|
DNA Methyltransferase
|
Metabolic Disease
Cancer
|
|
γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
|
-
- HY-N3522
-
|
|
Others
|
Inflammation/Immunology
|
|
Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific IgG2a and IgG2b antibody in the ovalbumin (OVA)-immunized mice .
|
-
- HY-14364
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
|
-
- HY-110171
-
iMDK
2 Publications Verification
|
PI3K
|
Cancer
|
|
iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
- HY-108234
-
|
VU 255035
|
mAChR
|
Neurological Disease
|
|
VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations .
|
-
- HY-146190
-
|
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Callophycin A, a red seaweed derived metabolite, possessing potent activity against Candida albicans with MIC of 62.5~250 mg/L. Callophycin A significantly reduces fungal burden of vaginal candidiasis induced mice, also decreases inflammatory response and immune molecules .
|
-
- HY-D0873
-
|
EPPS
|
Amyloid-β
|
Neurological Disease
|
|
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier .
|
-
- HY-P99216
-
|
PF-04360365; RN 1219
|
EGFR
|
Neurological Disease
|
|
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease .
|
-
- HY-P99908
-
|
NT-17
|
Interleukin Related
|
Cancer
|
|
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4 + and CD8 + cells in both human and mice. Efineptakin alfa can be used for glioblastoma research .
|
-
- HY-148560
-
|
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
ccc_R08 is a non-cytotoxic and orally active cccDNA inhibitor that reduces cccDNA levels in the liver of HBV-infected mice. ccc_R08 can be used in the study of HBV virus (hepatitis B virus) infection .
|
-
- HY-155652
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice .
|
-
- HY-107504
-
|
|
mGluR
|
Neurological Disease
|
|
VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .
|
-
- HY-155329
-
|
|
HDAC
|
Inflammation/Immunology
|
|
GK718 is a HDAC1/3 inhibitor (IC50: 259 and 139 nM respectively). GK718 increased acetylated histone H3 level in cells. GK718 inhibits Bleomycin (HY-108345) induced pulmonary fibrosis in mice .
|
-
- HY-121431
-
|
|
Others
|
Inflammation/Immunology
|
|
FR-901235 is a new type of immunoactive substance produced by an imperfect fungus, Paecilomyces carneus F-4882. FR-901235 partially restored the impaired delayed-type hypersensitivity to sheep red blood cells in tumor-bearing mice .
|
-
- HY-P10200
-
|
|
Bacterial
|
Infection
|
|
CP7-FP13-2 is a peptide with antivirulence factor and antibacterial activity. CP7-FP13-2 inhibits the formation of Staphylococcus aureus biofilm and has good antibacterial efficacy in mice .
|
-
- HY-158006
-
|
|
MetAP
|
Cancer
|
|
SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
|
-
- HY-120225
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
NJK14047 inhibits p38 MAPK and the differentation of naive T-cells to Th1 and Th17 cells. NJK14047 ameliorates the collage-induced rheumatoid arthritis and Imiquimod (HY-B0180)-induced psoriasis in mice .
|
-
- HY-112680
-
|
|
G-quadruplex
|
Cancer
|
|
Carboxypyridostatin is a G-quadruplex ligand that has a highly molecular specificity to RNA on DNA G4s, and can reduce the proliferation of adult neural stem cells and progenitor cells derived from the subventricular zone of adult mice in vitro and in vivo .
|
-
- HY-158776
-
|
|
Parasite
|
Infection
|
|
SLU-10482 is an orally active anti-parasitic agent, that inhibits Cryptosporidium parvum with an IC50 of 0.0687 μM. SLU-10482 exhibits anti-infective efficacy in C. parvum infected mice with an AC50 of 0.0686 μM .
|
-
- HY-161937
-
|
|
Topoisomerase
Bacterial
|
Infection
|
|
Antibacterial agent 236 (Compound 4l) is an orally active inhibitor for DNA gyrase and topoisomerase IV (IC50 is 3.2 and 300 nM in Staphylococcus aureus), and exhibits board-spectrum antibacterial activity. Antibacterial agent 236 exhibits good pharmacokinetic properties in mice .
|
-
- HY-160237
-
|
|
TGF-β Receptor
|
Cancer
|
|
HYL001 (compund 338) is a potent inhibitor of TGFβ receptor 1 (ALK5) that is approximately 9 times more potent than the structurally related compound Galunisertib (HY-13226) and is able to eliminate liver metastases established in mice .
|
-
- HY-162477
-
|
|
Cathepsin
Apoptosis
|
Cancer
|
|
TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
|
-
- HY-B2241A
-
|
Aluminum potassium sulfate dodecahydrate, for cell culture
|
Biochemical Assay Reagents
|
Others
|
|
Potassiumalum, for cell culture (Aluminum potassium sulfate dodecahydrate, for cell culture) is an egg white adjuvant that can induce allergic reactions in mice; it can also be used for bacterial staining. Potassiumalum, for cell culture is a biomaterial or organic compound that can be used in life science research .
|
-
- HY-13513
-
U-104
5 Publications Verification
SLC-0111
|
Carbonic Anhydrase
|
Cancer
|
|
U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model .
|
-
- HY-14530
-
|
AG 2037
|
Antifolate
|
Cancer
|
|
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice .
|
-
- HY-101030
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-107734
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
Endocrinology
|
|
L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure .
|
-
- HY-N7047
-
|
8-Epidiosbulbin E acetate
|
Bacterial
|
Infection
|
|
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice .
|
-
- HY-110120
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect .
|
-
- HY-N0506
-
|
|
Interleukin Related
|
Neurological Disease
|
|
Rosarin is a cinnamyl alcohol?glycoside isolated from?Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1?β, and TNF- α in the kidney and prefrontal cortex of brain in mice? .
|
-
- HY-133533
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice .
|
-
- HY-N7514
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice .
|
-
- HY-112680A
-
|
|
G-quadruplex
|
Cancer
|
|
Carboxy pyridostatin trifluoroacetate salt is a G-quadruplex ligand that has a highly molecular specificity to RNA on DNA G4s, and can reduce the proliferation of adult neural stem cells and progenitor cells derived from the subventricular zone of adult mice in vitro and in vivo .
|
-
- HY-N9536
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect .
|
-
- HY-132302
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-103639
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis .
|
-
- HY-156566
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
|
-
- HY-N12141
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome .
|
-
- HY-156422
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
KPZ560 is a potent inhibitor of HDAC1 and HDAC2, with IC50s of 12 nM and 68 nM, respectively. KPZ560 can increase in the spine density of granule neuron dendrites of mice and inhibitor cell growth of breast cancer cell line MCF .
|
-
- HY-117603
-
|
|
Glucokinase
|
Infection
|
|
CM-10-18 is a potent and orally active inhibitor of both α-glucosidases I and II in vitro and in treated animals. CM-10-18 inhibits DENV infection of cultured human cells and reduces the peak viremia of DENV in mice .
|
-
- HY-149719
-
|
|
Ferroptosis
|
Metabolic Disease
|
Ferroptosis-IN-4 (compound 6k) is a ferroptosis inhibitor with EC50 value of 20 μM. Ferroptosis-IN-4 has no obvious cytotoxicity. Ferroptosis-IN-4 has a protective effect in glycerol-induced RM-AKI mice with alleviating kidney dysfunction .
|
-
- HY-157326
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-6 (compound 17d) is a potent and selective inhibitor of hMAO-B with an IC50 of 67.02 nM. hMAO-B-IN-6 significantly improves Scopolamine (HY-N0296)-induced cognitive impairment in AD mice .
|
-
- HY-X0009A
-
|
|
CDK
|
Cancer
|
|
JSH-009 dimaleate (Compound 1) is a potent and highly selective CDK9 inhibitor with an IC50 of 0.928 nM. JSH-009 can effectively inhibit the growth of subcutaneous tumor (cute myelogenous leukemia MV4-11) mice .
|
-
- HY-118426
-
|
(Rac)-IND 58359; (Rac)-R115777
|
Others
|
Cancer
|
|
(Rac)-Tipifarnib ((Rac)-IND 58359; (Rac)-R115777) is a potent farnesyl protein transferase inhibitor that specifically targets the pro-tailation process of Ras proteins. (Rac)-Tipifarnib showed significant in vivo antitumor effects after oral administration to mice .
|
-
- HY-117172
-
|
|
Others
|
Metabolic Disease
|
|
CP320626 is a potent inhibitor of human liver glycogen phosphorylase (IC50=205 nM). CP320626 reduces blood glucose in diabetic mice without changing plasma insulin levels. CP320626 can be used in the study of type 2 diabetes .
|
-
- HY-N1472
-
|
|
Apoptosis
Reactive Oxygen Species
PPAR
GSK-3
Tau Protein
Ras
TGF-β Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways .
|
-
- HY-133079
-
|
tetra-isopalmitoyl Ascorbic acid; IPAA; Tetrahexyldecyl Ascorbate
|
Prostaglandin Receptor
|
Endocrinology
|
|
Ascorbyl tetraisopalmitate is a lipophilic derivative of vitamin C (L-ascorbic acid). It protects against UVB-, hydrogen peroxide-, or tert-butyl hydroperoxide-induced decreases in cell viability in HaCaT keratinocytes when used at a concentration of 100 μM.1 Ascorbyl tetraisopalmitate (20 μM) decreases IL-1α and prostaglandin E2 production in unstimulated and UVB-stimulated HaCaT keratinocytes. Topical application of ascorbyl tetraisopalmitate (1%) increases viable epidermis thickness, stratum corneum water content, and skin smoothness and decreases skin roughness in hairless mice.2 Formulations containing ascorbyl tetraisopalmitate have been used in cosmetic products as skin-lightening agents.
|
-
- HY-125327
-
|
|
Others
|
Metabolic Disease
|
|
YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.
|
-
- HY-100827
-
|
LF22-0542
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
|
-
- HY-B0448R
-
|
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin (Standard) is the analytical standard of Phenytoin. This product is intended for research and analytical applications. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-13818
-
Stattic
Maximum Cited Publications
173 Publications Verification
|
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727) . Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .
|
-
- HY-101954
-
|
ORI-9020; SB-9000
|
HBV
|
Infection
|
|
Inarigivir (ORI-9020) is a dinucleotide antiviral drug that can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) act as a RIG-I agonist to activate cellular innate immune responses .
|
-
- HY-N3015
-
|
|
Others
|
Metabolic Disease
|
|
Bruceine E is a quassinoid from seeds of Brucea javanica (L.) Merr, exhibiting hypoglycemia effect . Bruceine E exhibits blood glucose lowering effect in both nondiabetic mice and Streptozotocin (STZ (HY-13753))-induced diabetic rats at lower dose .
|
-
- HY-P1149A
-
|
Epithalon TFA; Epithalamin TFA
|
Telomerase
|
Neurological Disease
Cancer
|
|
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-N6608
-
|
Eserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning .
|
-
- HY-131034
-
|
|
Wnt
|
Others
|
|
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats .
|
-
- HY-110171A
-
|
|
PI3K
|
Cancer
|
|
iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
- HY-W008151
-
|
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
Diphenyl Phosphate inhibits growth and energy metabolism in zebrafish and mice in a sex-specific manner. Diphenyl Phosphate can inhibit the activity of SDH (respiratory complex II), reduce the expression of CPT1 and disrupts the integrity of the mitochondrial membrane. Diphenyl Phosphate may be used in research on metabolic diseases .
|
-
- HY-145119
-
|
|
SARS-CoV
|
Infection
|
|
GS-621763 is an orally available precursor to GS-441524 that exhibits anti-SARS-CoV-2 viral activity in mice. GS-621763 reduces viral load to undetectable levels in ferrets infected with SARS-CoV-2 .
|
-
- HY-P3304
-
|
|
GHSR
|
Neurological Disease
Cancer
|
|
MR 409 is a selected growth hormone-releasing hormone (GHRH) agonist. MR 409 has remarkable neuroprotective effects through enhancing endogenous neurogenesis in cerebral ischemic mice. MR 409 also inhibits the in vivo growth of lung cancer .
|
-
- HY-145721
-
|
GED-0301
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
|
-
- HY-147529
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice .
|
-
- HY-130136
-
|
|
Ser/Thr Protease
|
Others
|
|
TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice .
|
-
- HY-N4024
-
|
|
Others
|
Inflammation/Immunology
|
|
Hyptadienic acid is a triterpene acid that can be isolated from the leaves of Perilla frutescens. Hyptadienic acid inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice with an ID50 value of 0.13 mg/ear. Hyptadienic acid can be used for the research of inflammation .
|
-
- HY-P5117
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice .
|
-
- HY-149298
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice .
|
-
- HY-N11911
-
|
(-)-Verazine
|
Fungal
|
Infection
Neurological Disease
|
|
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases .
|
-
- HY-156117
-
|
|
STING
|
Cancer
|
|
LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC50=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice .
|
-
- HY-101220
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
RMI-61140 is an orally active neuroleptics. RMI-61140 decreases spontaneous motility and muscle tone in mice. RMI-61140 increases barbit urate-induced sleep and causes eyelid ptosis. RMI-61140 can be used for schizophrenia research .
|
-
- HY-W016145
-
|
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
L-Glutamic acid monosodium hydrate is a nutritional additive and flavoring agent. L-Glutamic acid monosodium hydrate can reduce obesity and induce metabolic disorders associated with oxidative stress. L-Glutamic acid monosodium hydrate induces oxidative stress,DNA damage and apoptosis in the liver and brain tissues of mice .
|
-
- HY-157085
-
|
|
HSP
|
Cancer
|
|
BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
|
-
- HY-P10032A
-
-
- HY-161281
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with IC50 of 0.52 μM. α-Glucosidase-IN-49 has oral bioactivity that can reduce blood glucose and improve glucose tolerance in mice .
|
-
- HY-158093
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages .
|
-
- HY-160769
-
|
|
YAP
|
Others
|
|
NIBR-LTSi is an orally active and selective LATS kinase inhibitor. NIBR-LTSi can activate YAP signaling. NIBR-LTSi promotes stem cell proliferation, maintains stemness and blocks differentiation. NIBR-LTSi accelerates liver regeneration following extended hepatectomy in mice .
|
-
- HY-160818
-
|
|
Sirtuin
|
Cancer
|
|
MC3138 is a selective SIRT5 activator. MC3138 has antitumor activity on human PDAC cells, with IC50 values of 25.4-236.9 μM. MC3138 combined with Gemcitabine (HY-17026) significantly inhibits tumor growth in mice .
|
-
- HY-123171
-
|
|
Others
|
Metabolic Disease
|
|
ASP8497 is a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor that reduces blood glucose levels and increases plasma active GLP-1 and insulin levels without causing hypoglycemia in fasted normal mice. ASP8497 can be utilized for antihyperglycemic research .
|
-
- HY-B0448AR
-
|
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin (sodium) (Standard) is the analytical standard of Phenytoin (sodium). This product is intended for research and analytical applications. Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-12995
-
|
|
FLAP
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BI 665915 is an orally active and potent 5-lipoxygenase-activating protein (FLAP) inhibitor. BI 665915 inhibits FLAP production that blocks LTB4 biosynthesis in mice. BI 665915 is promising for research of various inflammatory diseases, including respiratory and cardiovascular diseases .
|
-
- HY-W345885
-
|
|
β-glucuronidase
|
Metabolic Disease
|
|
Saccharic acid is a competitive inhibitor of β-glucuronidase. Saccharic acid considerably retards hydrolysis of the glucuronide of 'l-ortho-hydroxyphenylazo-2-naph-thol' by frozen mouse kidney sections, but has no effect on liver regeneration following damage and on growth in infant mice .
|
-
- HY-155029
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-16 is a soluble epoxide hydrolase (sEH) inhibitors with an IC50 of 2 nM. sEH inhibitor-16 reduces the inflammatory damage in Cerulein (HY-A0190)-induced acute pancreatitis (AP) in mice and can be used for inflammation/immunology research .
|
-
- HY-B0401R
-
|
|
Na+/K+ ATPase
|
Metabolic Disease
Cancer
|
|
Tolbutamide (Standard) is the analytical standard of Tolbutamide. This product is intended for research and analytical applications. Tolbutamide is an orally active KATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete .
|
-
- HY-17553
-
|
MKC-231
|
iGluR
|
Neurological Disease
|
|
Coluracetam (MKC-231) is an orally taken choline uptake enhancer. Coluracetam can improve the reduced acetylcholine levels in the hippocampus of rats and mice, enhancing learning difficulties, memory deficits, and cognitive impairments. Coluracetam induces a lower degree of hepatic venous hyperglycemia .
|
-
- HY-B1002
-
|
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Infection
|
|
Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice .
|
-
- HY-100442
-
|
ABR-215757; ABR 25757
|
SARS-CoV
|
Metabolic Disease
Inflammation/Immunology
|
|
Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
|
-
- HY-N6857
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades .
|
-
- HY-N0592
-
|
|
NF-κB
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-N1388
-
|
|
Others
|
Inflammation/Immunology
|
|
Tussilagone, a major active component in Tussilago farfara, has anti-inflammatory effect. Tussilagone ameliorates inflammatory responses in dextran sulphate sodium-induced murine colitis. Tussilagone inhibits the inflammatory response and improves survival in cecal ligation and puncture (CLP)-induced septic mice .
|
-
- HY-D1066
-
|
|
Fluorescent Dye
|
Others
|
|
NIR-Thiol dinitrobenzenesulfonate has both absorption and emission in the NIR region. NIR-Thiol dinitrobenzenesulfonate responds to thiol with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-Thiol dinitrobenzenesulfonate is capable of imaging endogenously produced thiol in living cells and mice .
|
-
- HY-B0534S1
-
|
Ro111163-d4
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-W018723
-
|
p-Aminobenzamidine dihydrochloride
|
Ser/Thr Protease
|
Cancer
|
|
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice .
|
-
- HY-147204
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A) .
|
-
- HY-151342
-
|
|
Others
|
Others
|
|
Ser@TPP@CUR is a Curcumin (HY-N0005) derivative. Ser@TPP@CUR effectively ameliorates injured renal tubular epithelial cells and improves renal functions of acute kidney injury (AKI) mice. Ser@TPP@CUR can be used for the research of AKI .
|
-
- HY-148708
-
|
|
iGluR
|
Neurological Disease
|
|
Oleoyl-D-lysine is a selective Glycine Transporter-2 (GlyT2) inhibitor based on lipid. Oleoyl-D-lysine reverses neuropathic pain in mice, shows antidrowsiness effect on chronic neuropathic pain. Oleoyl-D-lysine is safe and effective without respiratory depression .
|
-
- HY-103400
-
|
8-Cl-Ado
|
AMPK
Autophagy
|
Cancer
|
|
8-Chloroadenosine (8-Cl-Ado), a unique ribonucleoside analog, depletes endogenous ATP that subsequently induces the phosphorylation and activation of AMPK. 8-Chloroadenosine induces autophagic cell death. 8-Chloroadenosine effectively inhibited in vivo tumor growth in mice .
|
-
- HY-N0592A
-
|
|
NF-κB
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-W369099
-
|
|
STAT
Apoptosis
|
Cancer
|
|
HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice .
|
-
- HY-N12016
-
|
|
Others
|
Metabolic Disease
|
|
Fulvotomentoside B is a saponin isolated from Lactobacillus flavus. Fulvotomentoside compounds can significantly reduce serum glutamate pyruvate transaminase (SGPT) and triacylglycerol (GT) levels in mice poisoned by CCl4, d-galactosamine (d-gal) and acetaminophen, and significantly alleviate liver pathology. damage .
|
-
- HY-P10057
-
|
|
Apoptosis
|
Cancer
|
|
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC50 value of 130 nM. cpm-1285 reduces tumor burden in mice .
|
-
- HY-163003
-
|
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 19 (compound 10) is an orally available antitrypanosomal agent. Antitrypanosomal agent 19 effectively inhibits the growth of trypanosomatids T. b. brucei, T. b. gambiense and T. b. rhodesiense, mitigating the Human trypanosomiasis (HAT)-induced acute infectious toxicity in mice .
|
-
- HY-157211
-
|
|
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 66 (compound 8) is a pterostilbene derivative with anti-inflammatory activity. Anti-inflammatory agent 66 inhibits pro-inflammatory cytokines by blocking the LPS-induced NF-κB/MAPK signaling pathway and effectively alleviates DSS-induced acute colitis in mice .
|
-
- HY-163320
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice .
|
-
- HY-162387
-
-
- HY-69019A
-
|
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
7-Nitroindazole sodium is a selective and BBB-penatrable inhibitor of nitric oxide synthase (NOS). 7-Nitroindazole sodium can inhibit the activity of central NOS with an IC50 of 0.47 μM in the cerebellum of mice. 7-Nitroindazole sodium has anti-injurious and neuroprotective properties .
|
-
- HY-114611
-
|
|
IRE1
|
Metabolic Disease
|
|
BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress .
|
-
- HY-162765
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV4-IN-5 (Compound 1f) is a potent TRPV4 inhibitor (IC50 = 0.46 μM). TRPV4-IN-5 significantly alleviates the symptoms of acute lung injury induced by lipopolysaccharide (HY-D1056) in mice .
|
-
- HY-113412AR
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
3-Methylhistamine (dihydrochloride) (Standard) is the analytical standard of 3-Methylhistamine (dihydrochloride). This product is intended for research and analytical applications. 3-Methylhistamine dihydrochloride is a degradation product of histamine. 3-Methylhistamine dihydrochloride, a methylated product of histamine, is associated with immune response and shows upregulation in the vaccinated mice .
|
-
- HY-162893
-
|
|
Glucosidase
|
Metabolic Disease
|
|
SX29 is an orally active non-competitive α-glucosidase inhibitor with an IC50 value of 2.12 μM. SX29 exhibits hypoglycemic activity, and oral administration of SX29 can reduce blood glucose levels and improve glucose tolerance in diabetic mice .
|
-
- HY-14229
-
|
CCDC
|
G protein-coupled Bile Acid Receptor 1
Calcium Channel
|
Metabolic Disease
|
|
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
|
-
- HY-103216A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport .
|
-
- HY-W677042
-
|
5α-Androst-16-en-3α-ol
|
GABA Receptor
|
Neurological Disease
|
|
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and human male axillary sweat. α-Androstenol is also a positive modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50=0.4 uM). α-Androstenol decreases immobility time in the forced swim test and increases time spent in the open arms of the elevated plus maze in mice. α-Androstenol protects against seizures induced by Pentylenetetrazole or electroshock with anxiolytic-like activity in mice .
|
-
- HY-10367
-
|
CI-1033; PD-183805
|
EGFR
Orthopoxvirus
|
Infection
Cancer
|
|
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice .
|
-
- HY-N7272
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
|
-
- HY-108559
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .
|
-
- HY-P2251
-
|
|
HIV
Microtubule/Tubulin
|
Infection
Inflammation/Immunology
Cancer
|
|
T-peptide, a Tuftsin analog, can be used for the research of human immunodeficiency virus (HIV) infection. T-peptide prevents cellular immunosuppression and improves survival rate in septic mice. T-peptide also can inhibit the growth of residual tumor cells after surgical resection .
|
-
- HY-124713
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
ML372 inhibits survival motor neuron (SMN) protein ubiquitination, increases SMN protein stability without affecting mRNA expression. ML372 improves spinal muscular atrophy (SMA) in mice. ML372 is brain penetrant and has a reasonable exposure and half-life in vivo .
|
-
- HY-111432
-
|
|
Ras
|
Others
|
|
CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma .
|
-
- HY-122529
-
|
|
Bacterial
|
Infection
|
|
Almurtide (nor-MDP), a muramyl dipeptide derivative with anti-inflammatory and anti-tumor activity. Almurtide also shows protective effects against intraperitoneal Pseudomonas aeruginosa infection or intravenously Candida albicans infection in mice. Almurtide also inhibits the carcinogenic Friend leukemia virus .
|
-
- HY-149101
-
|
IDP
|
Others
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Riboxin (IDP), an orally active purine derivative-hypoxanthine rlboside, has antihypoxic and antihyperthermic activity. Riboxin also has an antiarrhythmic action in cats, rabbits, and mice with cardiac rhythm disorders induced by Ouabain. Riboxin protects animals against the noxious effects of γ-irradiation .
|
-
- HY-145119S
-
|
VV116 free base; GS-621763-d1
|
Isotope-Labeled Compounds
|
Others
|
|
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
|
-
- HY-P5878
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
|
-
- HY-P5578
-
|
|
GCGR
|
Metabolic Disease
|
|
A8SGLP-1 is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 reduces blood glucose in db/db mice without affecting its function .
|
-
- HY-P5975
-
|
Z-LLL-FMK
|
Cathepsin
SARS-CoV
|
Infection
|
|
Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge .
|
-
- HY-156466
-
|
|
JAK
|
Inflammation/Immunology
|
|
QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice .
|
-
- HY-149708
-
|
|
ICMT
|
Others
|
|
UCM-13207 (compound 21) is a selective ICMT inhibitor that ameliorates basic progeria-like features. UCM-13207 can improve the survival rate of LmnaG609G/G609G mice in the mouse premature aging model .
|
-
- HY-19839
-
|
Antibiotic C 15003P3'; Maytansinol butyrate
|
Antibiotic
|
Infection
Cancer
|
|
Ansamitocin P 3' (Antibiotic C 15003P3') is an anti-tumor antibiotic. Ansamitocin P 3' prolongs the survival of mice with leukemia P388, melanoma B16, leukemia L1210, sarcoma 180, Ehrlich carcinoma and mast cell tumor P815 .
|
-
- HY-14942
-
|
RTA 744 free base; WP 744 free base; WP 769
|
Others
|
Cancer
|
|
Berubicin (RTA 744 free base; WP 744) is a 4'-O-benzyldoxorubicin that inhibits P-gp and MRP1-mediated efflux and has anticancer activity. Berubicin inhibits glioblastoma multiforme (GBM) and exhibits cytotoxicity. Berubicin has poor bioavailability in mice .
|
-
- HY-111315
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
|
|
XEN103 is a SCD1 inhibitor, with IC50s of 14 nM and 12 nM for mSCD1 and SCD1 in HepG2 cell. XEN103 can be used for research of obesity and type 2 diabetes. XEN103 also induces sebaceous gland atrophy in mice .
|
-
- HY-B0860R
-
|
|
Others
|
Cancer
|
|
Diuron (Standard) is the analytical standard of Diuron. This product is intended for research and analytical applications. Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male and female mice by 73 and 27%, respectively.
|
-
- HY-164401
-
|
|
Others
|
Cancer
|
|
QBS10072S is a bifunctional chemotherapeutic agent, through combination of a cytotoxin and a selective LAT1 transporter substrate. QBS10072S exhibits cytotoxicity in MDA-MB-231 cell and antitumor efficacy in mice. QBS10072S is blood-brain barrier (BBB) penetrable .
|
-
- HY-N0901AR
-
|
|
Autophagy
Beclin1
α-synuclein
|
Neurological Disease
Cancer
|
|
Corynoxine B (Standard) is the analytical standard of Corynoxine B. This product is intended for research and analytical applications. Corynoxine B is a natural alkaloid and autophagy inducer that can improve Mn induced cellular autophagy dysregulation and enhance clearance of alpha synuclein (alpha syn) in Parkinson's disease mice .
|
-
- HY-164535
-
|
AMG 133
|
GLP Receptor
|
Metabolic Disease
|
|
Maridebart cafraglutide (AMG 133) is an antibody-peptide conjugate acting as a GLP-1 receptor agonist and an antagonist of the GIP receptor. Maridebart cafraglutide reduces body weight and improve metabolic markers in male obese mice and cynomolgus monkeys. Maridebart cafraglutide is promising for research of obesity .
|
-
- HY-19848
-
|
LBM-642
|
PPAR
|
Metabolic Disease
|
|
Cevoglitazar (LBM-642) is an orally active and highly potent PPARα and PPARγ dual agonist. Cevoglitazar can reduce food intake, body weight, and fasting plasma insulin in obese mice and cynomolgus monkeys. Cevoglitazar has the potential for diabetes and obesity-related disorders research .
|
-
- HY-103639A
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis .
|
-
- HY-B0534R
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide (Standard) is the analytical standard of Moclobemide. This product is intended for research and analytical applications. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-113354
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
|
-
- HY-109506
-
DPPC
5 Publications Verification
129Y83
|
Liposome
Endogenous Metabolite
|
Others
|
|
DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
|
-
- HY-N7026
-
|
|
Others
|
Metabolic Disease
|
|
Celosin I, an oleanane-type triterpenoid saponin isolated from the seeds of Celosia argentea L, could be used as chemical markers for the quality control of C. argentea seeds. Celosin I exhibits significant hepatoprotective effect on carbon tetrachloride-induced and N,N-dimethylformamide-induced hepatotoxicity in mice .
|
-
- HY-D0887
-
|
IMP disodium salt; Disodium inosinate
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Disodium 5'-inosinate (IMP disodium salt) is a nucleotide-based umami agent. Disodium 5'-inosinate can bind to umami receptors and stimulate taste nerves, allowing the brain to perceive umami. In addition, Disodium 5'-inosinate produces a transient behavioral excitement in mice .
|
-
- HY-131042
-
NNMTi
3 Publications Verification
|
Others
|
Metabolic Disease
|
|
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues . NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice .
|
-
- HY-P3102
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
|
-
- HY-103111
-
|
|
mGluR
|
Neurological Disease
|
|
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
|
-
- HY-107503
-
|
|
mGluR
|
Neurological Disease
|
|
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
|
-
- HY-132302A
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-145690
-
|
|
FLT3
|
Cancer
|
|
HP1328 is a potent inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1328 is a benzoimidazole scaffold-based compound. HP1328 significantly reduces the leukemia burden and prolongs the survival of mice with FLT3/ITD leukemia .
|
-
- HY-69019
-
|
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
7-Nitroindazole is a selective and BBB-penatrable inhibitor of nitric oxide synthase (NOS). 7-Nitroindazole can inhibit the activity of central NOS with an IC50 of 0.47 μM in the cerebellum of mice. 7-Nitroindazole has anti-injurious and neuroprotective properties .
|
-
- HY-144361
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
|
-
- HY-121852
-
|
SCH-225336
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice .
|
-
- HY-150503
-
|
|
HDAC
|
Neurological Disease
|
|
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .
|
-
- HY-124244
-
|
PPARδ/γ agonist 1
|
PPAR
|
Neurological Disease
|
|
DB-959 (PPARδ/γ agonist 1) is a potent PPAR agonist targeting PPARδ/γ. DB-959 improves spatial learning and memory in mice induced by Streptozotocin (HY-13753) and has the potential to improve Alzheimer's disease (AD). .
|
-
- HY-149240
-
|
|
P-glycoprotein
|
Cancer
|
|
Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor with significant antitumor activity and less toxicity to normal and pseudonormal cells. Anticancer agent 108 (Compound 3.10) had no acute toxic effect on С57BL/6 mice .
|
-
- HY-149357
-
|
|
HBV
|
Infection
|
|
Yhhu6669 is an anti-HBV agent. Yhhu6669 inhibits HBV DNA. Yhhu6669 inhibits HBV replication by inducing the formation of DNA-free capsids. Yhhu6669 decreases HBV DNA and HBcAg in AAV/HBV-infected mice. Yhhu6669 has favorable PK properties .
|
-
- HY-149874
-
|
|
DGK
|
Inflammation/Immunology
Cancer
|
|
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research .
|
-
- HY-156593
-
|
|
ROCK
|
Cancer
|
|
ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .
|
-
- HY-P10039
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) rat is a β-amyloid peptide (Abeta), a metal-binding domain fragment of amyloid. Three amino acid substitutions in β-Amyloid (1-16) rat that differ from humans render rats and mice less susceptible to AD-like neurodegeneration .
|
-
- HY-N11286
-
|
TG-DHA; Meganol D
|
Others
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases .
|
-
- HY-161671
-
|
|
nAChR
|
Neurological Disease
|
|
GAT2711 (compound 3h) is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells and exhibits analgesic activity in α7 knockout mice .
|
-
- HY-116881
-
|
|
mAChR
|
Neurological Disease
|
|
SCH 57790 is a selective antegonist for muscarinic M2 receptor, which increases acetylcholine release, and thus improves cognitive performance. SCH 57790 reverses Scopolamine (HY-N0296)-induced memory deficits in mice, without significant toxicity (100 mg/kg).
|
-
- HY-123020
-
|
BDA-366 analog
|
Others
|
Cancer
|
|
CYD-2-88 (BDA-366 analog) is a BDA-366 (HY-101083) (Bcl2 BH4 antagonist) analog. CYD-2-88 (20 mg/kg, i.p.) inhibits tumor growth in NSCLC H460 xenografts mice .
|
-
- HY-105294
-
|
|
Dopamine Receptor
|
Others
|
FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks .
|
-
- HY-119048
-
|
2'-Chloropentostatin
|
Others
|
Others
|
|
Adechlorin (2'-Chloropentostatin) is an adenosine deaminase inhibitor isolated from actinomycete culture, with potent inhibitory activity against calf intestinal adenosine deaminase, a Ki value that is comparable to other known inhibitors, and can enhance the antiviral activity of Ara-A, and has lower acute toxicity in mice than other analogs.
|
-
- HY-B0131A
-
|
|
Others
|
Cardiovascular Disease
|
|
Alprostadil sodium is a prostaglandin receptor ligand that exhibits Ki values of 36, 10, 1.1, 2.1, and 33 nM for the EP1, EP2, EP3, EP4, and IP receptors in mice, respectively. It promotes vasodilation and inhibits platelet aggregation, making it a useful vasodilator for investigating peripheral vascular disease.
|
-
- HY-120828
-
|
CJC 1134PC
|
GLP Receptor
|
Metabolic Disease
|
|
Albenatide (CJC 1134PC) is a modified Exendin-4 (HY-13443) analogue conjugated to human recombinant albumin (HRA) in vitro to form a long-acting DPP-4-resistant GLP-1R agonist. Albenatide covalently binds through a low-molecular chemical linker (cys-C13H19O6N3-lys) to the cysteine residue in position 34 of HRA. Albenatide increases cyclic AMP (cAMP) production in vitro. Albenatide reduces glucose excursions, food intake, gastric emptying in wild-type mice and improves glucose tolerance and reduces body weight in high-fat diet mice .
|
-
- HY-118030
-
|
|
Calcium Channel
|
Neurological Disease
|
|
RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
|
-
- HY-132579A
-
|
RG6042 sodium; IONIS-HTTRx sodium
|
Huntingtin
|
Neurological Disease
|
|
Tominersen sodium is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen sodium can be used for the research of Huntington’s disease (HD) .
|
-
- HY-155553
-
|
|
GPR119
|
Metabolic Disease
|
|
GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes .
|
-
- HY-154974
-
|
|
Liposome
|
Cancer
|
|
LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model .
|
-
- HY-120110
-
IOX4
5 Publications Verification
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
Inflammation/Immunology
|
|
IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
|
-
- HY-B1266
-
|
Eserine salicylate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning .
|
-
- HY-124373
-
|
|
MMP
|
Metabolic Disease
|
|
ND-336 is a selective inhibitor of matrix metalloproteinase (MMP)-2, MMP-9, and MMP-14, with Kis of 85, 150, and 120 nM, respectively. ND-336 accelerates diabetic wound healing in mice by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound .
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-147049
-
|
|
Others
|
Metabolic Disease
|
|
PAL-4 (compound 4) is a potent, selective and reversible Lysophospholipase-like 1 (LYPLAL1) activator with EC50 value of 0.39 μM and 0.49 μM for mice LYPLAL1 and huamn LYPLAL1, respectively. PAL-4 can be used for researching metabolic disorders .
|
-
- HY-147014
-
|
|
CMV
Orthopoxvirus
|
Infection
|
|
Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guinea pig cytomegalovirus (GPCMV) infection and decreases viral replication in guinea pig model .
|
-
- HY-N1428A
-
|
|
Endogenous Metabolite
Apoptosis
Antibiotic
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
-
- HY-120514
-
|
|
TRP Channel
Potassium Channel
|
Cardiovascular Disease
|
|
JNc-440 is a potent antihypertensive agent. JNc-440 can enhance the interaction of TRPV4 and Ca 2+-activated potassium channel 3 (KCa2.3) in endothelial cells. JNc-440 can also enhance vasodilation, and exerted antihypertensive effects in mice .
|
-
- HY-13589
-
|
LU103793 free base
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer .
|
-
- HY-152857
-
|
LY3473329
|
Others
|
Cardiovascular Disease
|
|
Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)
formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys .
|
-
- HY-149429
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) .
|
-
- HY-111187
-
|
KX-02
|
Src
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell .
|
-
- HY-P5578A
-
|
|
GCGR
|
Metabolic Disease
|
|
A8SGLP-1 TFA is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 TFA reduces blood glucose in db/db mice without affecting its function .
|
-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-149662
-
-
- HY-163066
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-44 (compound IT4) is an inhibitor of α-glucosidase with IC50 value of 2.35 μM. α-Glucosidase-IN-44 has an oral activity. α-Glucosidase-IN-44 suppresses fasting blood glucose levels in diabetic mice .
|
-
- HY-163363
-
|
|
Adrenergic Receptor
|
Cancer
|
|
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
|
-
- HY-162406
-
|
|
TAM Receptor
|
Cancer
|
|
UNC8969 (compound 43) is a MERTK/AXL dual inhibitor with IC50s of 1.1±0.8 nM for MERTK and 5.3 ± 2.7 nM for AXL. UNC8969 also exerts a T1/2 of 7.3 h with 5 mg/kg i.v. in mice .
|
-
- HY-121111
-
|
|
Others
|
Cancer
|
|
Agaritine is a compound isolated from the commonly cultivated commercial mushroom Agaricus bisporus. Agaritine is hydrolyzed by an enzyme system present in the mushroom into 4-(hydroxymethyl)benzenediazonium ion, which is a carcinogen in mice. Agaritine is structurally similar to some known carcinogens and can be used for research in cancer and food safety .
|
-
- HY-162655A
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
SLF80821178 hydrochloride is an orally active inhibitor for sphingosine-1-phosphate transporter (Spns2), that inhibits the sphingosine-1-phosphate (S1P) release in HeLa with an IC50 of 51 nM. SLF80821178 hydrochloride reduces the circulating lymphocyte without affecting plasma S1P levels in mice .
|
-
- HY-N0031R
-
|
|
Others
|
Inflammation/Immunology
|
|
Plantamajoside (Standard) is the analytical standard of Plantamajoside. This product is intended for research and analytical applications. Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation .
|
-
- HY-N3312R
-
|
|
Endogenous Metabolite
|
Infection
|
|
Matairesinol (Standard) is the analytical standard of Matairesinol. This product is intended for research and analytical applications. Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-168021
-
|
|
Monoamine Oxidase
Serotonin Transporter
|
Neurological Disease
|
MAO-A/SERT-IN-1 is an inhibitor of MAO-A/serotonin transporter (SERT). MAO-A/SERT-IN-1 can reduce SERT-mediated reuptake of 5-HT and has neuroprotective effects in cell inhibition models. MAO-A/SERT-IN-1 can improve depressive behavior in zebrafish and mice .
|
-
- HY-13589A
-
|
LU103793 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) hydrochloride is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin hydrochloride blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin hydrochloride can be used to research anticancer .
|
-
- HY-121671
-
|
|
RAR/RXR
|
Neurological Disease
|
|
TBTC is a selective agonist with the activity of improving behavioral deficits in Alzheimer's disease model mice. TBTC can effectively activate the heterodimerization of RXRα with LXRα or PPARγ. TBTC stimulates the expression of apoE, ABCA1, and ABCG1 genes and reduces Aβ content in cells and animal models .
|
-
- HY-158311
-
|
|
RANKL/RANK
p38 MAPK
NF-κB
|
Endocrinology
|
|
Anti-osteoporosis agent-8 (Compound 4aa) is an inhibitor for RANKL, which inhibits RANKL-induced osteoclastogenesis and osteoclast differentiation (IC50 is 2.41 μM) in cells RAW264.7. Anti-osteoporosis agent-8 ameliorates bone loss in an ovariectomized (OVX) mice model .
|
-
- HY-13859
-
|
L-FMAU
|
HBV
DNA/RNA Synthesis
Orthopoxvirus
|
Infection
|
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
|
-
- HY-100968
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats .
|
-
- HY-W008610
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats .
|
-
- HY-N2320
-
|
Eserine hemisulfate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning .
|
-
- HY-P1422
-
Spadin
1 Publications Verification
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research .
|
-
- HY-P3102A
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
|
-
- HY-101064
-
|
N-FMOC-leucine; NPC 15199; NSC 334290
|
PPAR
|
Metabolic Disease
|
|
Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .
|
-
- HY-124717
-
|
|
Endogenous Metabolite
|
Others
|
|
YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration .
|
-
- HY-N10390
-
|
|
Others
|
Cancer
|
|
3β-Hydroxylanosta-8,24-dien-21-al is a lanostane-type triterpene. 3β-Hydroxylanosta-8,24-dien-21-al can inhibit the tumor promotion, reducing the percentage of mice bearing papillomas .
|
-
- HY-148413
-
|
ISIS 3521 sodium
|
PKC
|
Cancer
|
|
Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
|
-
- HY-108742
-
|
BA 058; BIM 44058
|
PTHR
Arrestin
|
Metabolic Disease
Cancer
|
|
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis .
|
-
- HY-12611
-
|
GW-869682X
|
SGLT
|
Metabolic Disease
|
|
Sergliflozin etabonate (GW-869682X) is a potent and orally active sodium glucose cotransporter (SGLT2) inhibitor. Sergliflozin etabonate shows antidiabetic and antihyperglycemic effects. Sergliflozin etabonate significantly reduces non-fasting blood glucose levels in diabetic mice. Sergliflozin etabonate has the potential for the research of diabetes .
|
-
- HY-13659
-
|
NSC 650426
|
Antibiotic
Bcl-2 Family
Apoptosis
|
Infection
Cancer
|
|
KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
|
-
- HY-W250113
-
|
Zymosan A from Saccharomyces cerevisiae
|
Toll-like Receptor (TLR)
|
Others
Inflammation/Immunology
|
|
Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury .
|
-
- HY-153306
-
|
|
PI3K
|
Cancer
|
|
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
|
-
- HY-D2279
-
|
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively .
|
-
- HY-161893
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 15 (Compound 9o10) exhibits antibacterial activity, that inhibits methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 0.0625 μg/mL. Anti-MRSA agent 15 exhibits low hemolysis and low cytotoxicity. Anti-MRSA agent 15 exhibits anti-infective in mice .
|
-
- HY-12580
-
|
|
MDM-2/p53
|
Cancer
|
|
RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
|
-
- HY-168031
-
-
- HY-155052
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-2 (compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils .
|
-
- HY-128435
-
|
|
Others
|
Metabolic Disease
|
|
2,4'-Dihydroxybenzophenone ((Z)-SU4312) exhibited estrogenic activities. 2,4'-Dihydroxybenzophenone has oral bioactivity that can effectively protect C57BL/6J mice from Acetaminophen (HY-66005, APAP)-induced hepatotoxicity .
|
-
- HY-B1192
-
|
β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate
|
Estrogen Receptor/ERR
HBV
Bcl-2 Family
|
Neurological Disease
|
|
Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice .
|
-
- HY-N0219
-
|
(+)-Bicuculline; d-Bicuculline
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
|
-
- HY-N1428
-
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice .
|
-
- HY-108497
-
|
|
Somatostatin Receptor
|
Neurological Disease
Cancer
|
|
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice .
|
-
- HY-135747
-
|
GR-7
|
Bacterial
|
Infection
|
|
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice .
|
-
- HY-134494
-
|
|
GPR68
|
Neurological Disease
|
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .
|
-
- HY-P1136B
-
-
- HY-12736
-
|
|
Syk
ERK
|
Inflammation/Immunology
Cancer
|
|
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1) . GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .
|
-
- HY-12736A
-
|
|
Syk
ERK
|
Inflammation/Immunology
Cancer
|
|
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1) . GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .
|
-
- HY-101954A
-
|
ORI-9020 ammonium; SB-9000 ammonium
|
HBV
|
Infection
Inflammation/Immunology
|
|
Inarigivir (ORI-9020) ammonium is a dinucleotide antiviral drug that can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) ammonium acts as a RIG-I (Retinoic acid-inducible gene-I) agonist to activate cellular innate immune responses .
|
-
- HY-132579
-
|
RG6042; IONIS-HTTRx
|
Huntingtin
|
Neurological Disease
|
|
Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD) .
|
-
- HY-19893
-
|
(+)-Antroquinonol
|
Keap1-Nrf2
|
Inflammation/Immunology
Cancer
|
|
Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects . Antroquinonol can be used for the research of colon cancer . Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice .
|
-
- HY-103327
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-110198
-
|
|
Prostaglandin Receptor
PERK
|
Inflammation/Immunology
|
|
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
|
-
- HY-146280
-
|
|
GABA Receptor
|
Neurological Disease
Metabolic Disease
|
|
mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice .
|
-
- HY-147016
-
|
|
Orthopoxvirus
|
Infection
|
|
NIOCH 14 is a antiviral agent and a pro-agent. NIOCH 14 has antiviral activity against orthopoxviruses. NIOCH 14 can significantly lower proportions of infected mice, and virus production levels in the lungs. NIOCH 14 can be used for researching anti-smallpox . NIOCH 14 shows anti-orthopoxvirus activity.
|
-
- HY-B1794
-
-
- HY-150186
-
|
|
RXFP Receptor
|
Metabolic Disease
|
|
RXFP2 agonist 2 is a selective，orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 µM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis .
|
-
- HY-P99708
-
|
ABBV-151; ARGX-115
|
TGF-beta/Smad
|
Cancer
|
|
Livmoniplimab (ABBV-151) is a monoclonal antibody against GARP/TGF-β1 that can inhibit the release of active TGF-β1. Livmoniplimab has anti-tumor activity in colon cancer mice. Livmoniplimab can be used for the study of locally advanced or metastatic solid tumors .
|
-
- HY-153261
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-17 is a potent, selective and orally active NLRP3 inflammasome inhibitor with an IC50 value of 7 nM. NLRP3-IN-17 significantly inhibits NLRP3 dependent IL-1β secretion in mice and can be used for chronic inflammatory diseases research .
|
-
- HY-153798
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 10 (compound 42) is an agonist of GLP Receptor. GLP-1 receptor agonist 10 inhibits food intake and reduces glucose excursion in mice. GLP-1 receptor agonist 10 can be used in the study of type 2 diabetes (T2DM) and obesity .
|
-
- HY-N0278
-
|
Pulsatilla camphor; Anemonine; trans-Anemonin
|
PKC
NO Synthase
|
Inflammation/Immunology
|
|
Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases .
|
-
- HY-155682
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 150 (compound 5g) is an antibacterial agent with potent antibacterial activity against both Gram-positive bacteria and Gram-negative bacteria (MIC values ranging from 1-32 μg/mL). Antibacterial agent 150 can increase survival rate of MRSA (Methicillin-resistant Staphylococcus aureus)-infected mice .
|
-
- HY-155548
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. RORγt inverse agonist 31 can alleviate the severity of Imiquimod (HY-B0180)-induced psoriasis in mice .
|
-
- HY-119789
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Albofungin (Antibiotic P-42-1) is isolated from the culture filtrate of Actinomyces tumemacerans strain INMI.P-42. Albofungin shows highly active on a wide variety of gram-positive bacteria and fungi. Albofungin shows cytotoxic to HeLa cell cultures and exhibited antitumor activity on EHRLICH ascites tumor in mice.
|
-
- HY-N12249
-
|
|
Amyloid-β
TMV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC50: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice .
|
-
- HY-P1434
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
[Pro3]-GIP (mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (mouse) can be used for research of type 2 diabetes .
|
-
![[Pro3]-GIP (mouse)](//file.medchemexpress.eu/product_pic/hy-p1434.gif)
- HY-124941
-
|
|
Keap1-Nrf2
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro .
|
-
- HY-149776
-
|
|
nAChR
|
Neurological Disease
|
|
RGH-560 (compound 53) shows highly advanced α7 nAChR positive modulator properties and favorable physicochemical features. RGH-560 has robust procognitive in vivo potential. RGH-560 can be used to study Scopolamine (HY-N0296) -induced amnesia in mice .
|
-
- HY-161246
-
|
|
Others
|
Neurological Disease
|
|
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
|
-
- HY-W795264
-
|
|
Parasite
|
Infection
|
|
FR900098 is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 has no effect on bone marrow red blood cells in NMRI mice .
|
-
- HY-109120S
-
-
- HY-B0534S
-
|
Ro111163-d8
|
Isotope-Labeled Compounds
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-162565
-
|
|
STK33
CDK
RET
|
Endocrinology
|
|
CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive .
|
-
- HY-159131
-
-
- HY-159106
-
-
- HY-161890
-
|
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
Antimycobacterial agent-8 (Compound 49) is an inhibitor for DNA gyrase. Antimycobacterial agent-8 exhibits antibacterial activity against Mycobacterium tuberculosis and M. abscessus with MIC90 of 2.5 μM and 0.63 μM. Antimycobacterial agent-8 exhibits good plasma protein binding ability in mice .
|
-
- HY-164320
-
|
|
Others
|
Cancer
|
|
Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-163885
-
|
|
Cholinesterase (ChE)
Beta-secretase
γ-secretase
|
Neurological Disease
|
|
SSZ is a multi-target inhibitor, which targets multiple pathological mechanisms of Alzheimer's disease (AD). SSZ targets acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. SSZ ameliorates Alzheimer’s diseases and exhibits neuroprotective effect in mice .
|
-
- HY-162727
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
GCS-12 is a Th1/2-balanced sulfonamide glycolipid with improved interaction with CD1d. GCS-12 is an agonist for natural killer T (NKT) cell, that induces the secretion of cytokine IFN-γ and IL-4, and exhibits immunomodulatory and anti-tumor activities in mice .
|
-
- HY-N1570R
-
|
|
Salt-inducible Kinase (SIK)
|
Inflammation/Immunology
|
|
Pterosin B (Standard) is the analytical standard of Pterosin B. This product is intended for research and analytical applications. Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3 .
|
-
- HY-N5106R
-
|
|
Apoptosis
|
Cancer
|
|
(E)-Flavokawain A (Standard) is the analytical standard of (E)-Flavokawain A. This product is intended for research and analytical applications. (E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice .
|
-
- HY-168002
-
|
|
Others
|
Inflammation/Immunology
|
MPO-IN-8 is an orally active myeloperoxidase (MPO) inhibitor. MPO-IN-8 can inhibit the generation of hypochlorous acid in neutrophils and the release of extracellular traps (NETosis). In mice with gouty arthritis, MPO-IN-8 can reduce swelling, lower peroxidase activity, and decrease IL-1β levels .
|
-
- HY-W654264
-
|
|
Endogenous Metabolite
Integrin
|
Cardiovascular Disease
|
|
2-Methylbutyrylcarnitine (chloride) is a gut microbial metabolite which binds to integrin α2β1 in platelets, potentiating cytosolic phospholipase A2 (cPLA2) activation and platelet hyperresponsiveness. 2-Methylbutyrylcarnitine (chloride) enhances platelet hyperreactivity and thrombus formation in mice. 2-Methylbutyrylcarnitine (chloride) is a branched-chain acylcarnitine .
|
-
- HY-164547
-
|
|
Porcupine
Wnt
β-catenin
|
Cancer
|
WHN-88 is a Porcupine (PORCN) inhibitor. WHN-88 can eliminate the palmitoylation of Wnt ligands, preventing their secretion and subsequent Wnt/β-catenin signaling. WHN-88 can inhibit cancer cell stemness and suppress the occurrence and development of breast tumors in MMTV-Wnt1 transgenic mice .
|
-
- HY-169104
-
|
|
Bacterial
|
Infection
|
|
InhA-IN-8 (compound 6c) is an orally active inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase). InhA-IN-8 has good inhibitory activity against Mtb UalRv (MIC = 0.5-1 μg/mL). InhA-IN-8 can be used in research on acute tuberculosis model mice .
|
-
- HY-120187
-
|
|
Others
|
Others
|
|
DDCPPB-Glu (compound 3a) is a compound with anti-tumor activity, which has the activity of inhibiting tumor cell growth and prolonging survival. DDCPPB-Glu has growth inhibition effect on various tumor cell lines, can increase the survival time of leukemia mice, and has inhibitory effect on tumors such as colon cancer and lung cancer.
|
-
- HY-167741
-
|
|
Others
|
Cardiovascular Disease
Neurological Disease
|
|
Chlorisondamine is a nicotinic antagonist that acts as a ganglionic blocker and has been utilized to evaluate the neurogenic contributions to blood pressure and sympathetic vasomotor tone in animal models. Chlorisondamine has demonstrated antihypertensive properties, primarily being assessed through its effects on blood pressure, cardiac output, and heart rate in various experimental settings, particularly in mice.
|
-
- HY-168629
-
|
|
FXR
|
Metabolic Disease
|
|
FXR agonist 9 (compound 26) is an oral active and selectivity FXR partial agonist with the EC50 of 0.09 µM (75.13 % maximum efficacy). FXR agonist 9 ameliorates pathological features in HFD + CCl4-(HY-Y0298) induced metabolic dysfunction-associated steatohepatitis mice .
|
-
- HY-100935R
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Cimaterol (Standard) is the analytical standard of Cimaterol. This product is intended for research and analytical applications. Cimaterol (CL 263780) is a β-adrenergic agonist on energy metabolism in ob/ob mice . The Kd for Cimaterol binding to the L6 β-receptor is 26 nM which is compatible with its EC50 for the stimulation of protein synthesis (approx 5 nM) .
|
-
- HY-117051
-
|
|
Others
|
Cancer
|
|
STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
|
-
- HY-118032
-
|
|
Apoptosis
Autophagy
JNK
ERK
|
Cancer
|
|
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice .
|
-
- HY-66005
-
-
- HY-N6608S
-
|
Eserine-d3
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
|
-
- HY-P0119
-
|
|
GCGR
MEK
Akt
MMP
JNK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe −/− Irs 2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .
|
-
- HY-101030A
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-107999
-
CADD522
3 Publications Verification
|
Reactive Oxygen Species
|
Cancer
|
|
CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer .
|
-
- HY-N6869
-
|
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-P1422A
-
|
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research .
|
-
- HY-P1136C
-
-
- HY-130602
-
|
|
PROTACs
MEK
|
Cancer
|
|
MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively .
|
-
- HY-112081
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
|
-
- HY-141523
-
|
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
|
-
- HY-119347
-
|
|
IFNAR
STAT
|
Inflammation/Immunology
Cancer
|
|
Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4 + T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice .
|
-
- HY-113314
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
|
-
- HY-145733
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage .
|
-
- HY-144070
-
|
|
Others
|
Cancer
|
|
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
|
-
- HY-143420
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model .
|
-
- HY-N2573A
-
|
L-Corydalmine hydrochloride; TLZ-16-CL
|
Fungal
CXCR
|
Infection
Neurological Disease
|
|
Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi . Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
|
-
- HY-107761
-
|
|
Others
|
Neurological Disease
|
|
JMV 390-1 (Compound 6a) is a potent multipeptidase inhibitor. JMV 390-1 behaves as a full inhibitor of the major neurotensin (NT)/neuromedin N (NN) degrading enzymes in vitro with IC50 values from 30 to 60 nM. JMV 390-1 increases endogenous recovery of NT and NN from slices of mice hypothalamus depolarized with potassium .
|
-
- HY-146496
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice .
|
-
- HY-143237
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research .
|
-
- HY-B2201
-
|
Sodium citrate; Trisodium citrate anhydrous
|
Apoptosis
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice .
|
-
- HY-151959
-
|
|
FXR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-149940
-
|
|
SARS-CoV
|
Infection
|
|
SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 µg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice .
|
-
- HY-153699
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .
|
-
- HY-N11872
-
|
|
Others
|
Neurological Disease
|
|
Suffruticosol A is a neuroprotective agent that restores scopolamine-induced cellular neurodegenerative damage. Suffruticosol A ameliorates hippocampal cholinergic deficits and partially enhances BDNF signaling. Suffruticosol A has neuromodulatory effects in a Scopolamine (HY-N0296)-induced model, restoring memory and cognitive performance in mice. Suffruticosol A can be isolated from seeds of P. lactiflora .
|
-
- HY-P5550
-
|
|
Influenza Virus
|
Infection
|
|
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection .
|
-
- HY-129297
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
CMPF can be found in trace constituent of urine and blood. CMPF is a biomarker of type 2 diabetes. CMPF can act on the β cell and induces impaired mitochondrial function. CMPF decreases glucose-induced ATP accumulation, and induces oxidative stress. CMPF reverses hepatic lipid accumulation and improves insulin sensitivity in obese mice .
|
-
- HY-N12353
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Stevisalioside A (Compound 2) can be isolated from Stevia serrata roots. Stevisalioside A is an orally active antidiabetic agent. Stevisaliosides A inhibits PTP1B (IC50: 526.8 μM). Stevisalioside A reduces blood glucose levels and the postprandial peak in oral glucose and insulin tolerance tests in Streptozotocin (HY-13753) induced hyperglycemic mice .
|
-
- HY-18164
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TASP0277308 is a highly selective S1P1 antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice .
|
-
- HY-B0892R
-
|
Benzenemethanol (Standard)
|
Toll-like Receptor (TLR)
Cytochrome P450
|
Inflammation/Immunology
|
|
Benzyl alcohol (Standard) is the analytical standard of Benzyl alcohol. This product is intended for research and analytical applications. Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice .
|
-
- HY-139247
-
|
|
Others
|
Inflammation/Immunology
|
|
pNPS-DHA (Compound 19) is an orally active DHA-ethanolamide (DHEA) derivative that has antiallergic activity. pNPS-DHA inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) reaction in mice. pNPS-DHA has anti-degranulating activity in RBL-2H3 mast cells with an IC50 of 15 μM .
|
-
- HY-122817
-
|
|
Antibiotic
Parasite
|
Infection
|
|
FR900098 sodium is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 sodium has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 sodium has no effect on bone marrow red blood cells in NMRI mice .
|
-
- HY-160554
-
|
|
Liposome
|
Infection
Inflammation/Immunology
|
|
C12-113 is a lipidoid delivery agent that can be used to transfect siRNA into cells. C12-113 can also be combined with other lipids to form lipid nanoparticles (LNPs) for the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice .
|
-
- HY-163433
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-57 (Compound 10c) is a competitive and orally active α-glucosidase inhibitor with an IC50 value of 0.180 μM and a Ki of 0.15 μM. α-Glucosidase-IN-57 can reduce fasting and overall blood glucose levels in mice, and can be used for anti-diabetes research .
|
-
- HY-109120S1
-
-
- HY-155052A
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-2 (compound 5i) TFA is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 TFA inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils .
|
-
- HY-161458
-
|
|
GSK-3
Tau Protein
|
Neurological Disease
|
|
GSK-3β inhibitor 16 (compound 7c) is a GSK-3β inhibitor with the IC50 of 4.68 nM. GSK-3β inhibitor 16 decreases Tau hyperphosphorylated aggregate and alleviates cognitive impairments in the Scopolamin (HY-N0296)-induced model in mice .
|
-
- HY-129406
-
|
|
Others
|
Cardiovascular Disease
|
|
AF 698 is a phthalate derivative of Apovincamine (HY-135743) that can be used as a peripheral vasodilator with selective vasomotor effects on cerebral microvascular circulation. AF 698 has better vasodilator effect than Vincamine (HY-B1021), but there is no significant difference in the protective effect of the two drugs against hypobaric hypoxia-induced lethality in mice .
|
-
- HY-159088
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
|
-
- HY-158725
-
|
|
Others
|
Others
|
|
N-Octadecenoyl-(cis-9) -Sulfatide is a glycolipid found in the brains of mice. N-Octadecenoyl-(cis-9) -Sulfatide can be used as a standard for the determination of C18:13 '-mergogalactosyllactose in dry blood stains of patients with chromatic leukodystrophy (MLD) by ultra-high performance liquid chromatography-mass spectrometry (UPLC-MS) .
|
-
- HY-N0506R
-
|
|
Interleukin Related
|
Neurological Disease
|
|
Rosarin (Standard) is the analytical standard of Rosarin. This product is intended for research and analytical applications. Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .
|
-
- HY-114527
-
|
|
Apoptosis
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
|
-
- HY-169080
-
|
|
Apolipoprotein
|
Neurological Disease
|
|
ABCA1 inducer 1 is a nonlipogenic ABCA1 inducer. ABCA1 inducer 1 increases ABCA1 expression, enhances apolipoprotein (APOE) lipidation and reverses multiple Alzheimer’s disease (AD) phenotypes, without increasing triglycerides in E3/4FAD mice that express human APOE 3/4 .
|
-
- HY-168567
-
|
|
RIP kinase
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
RIPK2-IN-6 (Compound 15a) is an inhibitor for RIPK, that inhibits the phosphorylation of RIPK2, and thus inhibits the NF-κB and MAPK signaling pathways. RIPK2-IN-6 exhibits anti-inflammatory and anti-fibrotic activities in Dextran sodium sulfate (HY-116282C)-induced mice colitis models .
|
-
- HY-159895
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice .
|
-
- HY-123733A
-
|
RPS-001 TFA
|
PSMA
|
Cancer
|
|
MIP-1095 (RPS-001) TFA is a potent inhibitor of PSMA with good biodistribution and efficient targeting of tumor lesions. In applications, MIP-1095 TFA will be isotopically labeled ( 131I labeled) as an imaging probe to indicate tumor progression. And 131I-MIP-1095 showed higher renal uptake in mice .
|
-
- HY-148016
-
|
|
Protease Activated Receptor (PAR)
ERK
|
Inflammation/Immunology
|
|
I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research .
|
-
- HY-12678
-
|
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-N0088
-
|
Acetovanillone
|
NADPH Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
|
-
- HY-14452
-
|
125B11
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
|
-
- HY-103157
-
|
NSC168807
|
Autophagy
Ferroptosis
|
Cardiovascular Disease
|
|
PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice .
|
-
- HY-N2342
-
|
PCC1
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
|
-
- HY-117370
-
|
AZ1
|
Deubiquitinase
|
Cancer
|
|
USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model .
|
-
- HY-108742A
-
|
BA 058 TFA; BIM 44058 TFA
|
Arrestin
PTHR
|
Metabolic Disease
Endocrinology
Cancer
|
|
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis .
|
-
- HY-N5097
-
|
|
PPAR
|
Metabolic Disease
|
|
13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice .
|
-
- HY-116175
-
|
|
Others
|
Metabolic Disease
|
|
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL) .
|
-
- HY-B1794A
-
|
|
Dopamine Receptor
Histamine Receptor
Bacterial
Amyloid-β
|
Infection
Neurological Disease
|
|
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
|
-
- HY-Z0283
-
|
Benzenecarboxamide; Phenylamide
|
Endogenous Metabolite
PARP
|
Others
|
|
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-N2573
-
|
L-Corydalmine; TLZ-16
|
Fungal
CXCR
|
Infection
Neurological Disease
|
|
Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi . Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
|
-
- HY-131891
-
|
|
mAChR
|
Neurological Disease
|
|
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
|
-
- HY-103089
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression .
|
-
- HY-143793
-
|
|
Lipocalin Family
|
Metabolic Disease
|
|
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice .
|
-
- HY-146505
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice .
|
-
- HY-124813
-
|
113B7
|
FAK
EGFR
MMP
|
Cancer
|
|
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
|
-
- HY-117764
-
|
|
mGluR
|
Neurological Disease
|
|
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
|
-
- HY-146495
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-19 (Compound 1c) is an antitubercular agent. Antitubercular agent-19 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-19 shows low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice .
|
-
- HY-146354
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity .
|
-
- HY-147222
-
SAE-14
1 Publications Verification
GPR183 antagonist-1
|
EBI2/GPR183
|
Neurological Disease
Inflammation/Immunology
|
|
SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC–induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice .
|
-
- HY-P99194
-
|
REGN1500
|
ANGPTL
Others
|
Cardiovascular Disease
Metabolic Disease
|
|
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia .
|
-
- HY-148764
-
|
|
Apoptosis
|
Cancer
|
|
M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer .
|
-
- HY-152199
-
|
|
Adenosine Deaminase
|
Metabolic Disease
|
|
AMPD2 inhibitor 2 (compound 21) is a potent AMP deaminase 2 (AMPD2) inhibitor with IC50s of 0.1 μM and 0.28μM for hAMPD2 and mAMPD2, respectively. AMPD2 inhibitor 2 has the potential for evaluating the physiological role of AMPD2 in mice maintained on a high fat diet .
|
-
- HY-P4154
-
|
ALM-488
|
Fluorescent Dye
|
Neurological Disease
Cancer
|
|
Bevonescein (ALM-488) is a novel, intravenously-administrated fluorescein-conjugated peptide that binds nerve-associated connective tissue, labels peripheral nerves under real-time fluorescence imaging (FL) in living mice and human ex vivo nerve tissue. Bevonescein is a peptide-linked tracer which fluorescently labeled both intact and degenerated nerves .
|
-
- HY-150236
-
|
|
Huntingtin
|
Neurological Disease
|
|
FITC-labeled Tominersen (sodium) is the Tominersen labeled with FITC. Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
|
-
- HY-117924
-
|
Autophagy enhancer-67
|
Autophagy
|
Neurological Disease
|
|
AUTEN-67 (Autophagy enhancer-67) is an orally active autophagy enhancer and MTMR14 inhibitor. AUTEN-67 has anti-aging and neuroprotective effects. AUTEN-67 protects neurons from stress-induced cell death. AUTEN-67 also restores nesting behavior in a mice model of Alzheimer disease .
|
-
- HY-N12042
-
-
- HY-110218
-
CW 008
1 Publications Verification
|
PKA
Epigenetic Reader Domain
|
Others
|
|
CW 008, a derivative of pyrazole-pyridine, is a CREB or PKA pathway agonist. CW 008 also is a stem cell differentiating agent. CW 008 stimulates osteoblast differentiation of human MSCs and increases bone formation in ovariectomized mice. CW008 promotes osteogenesis by activating cAMP/PKA/CREB signaling pathway and inhibiting leptin secretion .
|
-
- HY-149766
-
|
|
HDAC
|
Neurological Disease
|
|
PB94 is a selective HDAC11 inhibitor (IC50=108 nM). PB94 can be radiolabeled as [11C]-PB94 for use in positron emission tomography (PET), as well as brain uptake and metabolic properties in administered live animals. PB94 improves neuropathic pain in mice and could be used to study neurological indications .
|
-
- HY-157429
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
25N-N1-Nap (compound 16) is a β-arrestin-biased 5-HT2A agonist. 25N-N1-Nap antagonizes phencyclidine induced hyperactivity in Male C57BL/6 J mice .
|
-
- HY-N7741
-
|
Dehydrozaluzanin C-derivative
|
Others
|
Infection
Inflammation/Immunology
|
|
Isozaluzanin C (Dehydrozaluzanin c-derivative) is an anti-inflammatory agent that can be isolated from Saussurea lappa and has immunomodulatory effects. Isozaluzanin C improves tissue damage (lung, kidney, and liver) and excessive inflammation in mice induced by LPS (HY-D1056) or CRKP infection. Isozaluzanin C can be used in the study of bacterial infections and sepsi .
|
-
- HY-100442S
-
|
ABR-215757-d5; ABR 25757-d5
|
SARS-CoV
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
|
-
- HY-B1002R
-
|
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Infection
|
|
Oxolinic acid (Standard) is the analytical standard of Oxolinic acid. This product is intended for research and analytical applications. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice .
|
-
- HY-161425
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
|
-
- HY-126617
-
|
NSC 258308
|
Others
|
Cancer
|
|
Duclauxin decreases proliferation of tumor cells in vitro and increases the lifespan of mice innoculated with Ehrlich ascitic tumor cells. Duclauxin (10-30 μg/mL) inhibits mitochondrial respiration of P-388 tumor cells and nucleic acid synthesis in cell culture of Ehrlich cancer, the lymphadenomas NK/LI and L 5178, and sarcoma 37. Duclauxin also inhibits growth of wheat coleoptile.
|
-
- HY-113958
-
|
LM-2219
|
Others
|
Others
|
|
Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
|
-
- HY-121798
-
|
|
PPAR
|
Metabolic Disease
|
|
TZD18 is a potent and orally active PPARα and PPARγ dual agonist with IC50 values of 0.028, 0.057, >10 µM for PPARα, PPARγ, PPARδ, respectively. TZD18 reduces plasma levels of both glucose and triglycerides in diabetic mice. TZD18 has the potential for the research of type 2 diabetes .
|
-
- HY-117446
-
|
|
GPR119
|
Metabolic Disease
|
|
AS-1669058 is a GPR119 agonist and a potential inhibitor of type 2 diabetes. AS-1669058 induces insulin secretion in response to high blood glucose levels in vitro and in vivo and increases insulin promoter activity. In animal studies, AS-1669058 improved glucose tolerance and reduced blood glucose levels in db/db mice .
|
-
- HY-118184
-
|
|
PGE synthase
|
Cancer
|
|
AF3485 is a human mPGES-1 inhibitor that exhibits antitumor activity in vitro and in vivo. AF3485 inhibits tumor-associated angiogenesis by reducing PGE2 production, inhibiting EGFR signaling, and decreasing VEGF and FGF-2 expression. AF3485 reduced tumor growth in mice bearing human A431 xenograft tumors by subchronic administration.
|
-
- HY-120550
-
|
|
Parasite
|
Infection
|
|
RS 49676 is an N-substituted imidazole compound that exhibits strong in vitro activity against endogenous amoebae (ED50 < 0.1 ng/mL), but is ineffective against exogenous amoebae (epimastigotes). In vivo, RS 49676 (100 mg/kg/d, sc, 2 times) can prolong the average survival time of mice infected with Trypanosoma cruzi to more than 11 weeks.
|
-
- HY-164311
-
|
|
Others
|
Neurological Disease
|
|
GPR17 modulator-1 (Compound 2-046) is a modulator for G protein-coupled receptor 17 GPR17, with an IC50<10 nM for hGPR17 in CHO. GPR17 modulator-1 exhibits moderate pharmacokinetic characteristics in mice. GPR17 modulator-1 ix blood-brain barrier (BBB) permeable .
|
-
- HY-164397
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC50s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .
|
-
- HY-165035
-
|
Glucocerebrosides; Gaucher cerebroside; GluCers (gaucher's spleen)
|
Endogenous Metabolite
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Neurological Disease
Metabolic Disease
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Glucosylceramides are sphingolipid molecules found in both neuronal and non-neuronal mammalian tissues, as well as in low quantities across various plant species. Elevated levels of glucosylceramides provide cellular protection and prepare certain cells for proliferation; however, they have also been linked to obesity-induced insulin resistance in mice and to neuronal deficits observed in neuronopathic Gaucher disease .
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- HY-N1388R
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Others
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Inflammation/Immunology
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Tussilagone (Standard) is the analytical standard of Tussilagone. This product is intended for research and analytical applications. Tussilagone, a major active component in Tussilago farfara, has anti-inflammatory effect. Tussilagone ameliorates inflammatory responses in dextran sulphate sodium-induced murine colitis. Tussilagone inhibits the inflammatory response and improves survival in cecal ligation and puncture (CLP)-induced septic mice .
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- HY-N6857R
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NF-κB
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Inflammation/Immunology
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Armepavine (Standard) is the analytical standard of Armepavine. This product is intended for research and analytical applications. Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades .
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- HY-P10707
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Endogenous Metabolite
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Inflammation/Immunology
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Tpp-CAQK can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK, with excellent bioactivity. Mito-Tpp-CAQK can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury .
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- HY-164462
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PKC
NF-κB
Apoptosis
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Cancer
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BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
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- HY-169018
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- HY-164607
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DNA/RNA Synthesis
Others
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Cancer
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YL-5092 is an inhibitor for YT521-B homology (YTH) domain-containing protein 1 (YTHDC1). YL-5092 inhibits acute myeloid leukemia cell with IC50 of 0.28-2.87 μM. YL-5092 exhibits antitumor efficacy in MOLM-13 or U937 xenograft mice .
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- HY-116182
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Influenza Virus
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Infection
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RO5487624, an analogue of RO5464466 (HY-120690), is an orally active hemagglutinin (HA) inhibitor of influenza H1N1 viruses that abolishes influenza virus fusion by blocking HA conformational changes in low pH environments. RO5487624 displays a protective effect on mice that are lethally challenged with influenza H1N1 virus .
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- HY-116145
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Tyrosinase
NF-κB
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Inflammation/Immunology
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MHY884 is a tyrosinase inhibitor that suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress. MHY884 suppresses oxidative stress in the melanoma cells and attenuates UVB-induced oxidative stress, resulting in reduced NF-κB activity in irradiated mice. MHY884 is promising for research of UVB-induced skin damage .
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- HY-114724
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Histamine Receptor
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Inflammation/Immunology
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HSR-609 is an orally active amphoteric antiallergic agent. HSR-609 has a high affinity for histamine H1-receptor in the guinea pig cerebral cortex. HSR-609 inhibits allergic airway hyperresponsiveness to Acetylcholine. HSR-609 shows poor ability to penetrate into the CNS in mice and guinea pigs .
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- HY-10289
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RO-4876904
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Dipeptidyl Peptidase
P-glycoprotein
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Cardiovascular Disease
Metabolic Disease
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Carmegliptin (RO-4876904) is an orally active, potent and long-acting dipeptidyl peptidase IV inhibitor. Carmegliptin is also a substrate of P-glycoprotein that synergizes with Verapamil (HY-14275). Carmegliptin improves insulin sensitivity and reduces hepatic glucose production in hyperglycemic mice. Carmegliptin is promising for research of type 2 diabetes, hypertension and cardiovascular disease .
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- HY-105578A
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MA 1143 hydrochloride
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Others
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Inflammation/Immunology
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Letimide hydrochloride (MA 1143 hydrochloride) is an analgesic with potent analgesic activity. Letimide hydrochloride has shown cytogenetic effects on human lymphocytes in in vitro experiments. Letimide hydrochloride did not exhibit significant chromosomal aberrations or sister chromatid exchanges in in vivo studies in mouse bone marrow cells. Teratogenic studies conducted on mice with Letimide hydrochloride also did not show obvious effects on inducing congenital malformations .
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- HY-W110242A
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Others
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Cardiovascular Disease
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(S)-CPP sodium serves as an inhibitor of the branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase, commonly referred to as BDK or keto acid dehydrogenase kinase. As a negative regulator of BCKDC activity, the inhibition of BDK by (S)-CPP (with an IC50 of 6.3 μM) results in the activation of the complex and a notable decrease in plasma levels of leucine/isoleucine and valine in wild-type mice.
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- HY-168572
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BCRP
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Cancer
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MZ82, Ko 143 (HY-10010) derivative, is a ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor with the IC50 of ~23 nM. MZ82 not only shows greatly improved metabolic stability over Ko 143 (HY-10010) in liver microsomes but also in mice, and is able to penetrate into the brain .
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- HY-W012481
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Ethylphenylhydantoin; Phenylethyihydantoin; Desmethylmephenytoin
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Drug Metabolite
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Neurological Disease
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Nirvanol is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the Maximal Electroshock (M.E.S.) seizure model in mice. The ED50 of Nirvanol is 23 mg/kg (measured 30 minutes after intraperitoneal injection) and 30 mg/kg (measured 2 hours after intraperitoneal injection). Nirvanol shows potential for research in epilepsy-related neurological disorders .
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- HY-W587957
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Bacterial
Parasite
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Infection
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Gypsogenic acid is a triterpenoid acid that can be isolated from Miconia stenostachya and has antibacterial and trypanoidal activities. The MICs values of Gypsogenic acid for the oral bacterial pathogens Enterococcus faecalis, Streptococcus salivarius, Streptococcus haematococcus, Streptococcus mutans and sobrinus were 50-200 μg/mL. Gypsogenic acid can induce blood cortensite cleavage in isolated mice with IC50 56.6 μM .
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- HY-143330
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
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- HY-155068
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Reactive Oxygen Species
Apoptosis
Microtubule/Tubulin
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Cancer
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FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research .
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- HY-106129
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LY 320236
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5 alpha Reductase
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Endocrinology
Cancer
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Izonsteride (Compound LY320236) is an inhibitor of 5α-reductase (IC50 = 11.6 nM for type I; 7.37 nM for type II). LY320236 inhibits the activity of steroid 5α-reductase, preventing the conversion of testosterone (T) to dihydrotestosterone (DHT). LY320236 can significantly inhibit the growth of LNCaP tumors in thymic mice without exhibiting obvious host toxicity .
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- HY-158374
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IRAK
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Inflammation/Immunology
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BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
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- HY-B0111
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Dihydrospirorenone
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Progesterone Receptor
Androgen Receptor
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Endocrinology
Cancer
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Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
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- HY-111603
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Apoptosis
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Metabolic Disease
Inflammation/Immunology
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Calcium dobesilate is a vascular protector with oral activity that can clear hydroxyl free radicals, with an IC50 of 1.1 pM. Calcium dobesilate has antioxidant activity and helps to reduce oxidative stress and inflammation in the retinas of diabetic mice. Calcium dobesilate can be used to study chronic venous diseases, diabetic retinopathy, and the occurrence of hemorrhoids, among other conditions .
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- HY-126255
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NAMPT
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Metabolic Disease
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SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD +. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD + in mice .
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- HY-107818
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NF-κB
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Cardiovascular Disease
Inflammation/Immunology
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4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
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- HY-P1216
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Melanocortin Receptor
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Neurological Disease
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HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
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- HY-108497A
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Somatostatin Receptor
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Neurological Disease
Cancer
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L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice .
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- HY-124290
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AJM300
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Integrin
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Inflammation/Immunology
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Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice .
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- HY-131881
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mAChR
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Neurological Disease
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JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
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- HY-145153
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Cannabinoid Receptor
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Neurological Disease
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S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
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- HY-110190
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ML396
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mGluR
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Neurological Disease
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VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice .
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- HY-146723
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IKK
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Inflammation/Immunology
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IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality .
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- HY-126477
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NNK
1 Publications Verification
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Endogenous Metabolite
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Cancer
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NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
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- HY-146497
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones .
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- HY-33009
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Others
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Neurological Disease
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AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia .
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- HY-148141
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Complement System
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Inflammation/Immunology
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JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases .
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- HY-105070
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E5564 free base
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EBV
Toll-like Receptor (TLR)
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Infection
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Eritoran （E5564 free base） is a Toll-like receptor 4 (TLR4) antagonist. Eritoran protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran inhibits pathogenesis of filovirus infection. Eritoran has anti-inflammatory activity .
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- HY-155539
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Others
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Inflammation/Immunology
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Cisd2 agonist 2 (compound 6) is an orally active Cisd2 activator (EC50=191 nM), while the Cisd2 levels is correlated with nonalcoholic fatty liver disease (NAFLD). Cisd2 agonist 2 has no significant toxicity in vivo in Cisd2hKO-het mice (heterozygous hepatocyte-specific Cisd2 knockout) .
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- HY-149333
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Bacterial
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Infection
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BO-1 is a benzoate ester with antibacterial activity. BO-1 inhibits multidrug-resistant Staphylococcus aureus, and acts function synergistically with antibiotic, such as Ciprofloxacin (HY-B0356). BO-1 can reverse the resistance of antibiotic-resistant S. aureus strains, and decreases the level of inflammatory factors IL-6 and C-reactive protein in vivo in mice .
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- HY-W024365
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PROTAC Linkers
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Cancer
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3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system .
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- HY-156109
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PDHK
Mitochondrial Metabolism
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Cancer
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PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
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- HY-P3248
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Myelin basic protein (85-99) antagonist
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Biochemical Assay Reagents
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Inflammation/Immunology
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J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
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- HY-P1173
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Myristoylated L 803; GSK-3β Inhibitor XIII
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GSK-3
Amyloid-β
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Neurological Disease
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L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
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- HY-155463
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NOD-like Receptor (NLR)
Interleukin Related
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Inflammation/Immunology
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NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM .
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- HY-119678
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AMPK
Keap1-Nrf2
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Cardiovascular Disease
Metabolic Disease
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Fortunellin, is a flavonoid, that can be isolated from the fruits of Fortunella margarita (kumquat). Fortunellin exhibits little toxicity to mice and suppresses inflammation and ROS generation in H9C2 cells induced by LPS. Fortunellin protects against fructose-induced inflammation and oxidative stress by enhancing AMPK/Nrf2 pathway. Fortunellin can be used for diabetic cardiomyopathy research .
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- HY-100442S1
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- HY-122964
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Cannabinoid Receptor
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Metabolic Disease
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URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity .
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- HY-12557
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CaSR
Wnt
TNF Receptor
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Inflammation/Immunology
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γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation .
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- HY-109506S2
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(Rac)-129Y83-d6
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Isotope-Labeled Compounds
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Others
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(Rac)-DPPC-d6 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
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- HY-163797
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-40156A
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Bacterial
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Infection
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Mycobacterium Tuberculosis-IN-5 (Compound 11) is the HCl salt form of 5-Fluoroindole (HY-40156). Mycobacterium Tuberculosis-IN-5 is an antibacterial agent, that inhibits Mycobacterium tuberculosis with a MIC of 29.1 μM. Mycobacterium Tuberculosis-IN-5 exhibits metabolic stability in rat liver microsomes. Mycobacterium Tuberculosis-IN-5 exhibits anti-tuberculosis efficacy in mice .
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- HY-125677
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Caspase
Reactive Oxygen Species
Apoptosis
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Cancer
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SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC50 of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active .
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- HY-W781133
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cis-[Pt(NH3)2(N1-pyridine)Cl]Cl
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Others
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Cancer
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cDPCP (cis-[Pt(NH3)2(N1-pyridine)Cl]Cl) is a DNA crosslinking agent and also a substrate for OCT1 and OCT2. DPCP exhibits anticancer activity and can improve the survival rate of sarcoma-180 mice. cDPCP is suitable for the research of colorectal cancer and cancers with appropriate cation transporters .
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- HY-N7272R
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Phosphodiesterase (PDE)
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Metabolic Disease
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Cirsimarin (Standard) is the analytical standard of Cirsimarin. This product is intended for research and analytical applications. Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
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- HY-163978
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Adenosine Receptor
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Neurological Disease
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YGZ-331 is a sedative with a calming effect. YGZ-331 is a derivative of the adenosine nucleoside NGBA, which can increase GABA levels. YGZ-331 exerts a sedative-hypnotic effect by activating A1R and A2aR, and inhibiting CaMKII phosphorylation (pCaMKII) levels. YGZ-331 can reduce the spontaneous motor activity of mice .
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- HY-169026
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TGF-beta/Smad
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Cardiovascular Disease
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DCN1-IN-2 is a DCN1 inhibitor with an IC50 value of 2.96 nM. DCN1-IN-2 can alleviate Ang II/TGFβ-induced activation of cardiac fibroblasts. DCN1-IN-2 can reduce ISO-induced cardiac fibrosis and remodeling in mice by selectively inhibiting cullin 3 .
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- HY-N11286R
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Others
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Tridocosahexaenoylglycerol (Standard) is the analytical standard of Tridocosahexaenoylglycerol. This product is intended for research and analytical applications. Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases .
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- HY-12184
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Others
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Cardiovascular Disease
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ONO-AE 248 is a selective EP3 receptor agonist with cardioprotective activity. ONO-AE 248 reduces myocardial infarction size by selectively binding to the EP3α receptor in mice. The cardioprotective effect of ONO-AE 248 is independent of hemodynamic effects. The mechanism of ONO-AE 248 may involve activation of protein kinase C and opening of K(ATP) channels .
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- HY-165421
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Mps1
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Cancer
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Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
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- HY-169240
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MDM-2/p53
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Cancer
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MX69-102 (compound MX69-102) is an MDM-2/p53 inhibitor, inducing MDM2 degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice. .
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- HY-109506R
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Liposome
Endogenous Metabolite
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Others
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DPPC (Standard) is the analytical standard of DPPC. This product is intended for research and analytical applications. DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
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- HY-N0283
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Diacerhein; Diacetylrhein
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Interleukin Related
Calcium Channel
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Inflammation/Immunology
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Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research .
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- HY-18100A
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Sigma Receptor
Akt
NO Synthase
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Cardiovascular Disease
Neurological Disease
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PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
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- HY-110279
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Ogerin
1 Publications Verification
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GPR68
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Neurological Disease
|
|
Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders .
|
-
- HY-N6967
-
|
(-)-α-Bisabolol
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-125858
-
MI-1061
1 Publications Verification
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-B1640
-
|
Etacrynic acid
|
Glutathione S-transferase
NF-κB
Calcium Channel
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma .
|
-
- HY-W010042
-
|
L-(-)-Glucose
|
Others
|
Metabolic Disease
Cancer
|
|
L-Glucose (L-(-)-Glucose) is a stereoisomer of D-Glucose (HY-B0389), which does not readily enter the brain. L-Glucose can promote food intake. L-glucose is combined with a fluorescence detector to produce a fluorescent probe that can be used to visualize and characterize cancer cells. L-Glucose also can be used in the research to enhance memory in mice .
|
-
- HY-N7515
-
|
2',4',6'-Trihydroxychalcone
|
Bacterial
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Pinocembrin chalcone (2',4',6'-Trihydroxychalcone) is an antibacterial compound from Helichrysum Trilineatum. Pinocembrin chalcone facilitates AMP-activated protein kinase (AMPK) activation, improves glucose tolerance, increases muscle FAO and reduces fat accumulation in the liver and skeletal muscles in high-fat diet-induced (HFD) diabetic mice. Pinocembrin chalcone is promising for research of gastric ulcers and diabetes .
|
-
- HY-P1439A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
|
-
- HY-134901
-
WM-3835
2 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice .
|
-
- HY-144899
-
|
|
Notch
|
Cancer
|
|
ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice .
|
-
- HY-101064S2
-
|
N-FMOC-leucine-d3; NPC 15199-d3; NSC 334290-d3
|
PPAR
|
Metabolic Disease
|
|
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
|
-
- HY-101064S3
-
|
|
PPAR
|
Metabolic Disease
|
|
Fmoc-leucine-d10 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
|
-
- HY-123671
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy .
|
-
- HY-146435
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice .
|
-
- HY-146458
-
|
|
Bacterial
Cytochrome P450
|
Infection
|
|
Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice .
|
-
- HY-150654
-
|
|
Histone Methyltransferase
|
Cancer
|
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
|
-
- HY-148038
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice .
|
-
- HY-147395
-
|
|
GPR52
|
Neurological Disease
|
|
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .
|
-
- HY-151451
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca 2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain .
|
-
- HY-N11020
-
|
|
EBV
|
Infection
Inflammation/Immunology
|
|
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation .
|
-
- HY-114440
-
|
GR-MD-02
|
Galectin
Apoptosis
|
Cancer
|
|
Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM .
|
-
- HY-P99588
-
|
MYO-029
|
TGF-β Receptor
|
Metabolic Disease
|
|
Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research .
|
-
- HY-18100
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-113354S1
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
|
-
- HY-120171
-
|
|
DAGL
MAGL
|
Metabolic Disease
|
|
DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice . DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-153903
-
|
|
Others
|
Others
|
|
RASP-IN-1 (compound A) is a lipophili ccompound used for macular degeneration inhibition. RASP-IN-1 is biologically active in the retina of the rabbit's eye. Thirty minutes after IP treatment with 14C-RASP-IN-1 (10 mg/kg)，the Cmax amount of 14C-RASP-IN-1 in the posterior eye cup is 14.36 μg/g in mice model .
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-156120
-
|
|
CD38
|
Metabolic Disease
|
|
CD38 inhibitor 3 (compound 1) is a potent CD38 inhibitor (IC50=11 nM). CD38 inhibitor 3 can promote mitochondrial biogenesis, reduce lactate levels, and increase NAD+ content and Nrf2 expression. In a model of mitochondrial myopathy, CD38 inhibitor 3 increases muscle contraction/development and improves exercise tolerance in Pus1 -/- mice .
|
-
- HY-100840
-
|
(S)-4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
|
(S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice .
|
-
- HY-156374
-
|
|
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
|
|
D359-0396 is an orally active NLRP3 inflammasome inhibitor. D359-0396 inhibits pyroptosis and IL-1β release in macrophages. D359-0396 also inhibits the oligomerization of NLRP3, ASC and the cleavage of GSDMD. D359-0396 alleviates EAE, and also improves survival after septic shock in mice .
|
-
- HY-155478
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
|
-
- HY-161373
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
|
-
- HY-162428
-
|
|
Phosphatase
|
Cancer
|
|
PTPN2/1-IN-3 (compound 4) is a modified, orally active PTPN2/N1 inhibitor based on ABBV-CLS-484 (HY-145923). PTPN2/1-IN-3 has anti-tumor effects, inhibiting PTPN2 with an IC50 of 9.3 nM and having an oral bioavailability of 93% in mice .
|
-
- HY-158991
-
|
|
CFTR
|
Inflammation/Immunology
|
|
I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents .
|
-
- HY-109506S9
-
|
129Y83-13C2
|
Isotope-Labeled Compounds
Endogenous Metabolite
Liposome
|
Others
|
|
DPPC-13C2 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
|
-
- HY-163651
-
|
(R)-CR6086
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
(R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with Ki of 16.6 nM for human EP4. (R)-Vorbipiprant inhibits PGE2 (HY-101952)-induced cAMP production with an IC50 of 22 nM. (R)-Vorbipiprant exhibits immunomodulatory and anti-angiogenic activities, and ameliorates the collagen-induced arthritis in mice .
|
-
- HY-16121
-
|
|
Cathepsin
|
Others
|
|
CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. CAA-0225 can participate in the degradation of autophagosome membrane markers LC3-II and GABARAP (HY-P72639), improve cardiac function in mice with reperfusion injury, and kill and eliminate Trypanosoma brucei parasites [1][2][3].
|
-
- HY-162646
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg) .
|
-
- HY-117446A
-
|
|
GPR119
|
Metabolic Disease
|
|
AS-1669058 free base is a GPR119 agonist and a potential inhibitor of type 2 diabetes. AS-1669058 free base induces insulin secretion induced by high blood glucose levels in vitro and in vivo and increases insulin promoter activity. In animal studies, AS-1669058 free base improved glucose tolerance and reduced blood glucose levels in db/db mice.
|
-
- HY-161853
-
|
|
Others
|
Others
|
|
TX-2552 is an orally active tyrosine DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 value of 0.62 μM. TX-2552 can enhance the clastogenic activity of Topotecan (HY-13768) in mouse bone marrow cells, as well as the anti-tumor effect of Topotecan (HY-13768) in Krebs-2 ascites tumor mice .
|
-
- HY-162867
-
|
|
Ferroptosis
|
Cancer
|
Photosensitizer-5 is a photosensitizer. Photosensitizer-5 has cytotoxicity against HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. Photosensitizer-5 can lead to lipid peroxidation and induces cell death through an iron-independent ferroptosis-like pathway. Photosensitizer-5 shows anti-tumor activity in HeLa tumor-bearing mice .
|
-
- HY-106110
-
|
|
Others
|
Metabolic Disease
|
OP-2507 is a prostacyclin analog. OP-2507 can increase brain glucose levels in mice, suppress the breakdown of energy metabolism under hypoxic conditions, and has a protective effect against changes in cyclic nucleotides in hypoxic brain tissue (specifically, an increase in cyclic AMP and a decrease in cyclic GMP). OP-2507 provides protective effects against brain hypoxia and edema .
|
-
- HY-101775
-
|
|
Topoisomerase
|
Cardiovascular Disease
Cancer
|
|
9-hydroxyellipticine is an inhibitor of Topo II and RyR, exhibiting high affinity for DNA with a Pka value of 9.8 at pH 7.4. It has antitumor, antioxidant, and catecholamine-releasing activities, with IC50 values of 1.6 μM and 1.2 μM for Hela S-3 and 293T cells, respectively. It also demonstrates anticancer effects in L1210 leukemia mice .
|
-
- HY-N1428AR
-
|
|
Endogenous Metabolite
Apoptosis
Antibiotic
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid (monohydrate) (Standard) is the analytical standard of Citric acid (monohydrate). This product is intended for research and analytical applications. Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
-
- HY-162928
-
|
|
RIP kinase
|
Neurological Disease
|
|
RIPK1-IN-26 (Compound 8a) is a potent receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitor with cell anti-necroptosis potency. RIPK1-IN-26 demonstrats good metabolic stability and good binding specificity in mice. RIPK1-IN-26 is promising for research of PET imaging probe development and neurodegenerative disorders .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-100384
-
NKL 22
1 Publications Verification
|
HDAC
|
Neurological Disease
|
|
NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (HDAC), with an IC50 of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 exhibits selectivity over HDAC2/4/5/7/8 (IC50≥1.59 μM). NKL 22 ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice .
|
-
- HY-10626
-
|
|
LXR
FXR
ROR
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
|
-
- HY-N0307
-
|
|
Bcl-2 Family
|
Neurological Disease
|
|
Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory .
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation .
|
-
- HY-114169
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
|
-
- HY-110247
-
|
|
TNF Receptor
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques .
|
-
- HY-14452A
-
|
125B11 hydrobromide
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
|
-
- HY-P2260
-
|
|
Autophagy
HIV
|
Infection
|
|
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
|
-
- HY-P1259
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-122920
-
|
|
HSV
CMV
Influenza Virus
HIV
NOD-like Receptor (NLR)
YB-1
|
Infection
Inflammation/Immunology
|
|
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure .
|
-
- HY-125858A
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-103017A
-
|
|
IRAK
|
Infection
Inflammation/Immunology
Cancer
|
|
JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice . JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM .
|
-
- HY-12363
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
U-69593 is a potent and selective κ1-opioid receptor agonist . U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
|
-
- HY-144743
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research .
|
-
- HY-147692
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-14 (compound 2a) is a potent and selective COX-2 (cyclooxygenase-2) inhibitor. COX-2-IN-14 shows effective binding at the active site of COX-2 co-crystal. COX-2-IN-14 exhibits a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity in mice .
|
-
- HY-120589
-
|
|
mGluR
|
Neurological Disease
|
|
VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice . VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-132246
-
|
|
MAGL
|
Neurological Disease
|
|
WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
|
-
- HY-D1460
-
|
|
Bacterial
|
Infection
|
|
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies .
|
-
- HY-150501
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Diprovocim-X (compound 35) is a potent TLR1/TLR2 (toll-like receptor 1/2) agonist, with EC50 values of 0.14 and 0.75 nM for hTLR1/TLR2 and mTLR1/TLR2, respectively. Diprovocim-X is a potent adjuvant in vivo in mice, and serves to stimulate the adaptive immune response .
|
-
- HY-150723
-
|
|
Glucosidase
|
Metabolic Disease
|
|
PBI-6DNJ is an orally active and potent multivalent glycosidase inhibitor. PBI-6DNJ exhibits good inhibition activity against α-glucosidase from mice, with a Ki of 0.14 μM. PBI-6DNJ exhibits good hypoglycemic activity. PBI-6DNJ can be used for type 2 diabetes research .
|
-
- HY-151606
-
|
|
Akt
|
Cancer
|
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-123297
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes .
|
-
- HY-151876
-
|
|
Glucocorticoid Receptor
NF-κB
AP-1
|
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice .
|
-
- HY-125639
-
|
(rac)-AR-13324 M1 metabolite
|
PKC
ROCK
|
Cardiovascular Disease
|
|
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .
|
-
- HY-129163
-
|
10-Acetylphenoxazine
|
Pim
|
Cancer
|
|
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
|
-
- HY-149218
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research .
|
-
- HY-N0278A
-
|
(Rac)-Pulsatilla camphor; (Rac)-Anemonine
|
PKC
NO Synthase
|
Inflammation/Immunology
|
|
(Rac)-Anemonin ((Rac)-Pulsatilla camphor) is the diastereoisomer of Anemonin (HY-N0278). Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases .
|
-
- HY-149478
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
JT002 is an orally active inhibitor of the NLRP3 inflammasome. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice .
|
-
- HY-155991
-
|
|
Apoptosis
|
Cancer
|
|
RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity .
|
-
- HY-155193
-
|
|
Others
|
Inflammation/Immunology
|
|
XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
|
-
- HY-157082
-
|
|
Enterovirus
|
Infection
|
|
ZHSI-1 is an EV71 (Enterovirus 71) inhibitor that inhibits EV71/CVA16 replication and virus-induced pyroptosis associated with viral pathogenesis. ZHSI-1 effectively prevents EV71 infection in neonatal and young mice in animal models. ZHSI-1 can be used to study viral infections such as hand, foot and mouth disease (HFMD) .
|
-
- HY-120657
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
|
9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation. 9-PAHSA also improved carotid vascular calcification and attenuates cardiac hypertrophy and dysfunction in db/db mice. 9-PAHSA increases the viability of steatosis primary mouse hepatocytes (PMH). 9-PAHSA can be used in research on diabetes, inflammation, and cardiovascular disease .
|
-
- HY-157646
-
|
GYS1-IN-2
|
Others
|
Metabolic Disease
|
|
MZ-101 (GYS1-IN-2) is an orally active, potent and selective small-molecule glycogen synthase 1 (GYS1) inhibitor with with an IC50 value of 0.041 µM. MZ-101 reduces glycogen concentrations in cells and in mice. MZ-101 can used to study GYS1 -mediated Pompe disease and other glycogen storage diseases .
|
-
- HY-125527A
-
|
17(R)-RvD1; AT-RvD1
|
TRP Channel
|
Inflammation/Immunology
|
|
17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
- HY-162312
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-15805
-
|
|
Src
Btk
|
Cancer
|
|
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
|
-
- HY-105070A
-
|
E5564
|
EBV
Toll-like Receptor (TLR)
|
Infection
Inflammation/Immunology
|
|
Eritoran tetrasodium (E5564) is a Toll-like receptor 4 (TLR4) antagonist. Eritoran tetrasodium protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran tetrasodium decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran tetrasodium inhibits pathogenesis of filovirus infection. Eritoran tetrasodium has anti-inflammatory activity .
|
-
- HY-N1428S6
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Apoptosis
Antibiotic
|
Cancer
|
|
Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
|
-
- HY-B1266R
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine (salicylate) (Standard) is the analytical standard of Physostigmine (salicylate). This product is intended for research and analytical applications. Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning .
|
-
- HY-161901
-
|
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
BC-1293 is an inhibitor for E3 ligase subunit FBXO24. BC-1293 disrupts the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2) and increases the level of DARS2. BC-1293 increases levels of IL-1β, IL-9, MIP-2, and TNF α, and exhibits immunostimulatory activity in mice .
|
-
- HY-N0219R
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
|
-
- HY-P10653
-
|
|
HCV
HIV
|
Infection
|
|
C5A is a microbicidal peptide, anti-hepatitis C virus (HCV), and anti-HIV agent. C5A disrupts the membrane integrity of the HIV virion as well as the integrity of the conical capsid core that surrounds the viral genome. C5A inhibits in vitro infectivity of a broad range of primary HIV isolates in various primary target cells. C5A protects mice against vaginal and rectal HIV challenges .
|
-
- HY-159602
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BET BD2-IN-3 (compound I-58) is an inhibitor of BET, targeting the BD2 domain of BET. BET BD2-IN-3 can be radiolabeled with [11C] for positron emission tomography (PET) imaging. BET [11C]BD2-IN-3 showed suitable biodistribution in peripheral organs and tissues in PET applications in mice .
|
-
- HY-162831
-
|
|
Mitochondrial Metabolism
|
Others
|
|
MPC-IN-1 (compound 4i) is a cyanocinnamate-based, mitochondrial pyruvate transporter (MPC) inhibitor, and is a derivative of UK-5099 (HY-15475). MPC inhibitors promote the development of hair follicle stem cells without affecting normal cells. MPC-IN-1 promotes cellular lactate production and promotes significant hair growth in mice, and has the potential to be used to inhibit hair loss .
|
-
- HY-119110
-
|
|
MMP
|
Cancer
|
|
LY52 is an MMP-2 and MMP-9 inhibitor. LY52 can significantly block the proteolytic activity of gelatinases, reducing the expression of MMP-2 and MMP-9 in SKOV3 cells, thereby inhibiting cell invasion. LY52 can also suppress the pulmonary metastasis of Lewis lung carcinoma cells in mice. LY52 may be used in cancer research .
|
-
- HY-117569
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
KF24345 free base is an orally active adenosine uptake inhibitor. KF24345 free base inhibits adenosine uptake by human, mouse, rabbit and hamster erythrocytes with IC50 values ??of 59.5, 130.1, 104.2 and 30.9 nM, respectively. KF24345 free base has anti-inflammatory activity and can inhibit LPS-induced TNF-α production and leukopenia in mice .
|
-
- HY-162879
-
|
|
FAK
Src
Akt
Autophagy
|
Cancer
|
FAK inhibitor 7 is a type of FAK inhibitor with an IC50 value of 3.58 nM. FAK inhibitor 7 can inhibit the downstream signaling cascades of FAK (like Src and AKT), causing ovarian cancer cells to stall in the G0/G1 phase and induce cytotoxic autophagy. FAK inhibitor 7 can also suppress tumor metastasis and growth in ovarian cancer mice .
|
-
- HY-118668
-
|
|
Others
|
Others
|
|
ABD-350 is an antiresorptive agent that inhibits osteoclast activity without affecting osteoblast activity and preventing ovariectomy-induced bone loss. ABD-350 inhibits NF-κB ligand-induced inhibitor of NF-κB phosphorylation, leading to osteoclast apoptosis, but has no inhibitory effect on osteoblast function, effectively preventing bone loss in ovariectomized mice, and does not inhibit parathyroid hormone-induced bone formation.
|
-
- HY-122282
-
|
|
Others
|
Cardiovascular Disease
|
|
AZ11657312 is a P2X7 receptor antagonist with activity to restore stress natriuresis. AZ11657312 significantly increased renal medullary perfusion, only in mice treated with angiotensin II. AZ11657312 improves tissue oxygenation by blocking P2X7R, especially in areas of the kidney that are underoxygenated. Administration of AZ11657312 increased sodium excretion up to sixfold while normalizing blood pressure .
|
-
- HY-158315
-
|
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
|
|
NZ-97 is an inhibitor for dipeptidyl peptidase 4 (DPP4) with an IC50 of 18 nM. NZ-97 exhibits a low initial plasma exposure with Cmax of 0.13 µM, which is eliminated in 8 h. NZ-97 ameliorates damage in the Lipopolysaccharides (HY-D1056)-induced lung injury and Bleomycin (HY-108345)-induced lung fibrosis in mice model .
|
-
- HY-107758
-
|
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-113365
-
|
4-Cholesten-3-one
|
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
Cholestenone (4-cholesten-3-one) is an orally available antimicrobial agent that is metabolized primarily in the liver as an intermediate oxidation product of cholesterol. Cholestenone inhibits human dermal fibroblast migration and fights Helicobacter pylori infection in vitro and in mouse models by inhibiting cholesterol-α-D-glucopyranoside (CGL). Cholestenone also alleviates metabolic disorders caused by obesity in db/db mice .
|
-
- HY-N2787
-
|
|
Apoptosis
|
Cancer
|
|
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
|
-
- HY-101478
-
|
|
mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
|
-
- HY-112234
-
|
Sepiapterin
|
Endogenous Metabolite
|
Cancer
|
|
L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression .
|
-
- HY-W010520
-
|
|
Bacterial
MMP
Apoptosis
Fungal
|
Infection
Inflammation/Immunology
|
|
Methylothiazolinone is a bacterial and fungal inhibitor and preservative, as well as a sensitizer. Methylisothiazolinone can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce apoptosis and inflammatory response. Methylisothiazolinone can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
|
-
- HY-115681
-
|
6-Prenylnaringenin; (±)-6-Prenylnaringenin
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
|
-
- HY-P1302
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice .
|
-
- HY-P1259A
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-P2260A
-
|
|
Autophagy
HIV
|
Infection
|
|
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
|
-
- HY-126124
-
AP39
3 Publications Verification
|
Others
|
Cardiovascular Disease
Neurological Disease
|
|
AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research .
|
-
- HY-134923
-
CA77.1
2 Publications Verification
|
Autophagy
|
Neurological Disease
|
|
CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in?lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's?disease research .
|
-
- HY-145313
-
|
|
Others
|
Neurological Disease
|
|
TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC50s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice .
|
-
- HY-124284
-
-
- HY-108790
-
|
Peginterferon β-1a
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Peginterferon beta-1a (Peginterferon β-1a) is the first pegylated interferon beta-1a molecule. Peginterferon beta-1a induces cancer cells apoptosis and shows anti-tumor activities in nude mice models. Peginterferon beta-1a can be used for the research of cancer and multiple sclerosis (RMS) .
|
-
- HY-B1640A
-
|
Etacrynic acid sodium; Sodium etacrynate
|
NF-κB
Glutathione S-transferase
Calcium Channel
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-149984
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model .
|
-
- HY-149296
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK1-IN-12 is a selective inhibitor of JAK1, with IC50 of 0.0246 μM. And IC50s of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2. JAK1-IN-12 promotes hair growth in mice. JAK1-IN-12 can be used for research of immune and inflammatory diseases .
|
-
- HY-W001538
-
|
SPRC
|
STAT
MDM-2/p53
|
Inflammation/Immunology
|
|
S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca 2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties .
|
-
- HY-149428
-
AD4
1 Publications Verification
|
PROTACs
|
Cancer
|
|
AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
|
-
- HY-157252
-
|
|
Liposome
|
Cancer
|
|
CL4F8-6 is an ionizable cationic lipid with a pKa of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice .
|
-
- HY-125019
-
|
|
JAK
STAT
|
Inflammation/Immunology
|
|
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) .
|
-
- HY-161471
-
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Ser/Thr Protease
|
Inflammation/Immunology
|
|
DCLK1-IN-5 (Compound a24) is a DCLK1 inhibitor (IC50: 179.7 nM). DCLK1-IN-5 inhibits lipopolysaccharide (HY-D1056)-induced inflammation via inhibiting DCLK1-mediated IKKβ phosphorylation. DCLK1-IN-5 protects mice against inflammation-induced lung injury and sepsis .
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-
- HY-B1192R
-
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Estrogen Receptor/ERR
HBV
Bcl-2 Family
|
Neurological Disease
|
|
Estradiol benzoate (Standard) is the analytical standard of Estradiol benzoate. This product is intended for research and analytical applications. Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice .
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-
- HY-120600
-
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Necroptosis
Apoptosis
RIP kinase
|
Inflammation/Immunology
|
|
Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis. .
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-
- HY-162754
-
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Proteasome
|
Inflammation/Immunology
|
|
LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits LMP7 and LMP2 with IC50 of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases .
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-
- HY-162757
-
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GABA Receptor
Sodium Channel
|
Neurological Disease
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Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable .
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- HY-119347R
-
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IFNAR
STAT
|
Inflammation/Immunology
Cancer
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Cirsilineol (Standard) is the analytical standard of Cirsilineol. This product is intended for research and analytical applications. Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4+ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice .
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-
- HY-163923
-
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Apoptosis
|
Cancer
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Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg) .
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- HY-164546
-
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STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
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-
- HY-12153
-
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Cholinesterase (ChE)
|
Neurological Disease
|
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JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca 2+ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice .
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- HY-N6869R
-
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Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
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- HY-106899A
-
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(rel)-L-680573
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Others
|
Others
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(rel)-MK 287 ((rel)-L-680573) is a relative configuration of MK 287. MK 287, a tetrahydrofuran analog, potently inhibited [ 3H]C18-PAF binding to human platelet, polymorphonuclear leukocyte (PMN) and lung membranes with Kis of 6.1 nM, 3.2 nM and 5.49 nM, respectively. MK 287 inhibits PAF-induced lethality in mice and PAF-induced bronchoconstriction in guinea pigs .
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-
- HY-402361
-
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MEK
ERK
AP-1
|
Neurological Disease
Inflammation/Immunology
|
|
TERT activator-1 is a small molecule activator of telomerase reverse transcriptase (TERT). TERT activator-1 promotes TERT transcription through the MEK/ERK/AP-1 signaling cascade. TERT activator-1 promotes adult neurogenesis and enhances neuromuscular function. TERT activator-1 reduces cellular senescence and systemic inflammation in aged mice, and can be used in the study of aging .
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-
- HY-N1428R
-
|
|
Apoptosis
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Citric acid standard is the standard form of citric acid (HY-N1428). Citric acid standard is a natural preservative and food tartness enhancer. Citric acid standard induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid standard cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid standard causes renal toxicity in mice .
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- HY-158316
-
|
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Others
|
Others
|
|
BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumins (HY-W250978)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
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-
- HY-12678R
-
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ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
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- HY-15344
-
|
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Others
|
Neurological Disease
Metabolic Disease
|
|
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
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-
- HY-B1268
-
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Dioctyl sulfosuccinate sodium salt
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HSV
|
Others
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Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
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- HY-16785
-
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INXN-1001; RG-115932
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
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Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .
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-
- HY-15698A
-
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PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
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-
- HY-121495
-
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Parasite
|
Infection
|
|
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
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-
- HY-N0594
-
|
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Interleukin Related
|
Inflammation/Immunology
|
|
Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice . Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells .
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-
- HY-P1302A
-
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Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice .
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-
- HY-P2264
-
|
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Ephrin Receptor
|
Inflammation/Immunology
|
|
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
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-
- HY-N9481
-
-
- HY-108022A
-
|
MSDC-0602K
|
Insulin Receptor
PPAR
|
Metabolic Disease
|
|
Azemiglitazone potassium (MSDC-0602K), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC50 of 18.25 μM . Azemiglitazone potassium modulates the mitochondrial pyruvate carrier (MPC). Azemiglitazone potassium can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance . Azemiglitazone potassium, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide .
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-
- HY-144635
-
-
- HY-146401
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice .
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-
- HY-146151
-
|
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γ-secretase
Amyloid-β
|
Neurological Disease
|
|
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice .
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-
- HY-147720A
-
|
|
γ-secretase
|
Neurological Disease
|
|
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease .
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-
- HY-107916
-
|
TSH; Pretiron
|
Others
|
Metabolic Disease
Endocrinology
Cancer
|
|
Thyrotropin is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism .
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-
- HY-133180
-
|
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Wnt
β-catenin
|
Metabolic Disease
|
|
YW1128 (compound 3a) is a potent Wnt/β-Catenin inhibitor. YW1128 induces the proteasome degradation of β-catenin and subsequent inhibits the Wnt/β-catenin signaling in cells. YW1128 significantly decreases hepatic lipid accumulation. YW1128 improves glucose tolerance of high fat diet-fed mice without noticeable toxicity. YW1128 down regulates the genes involved in the glucose and fatty acid anabolism .
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-
- HY-119209
-
|
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5-HT Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
|
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction .
|
-
- HY-P99583
-
|
MEDI4893
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
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-
- HY-152142
-
|
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
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-
- HY-123983
-
|
|
Pim
DAPK
|
Cardiovascular Disease
|
|
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension .
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-
- HY-13991A
-
|
|
Ras
|
Metabolic Disease
Cancer
|
|
(S)-CCG-1423 is an inhibitor of Rho signaling that blocks the nuclear import of MRTF-A. (S)-CCG-1423 reduces the nuclear accumulation of MRTF-A and improves glucose uptake and tolerance in insulin-resistance mice in vivo. (S)-CCG-1423 exhibits higher inhibition activity than the SR- and the R-isomers of CCG-1423 (HY-13991). (S)-CCG-1423 can be used for the research of cancer and diabetes .
|
-
- HY-N11728
-
|
|
Amylases
Glucosidase
|
Metabolic Disease
|
|
2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC50 values of 6.94 μM and 23.35 μM respectively. 2,7"-Phloroglucinol-6, 6'-bieckol alleviates postprandial hyperglycemia in diabetic mice. 2,7"-Phloroglucinol-6,6'-bieckol can be used in diabetes research .
|
-
- HY-157172
-
|
|
Integrin
|
Infection
Neurological Disease
|
|
MorHap is a heroin hapten. MorHap conjugated to tetanus toxoid (TT), palm-CV2, and to monophosphoryl lipid A (MPLA)-containing liposomes partially blocks heroin-induced analgesia and hyperlocomotion in mice. MorHap designed conjugates also significantly inhibits HIV-1 binding to α4β7 receptors. MorHap can be used in research to develop vaccines related to heroin addiction and HIV-1 infection .
|
-
- HY-15698
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-106194
-
|
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
SLV310 is an orally active dopamine D2 receptor antagonist (Ki: 5 nM) and serotonin reuptake receptor inhibitor. SLV310 antagonizes Apomorphine (HY-12723) induced climbing behaviour and 5-HTP (HY-N0122) induced serotonin syndrome like behaviour in mice (ED50: 5.6 and 5.9 mg/kg, p.o.). SLV310 is an antipsychotic compound and can be used for schizophrenia research .
|
-
- HY-121328
-
|
S-2852F
|
Parasite
|
Infection
Neurological Disease
|
|
Empenthrin (S-2852F) is a synthetic pyrethroid. Empenthrin can be used in insecticides. Empenthrin shows a clear species-specificity in the inhibitory effect on the Pentobarbital (PTB)-metabolizing enzyme(s). Empenthrin prolongs PTB induced-sleeping time in mice through an inhibition of the PTB-metabolizing enzyme(s) in the liver, an effect that does not occur in rats. Empenthrin shows a clear species-specificity in the inhibitory effect on the PTB-metabolizing enzyme(s) .
|
-
- HY-111782
-
|
8-Thioguanosine
|
Others
|
Inflammation/Immunology
|
|
8-Mercaptoguanosine is an immunoadjuvant that affects the in vivo antibody response to the T-cell-independent antigen TNP-Ficoll. 8-Mercaptoguanosine enhances IgG1, IgG2, and IgG3 antibody responses, but has no effect on IgM antibody responses. 8-Mercaptoguanosine also enhances antibody responses to very weak antigens such as pneumococcal polysaccharide and restores antibody responses in immunodeficient xid mice that are non-reactive to TNP-Ficoll .
|
-
- HY-163817
-
|
|
PARP
|
Cancer
|
|
PARP1/2-IN-3 (Compound 29) is an orally active inhibitor for PARP 1 and PARP 2 with IC50 of 0.2235 nM and <0.001 nM. PARP1/2-IN-3 inhibits the proliferation of Capan-1 wildtype, AZD2281 or BMN673 resistant cells with IC50 of 1.82-9.98 nM. PARP1/2-IN-3 exhibits antitumor efficacy in mice .
|
-
- HY-162702
-
|
|
Androgen Receptor
PROTACs
|
Cancer
|
|
AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
|
-
- HY-N0088R
-
|
|
NADPH Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Apocynin (Standard) is the analytical standard of Apocynin. This product is intended for research and analytical applications. Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
|
-
- HY-N1369R
-
|
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Menthol (Standard) is the analytical standard of Menthol. This product is intended for research and analytical applications. Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice .
|
-
- HY-117702
-
|
|
Prolyl Endopeptidase (PREP)
Aminopeptidase
|
Metabolic Disease
|
|
RB 101 is an active mixed inhibitor against two enzymes which metabolize the enkephalins neutral endopeptidase and aminopeptidase N. RB 101 has rather long-lasting antinociceptive effects. RB 101 inhibits the in vivo [ 3H]DPN binding both under basal conditions and after swim stress in mice. RB 101 can be used to determine the precise in vivo localization of enkephalinergic pathways recruited by various stimuli .
|
-
- HY-19876
-
|
Debio-0827
|
Opioid Receptor
Aminopeptidase
Neprilysin
|
Neurological Disease
Metabolic Disease
|
|
PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
|
-
- HY-169007
-
|
|
STAT
|
Inflammation/Immunology
|
|
STAT3-IN-34 (Compound 15E) is an inhibitor for STAT3, and inhibits the nuclear translocation and transcriptional regulator activity of STAT3. STAT3-IN-34 inhibits the proliferation of cell HaCaT with IC50 of 0.008 μM. STAT3-IN-34 inhibits IL-17A expression and ameliorates Imiquimod (HY-B0180)-induced psoriasis in mice .
|
-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-113958R
-
|
|
Others
|
Others
|
|
Difethialone (Standard) is the analytical standard of Difethialone. This product is intended for research and analytical applications. Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
|
-
- HY-118758
-
|
γ-Kainic acid-glutamic acid
|
Sodium Channel
|
Neurological Disease
|
|
γ-Kainylglutamic acid (γ-Kainic acid-glutamic acid), a dipeptide derived from kainic and L-Glutamic acids, is a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties. γ-Kainylglutamic acid inhibits the stimulation of Na + fluxes induced in brain slices by the neuroexcitant N-methyl-D-aspartic acid. γ-Kainylglutamic acid is also effective in protecting mice from picrotoxin-induced convulsions with an EC50 value of 0.17 μmol .
|
-
- HY-Z0283R
-
|
|
Endogenous Metabolite
PARP
|
Others
|
|
Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-101780A
-
|
EDO-S101 hydrochloride; NL-101 hydrochloride
|
HDAC
|
Cancer
|
|
Tinostamustine hydrochloride (EDO-S101 hydrochloride) is a compound with anti-multiple myeloma activity and the ability to promote CD38 expression. Tinostamustine hydrochloride enhances the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab by increasing the acetylation level of histone H3. Tinostamustine hydrochloride can increase the expression of MICA and MICB, thereby activating NK cells. Tinostamustine hydrochloride can significantly delay tumor growth and improve the survival rate of mice .
|
-
- HY-168705
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 20 (Compound a4) is an anti-microbial agent (MIC: < 0.03125 μg/mL) against MRSA). Anti-MRSA agent 20 binds to the ribosomal peptidyl transferase center and inhibits bacterial survival by inhibiting MRSA toxin synthesis and bacterial division. Anti-MRSA agent 20 significantly reduces the MRSA load in the lungs and attenuates lung injury in the MRSA-infected mice (ED50 = 6.48 mg/kg) .
|
-
- HY-159942
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice .
|
-
- HY-118574
-
|
|
iGluR
|
Neurological Disease
|
|
UBP141 is a GluN2C/2D (NR2C/2D)-preferring receptor antagonist, with Kds of 2.8, 4.2, 14.2, and 19.3 μM for NMDA receptor subtypes: GluN2C, 2D, 2A, and 2B, respectively. UBP141 can induce potent motor impairment in WT mice .
|
-
- HY-B0413
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
Cancer
|
|
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-18555
-
TMPA
2 Publications Verification
|
Nuclear Hormone Receptor 4A/NR4A
AMPK
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation .
|
-
- HY-109086
-
|
JNJ-40346527; JNJ-527
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
|
|
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively . Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research .
|
-
- HY-135982
-
|
|
GPR109A
|
Metabolic Disease
|
|
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a .
|
-
- HY-B0854
-
|
|
Fungal
Keap1-Nrf2
Apoptosis
Lactate Dehydrogenase
Cytochrome P450
|
Infection
Metabolic Disease
Cancer
|
|
Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells .
|
-
- HY-N0401A
-
|
|
Bacterial
Estrogen Receptor/ERR
FATP
|
Infection
Metabolic Disease
|
|
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
|
-
- HY-N6962
-
|
|
TRP Channel
COX
Bacterial
|
Infection
Neurological Disease
Metabolic Disease
|
|
α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC50 values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice .
|
-
- HY-120601
-
|
ARS sodium
|
Others
|
Others
|
|
Alizarin Red S sodium is an anthraquinone derivative dye. When combined with cations such as calcium ions, the functional group of Alizarin Red S sodium can form a coordination bond with the cation through the oxygen atom to show orange-red fluorescence. Alizarin Red S sodium can be used for screening of calcium compounds in synovial fluid and detecting osteoblast differentiation, and can also be used for bone staining in mice. Excitation/emission wavelength: 500/570 nm .
|
-
- HY-108485
-
|
|
Src
Apoptosis
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans .
|
-
- HY-N2877
-
|
|
Potassium Channel
Sodium Channel
Na+/K+ ATPase
Calcium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
Annonacin is an acetylgenin that is toxic by inhibiting the pathway of the mitochondrial complex. Annonacin increases tau phosphorylation in R406W +/+ mice. Annonacin acts as an inhibitor of the sodium/potassium and sarcoplasmic reticulum (SERCA) ATPase pumps. Annonacin has significant killing effect on ovarian cancer cell, cervical cancer cell, breast cancer cell, bladder cancer cell and skin cancer cell. Annonacin induces apoptosis through Bax and Caspase-3-related pathways .
|
-
- HY-108538
-
|
|
Glutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-B0648
-
|
17α-Hydroxy-6α-methylprogesterone; U8840
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Medroxyprogesterone (17α-Hydroxy-6α-methylprogesterone) is a synthetic human variant of progesterone that is a progesterone receptor agonist with oral activity. Medroxyprogesterone can induce cell proliferation through the PI3K/Akt signaling pathway. Medroxyprogesterone has an inhibitory effect on atherosclerosis in mice. The progesterone agonist activity of Medroxyprogesterone is less effective than Medroxyprogesterone acetate (HY-B0469) .
|
-
- HY-103177
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice .
|
-
- HY-N6263
-
|
AcEGCG; Peracetylated (-)-epigallocatechin-3-gallate
|
Bacterial
|
Infection
Cardiovascular Disease
Cancer
|
|
EGCG Octaacetate (AcEGCG) is a proagent of Green tea epigallocatechin-3-gallate (EGCG). EGCG Octaacetate decreases the proinflammatory mediator levels by down-regulating of PI3K/Akt/NFκB phosphorylation and p65 acetylation. EGCG Octaacetate reduces colitis-driven colon cancer in mice. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB) .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-103511
-
|
|
GABA Receptor
|
Neurological Disease
|
|
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .
|
-
- HY-W115718
-
|
|
Dopamine β-hydroxylase
|
Neurological Disease
|
|
Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) .
|
-
- HY-101170
-
|
|
Imidazoline Receptor
Apoptosis
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .
|
-
- HY-P99156
-
|
BMS-986016
|
LAG-3
|
Cancer
|
|
Relatlimab (BMS-986016) is a human monoclonal antibody anti-LAG-3 antibody generated by immunization of transgenic mice bearing human immunoglobulin miniloci with recombinant LAG-3 protein. Relatlimab blocks LAG-3/MHC II interaction with an IC50 value of 0.67 nM and LAG-3/FGL1 interaction with an IC50 value of 0.019 nM. Relatlimab can be used in research of cancer .
|
-
- HY-123942
-
|
|
Toll-like Receptor (TLR)
TNF Receptor
p38 MAPK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses .
|
-
- HY-P99341
-
|
REGN10933
|
SARS-CoV
|
Infection
|
|
Casirivimab (REGN10933) is a human monoclonal antibody that targets the SARS-CoV-2 virus, which causes COVID-19. Casirivimab is ineffective against COVID-19 variants. Casirivimab can be used in combination with Imdevimab (HY-P99342), which alters the lung response of K18-hACE2 mice to the SARS-CoV-2 δ variant, effectively reducing viral load and improving symptoms .
|
-
- HY-124727
-
|
|
JAK
Apoptosis
|
Cancer
|
|
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
|
-
- HY-W013411
-
|
(E/Z)-UIC-1005
|
Others
|
Cancer
|
|
(E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of Locostatin. Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
|
-
- HY-W013411A
-
|
UIC-1005
|
Others
|
Cancer
|
|
Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
|
-
- HY-149917
-
|
|
PROTACs
Itk
|
Cancer
|
|
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels .
|
-
- HY-P4641
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-149838
-
|
|
NF-κB
|
Cancer
|
|
NF-κB-IN-9 is a nuclear factor kappa B (NF-κB) targeting sonosensitizer (λex/λem=489/628 nm). NF-κB-IN-9 exhibits strong inhibition on NF-κB signaling due to its two resveratrol units in one molecule. NF-κB-IN-9 has anti-tumor activity and shows remarkable sonocytotoxicity against cancer cells. NF-κB-IN-9 has biosafety in eenograft mice model.
|
-
- HY-149975
-
|
|
iGluR
|
Neurological Disease
|
|
AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice .
|
-
- HY-155525
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-NASH agent 1 (compound 3d)，a derivative of Elafibranor (HY-16737)，is a potent agonist of PPAR-α/δ，targeting to nonalcoholic steatohepatitis (NASH). Anti-NASH agent 1 (3-10 mg/kg; 4 weeks) improves hyperlipidemia，liver fat degeneration and liver inflammation in Methionine-choline deficiency (MCD) induced NASH mice model. Anti-NASH agent 1 shows low liver toxicity and potent liver protection effect .
|
-
- HY-106837
-
|
Y 24180
|
Platelet-activating Factor Receptor (PAFR)
|
Inflammation/Immunology
|
|
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca 2+ influx and intracellular Ca 2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice .
|
-
- HY-149555
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
|
-
- HY-155229
-
-
- HY-P5875
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-N2199
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .
|
-
- HY-149696
-
|
|
NF-κB
|
Cancer
|
|
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
|
-
- HY-162329
-
|
|
Bacterial
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Antibacterial agent 195 (compound A20), a Matrine (HY-N0164) derivative, is a potent antibiotic. Antibacterial agent 195 shows antibacterial activity against Gram-positive bacterium (MICS.aureus=0.021 mg/mL; MICP.acnes=0.030 mg/mL), Gram-negative bacterium (MICE.coli=0.092 mg/mL; MICC.albicans=0.379 mg/mL) and Fungus (MIC=2.806 mg/mL) .
|
-
- HY-W010520R
-
|
|
Bacterial
MMP
|
Infection
Inflammation/Immunology
|
|
Methylisothiazolinone (Standard) is the analytical standard of Methylisothiazolinone. Methylothiazolinone is a fungicide and preservative, as well as a sensitizer. Methylisothiazolinone can activate matrix metalloproteinases (MMPs) in human bronchial epithelial cells to induce cell apoptosis and inflammatory response. Methylisothiazolinone can promote the development of atopic dermatitis in mice by disrupting Th2/Th17 related immune responses. Methylisothiazolinone can cause mitochondrial damage in the endothelium of rat cerebral blood vessels .
|
-
- HY-118282
-
|
|
PGE synthase
|
Endocrinology
|
|
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice .
|
-
- HY-N9484S
-
|
|
Drug Metabolite
Isotope-Labeled Compounds
|
Others
|
|
Menthofuran- 13C2 is 13C labeled Menthol (HY-N1369). Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca ++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice .
|
-
- HY-A0114
-
|
RS 10029
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Moexiprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=2.1 nM) and an active metabolite of the prodrug Moexipril (HY-117281). It is formed from moexipril in vivo by side chain ester hydrolysis. Moexiprilat (10 nM) prevents the estrone- or angiotensin II-stimulated proliferation of primary neonatal rat cardiac fibroblasts. It reduces mean arterial blood pressure and increases the levels of atrial natriuretic peptide, a marker of hypertension, in ovariectomized mice when administered at a dose of 50 mg/kg per day.
|
-
- HY-N10653
-
|
(-)-Altemicidin
|
Others
|
Cancer
|
|
Altemicidin is a monoterpene alkaloid originally isolated from S. sioyaensis with acaricidal and anticancer activities. It is acaricidal to two-spotted spider mites (T. urticae) in a greenhouse pot test at concentrations of 10 and 100 ppm. Altemicidin inhibits the growth of murine L1210 lymphocytic leukemia and IMC carcinoma cells (IC50s=0.84 and 0.82 μg/mL, respectively). It is toxic to mice with an LD50 value of 0.3 mg/kg.
|
-
- HY-163683
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .
|
-
- HY-164036
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Lolamicin is a Gram-negative specific antibiotic. Lolamicin is active against more than 130 multidrug-resistant clinical isolates, has shown efficacy in multiple mouse models of acute pneumonia and sepsis infection, and protects the gut microbiome of mice against secondary infection with Clostridium difficile. The selective killing of pathogenic gram-negative bacteria by Lolamicin is a result of the low sequence homology of pathogenic bacteria and symbiotic bacteria. Lolamicin can be used in the study of infection caused by Gram-negative pathogens .
|
-
- HY-126170
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Valanimycin is an antibiotic, which inhibits Escherichia coli (BE1121) through interaction with DNA. Valanimycin exhibits cytotoxicity to mouse leukemia L1210, P388/S (doxorubicin (HY-15142A)-sensitive), and P388/ADR (doxorubicin-resistant), with IC50 of 0.79, 2.65, and 1.44 μg/mL, respectively. Valanimycin exhibits antitumor efficacy against ehrlich ascites tumors or L1210 in mice .
|
-
- HY-P9983
-
|
HuM-195
|
Others
Radionuclide-Drug Conjugates (RDCs)
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR? and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
|
-
- HY-162710
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC50 of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models .
|
-
- HY-162703
-
|
|
AMPK
|
Metabolic Disease
|
|
Lipid-lowering agent-2 (Compound 14d) is an orally active lipid-lowering agent with an EC50 of 0.06 μM. Lipid-lowering agent-2 inhibits the lipid synthesis, activates the AMPK signaling pathway, and exhibits anti-obesity effect. Lipid-lowering agent-2 inhibits food intake, improves the glucose metabolism, and reduces the body weight and adipose tissue in high-fat diet (HFD)-induced obese mice .
|
-
- HY-120667
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice .
|
-
- HY-123936
-
|
|
NF-κB
IKK
|
Neurological Disease
Inflammation/Immunology
|
|
SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases .
|
-
- HY-15698B
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-N12124
-
|
Monascinol
|
Akt
mTOR
AMPK
Androgen Receptor
Apoptosis
Autophagy
|
Cancer
|
|
Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
|
-
- HY-126477R
-
|
|
Endogenous Metabolite
|
Cancer
|
|
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
|
-
- HY-N2342R
-
|
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 (Standard) is the analytical standard of Procyanidin C1. This product is intended for research and analytical applications. Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
|
-
- HY-N6967R
-
|
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-14162
-
|
|
FLAP
|
Inflammation/Immunology
|
AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB4 and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma .
|
-
- HY-162863
-
|
|
Apoptosis
|
Cancer
|
ERK-MYD88 interaction inhibitor 1 is an ERK-MYD88 interaction inhibitor. ERK-MYD88 interaction inhibitor 1 can induce an HRI-mediated integrated stress response (ISR), leading to cancer cell-specific immunogenic cell apoptosis (apoptosis). ERK-MYD88 interaction inhibitor 1 can induce anti-tumor T cell responses in Lewis lung cancer mice, exhibiting anti-tumor activity .
|
-
- HY-N8818
-
|
|
Others
|
Inflammation/Immunology
|
|
3-Acetoxytirucalla-7,24-dien-21-oic acid, derived from Boswellia carteri, exhibits anti-inflammatory activity. Its ID50 for Phorbol 12-myristate 13-acetate (HY-18739)-induced ear swelling in mice is 0.06 mg per ear. 3-Acetoxytirucalla-7,24-dien-21-oic acid holds potential for research in the field of inflammation .
|
-
- HY-108035
-
|
MR04A3
|
GABA Receptor
|
Neurological Disease
|
|
(-)-JM-1232 (MR04A3) targets GABA A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI50 values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia .
|
-
- HY-169054
-
|
|
TSH Receptor
|
Cancer
|
|
NCATS-SM4420 (Compound A35) is an orally active thyroid-stimulating hormone receptor (TSHR) ligand that inhibits the proliferation of MDA-T32 and MDA-T85 cells in vitro (IC50 values of 0.71 μM and 0.38 μM, respectively) and suppresses metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds promise for research in the field of thyroid cancer .
|
-
- HY-169120
-
|
|
Others
|
Cancer
|
|
FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
|
-
- HY-118665
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
L-736380 is a high affinity CCK-B (cholecystokinin B receptor) receptor antagonist, with IC50 values of 0.054 nM and 400 nM for CCK-B and CCK-A, respectively. L-736380 dose-dependently inhibits gastric acid secretion in anesthetized rats (ID50, 0.064 mg/kg) and ex vivo binding of [125I]CCK-8S in BKTO mice brain membranes (ED50, 1.7 mg/kg) .
|
-
- HY-109086A
-
|
JNJ-40346527 hydrochloride; JNJ-527 hydrochloride
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Edicotinib hydrochloride is a potent, selective, brain penetrant and orally active?colony-stimulating factor-1 receptor (CSF-1R)?inhibitor with an IC50 of 3.2 nM. Edicotinib hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively . Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research .
|
-
- HY-167706
-
|
|
Others
|
Inflammation/Immunology
|
|
Diethyl-Lodoxamide is a highly potent GPR35 agonist with potential to inhibit inflammatory bowel disease. Diethyl-Lodoxamide activates GPR35 in humans, mice and rats, showing similar EC50 values. Diethyl-Lodoxamide can alleviate the clinical symptoms of DSS-induced inflammatory bowel disease in mouse models, and the effect is better than the traditional drug 5-ASA. The pharmaceutical properties of Diethyl-Lodoxamide have been optimized to better meet the requirements of drug design .
|
-
- HY-18956A
-
|
(E/Z)-Sephin1 hydrochloride; (E/Z)-IFB-088 hydrochloride
|
Phosphatase
|
Neurological Disease
|
|
(E/Z)-Icerguastat hydrochloride ((E/Z)-Sephin1 hydrochloride) is a selective inhibitor with activity that prolongs the phosphorylation effects of eIF2α. (E/Z)-Icerguastat hydrochloride protects cells from defects in proteostasis. (E/Z)-Icerguastat hydrochloride was shown to significantly extend the survival of infected prion mice in a mouse model. (E/Z)-Icerguastat hydrochloride effectively reduces PrPSc expression and prion sequence activity in various neuronal cell lines persistently infected with different prion strains .
|
-
- HY-159903
-
|
|
Influenza Virus
|
Infection
|
|
TQL-1055 is a semi-synthetic analog of the saponin adjuvant QS-21 (HY-101092) and can be used as a prophylactic vaccine adjuvant. TQL-1055 exhibits robust adjuvant activity for influenza antigens. TQL-1055 combined with the acellular pertussis vaccine (aP) shows good tolerance and enhances the antibody response to pertussis toxin (PT) in mice and rabbits. TQL-1055 is promising for research of chronic hepatitis B .
|
-
- HY-A0081
-
|
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
|
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-B1005
-
|
8-Quinolinol
|
Bacterial
Antibiotic
|
Cancer
|
|
8-Hydroxyquinoline (8-Quinolinol) is a lipophilic metal chelator that can be used as a fungicide .8-Hydroxyquinoline shows the MIC range of 27.56-55.11 μM (4-8 μg/mL) against the clinical isolates of Neisseria gonorrhoeae. 8-Hydroxyquinoline can bind to copper form complexes and transport copper into cells. 8-Hydroxyquinoline increases in the number of micronucleated polychromatic erythrocytes and can also make hair depigmented in mice .
|
-
- HY-B1350A
-
|
Sodium fusidate; SQ-16360
|
Bacterial
Antibiotic
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Fusidic acid sodium salt is an orally available antibacterial agent that inhibits bacterial protein synthesis by preventing the release of translation elongation factor G (EF-G) from ribosomes. Fusidic acid sodium salt inhibits the inhibitory and activating effects of interleukins IL-1 and IL-6 on glucose-induced insulin production and exhibits antidiabetic effects in a rat model. Fusidic acid sodium salt improves the symptoms of colitis in rats and inhibits the growth of Toxoplasma gondii and Listeria monocytogenes EGD in vitro, but not in mice .
|
-
- HY-B1245
-
|
Salicylsalicylic acid; Disalicylic acid
|
Reactive Oxygen Species
|
Inflammation/Immunology
Cancer
|
|
Salsalate is a potent antirheumatic drug with oral activity that reduces irritation during gastric absorption and avoids direct inhibition of cyclooxygenase. Salsalate not only has significant anti-inflammatory effects, but also reduces blood sugar levels, improves insulin resistance, and reduces the expression of cytokines. Salsalate can protect mice from metabolic disorders caused by high-fat diet and effectively improve the symptoms of type 2 diabetes, atherosclerosis and non-alcoholic steatohepatitis [2 ] .
|
-
- HY-101117
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
|
-
- HY-101903
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-W012974
-
|
β-Aminoisobutyric acid; BAIBA
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
3-Aminoisobutyric acid (β-Aminoisobutyric acid) has anti-inflammatory and antioxidant effects. 3-Aminoisobutyric acid increases the expression of brown adipocyte-specific genes in white adipose tissue and fatty acid β-oxidation in hepatocytes. 3-Aminoisobutyric acid attenuates insulin resistance and inflammation induced by palmitate or a high fat diet via an AMPK–PPARδ-dependent pathway in mice. 3-Aminoisobutyric acid is a catabolic metabolite of thymine and valine in skeletal muscle .
|
-
- HY-101029
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-59291
-
|
|
Endogenous Metabolite
Amino Acid Derivatives
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Levacetylleucine, an orally bioavailable and brain-penetrant endogenous metabolite, is an acetylated derivative of amino acid leucine. Levacetylleucine is the active form of N-acetyl-leucine (NAL). Levacetylleucine attenuates neuronal death and neuroinflammation in the cortical tissue of mice. Levacetylleucine also potentially improves ameliorates lysosomal and metabolic dysfunction. Levacetylleucine improves compensation of postural symptoms after unilateral chemical labyrinthectomy (UL) in rats. Levacetylleucine is promising for research of neurological manifestations of Niemann-Pick disease type C, traumatic brain injury and neurodegeneration prevention .
|
-
- HY-117482
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-100591
-
|
|
Sirtuin
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
|
-
- HY-N1420
-
|
L-Rhamnose
|
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
Cancer
|
|
Rhamnose (L-Rhamnose) is an orally active deoxysugar that is widely found in plants and bacteria. Rhamnose can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models, showing anti-aging effects. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose is also used in cancer research .
|
-
- HY-10081
-
GS-6201
1 Publications Verification
CVT-6883
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) . GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
|
-
- HY-125130
-
|
Hes-7-G
|
HMG-CoA Reductase (HMGCR)
Bacterial
Interleukin Related
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Hesperetin 7-O-glucoside is a typical flavonoid monoglucoside, which is an anti-inflammatory agent and an antihypertensive with orally active. Hesperetin 7-O-glucoside is a commonly used food adjuvant. Hesperetin 7-O-glucoside inhibits human intestinal maltase and human HMG-CoA reductase with Ki of 1.8 mM and 9.8 μM, respectively. Hesperetin 7-O-glucoside has antibacterial activity and can regulate intestinal flora and metabolic homeostasis in mice .
|
-
- HY-W014421
-
|
|
TRP Channel
|
Neurological Disease
|
|
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM .
|
-
- HY-16361A
-
|
CGP3466B; CGP3446 maleate; TCH346 maleate
|
Apoptosis
|
Neurological Disease
Metabolic Disease
|
|
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease . Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD) . Omigapil (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-117482A
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-101903A
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-17623
-
|
CJ-12420; RQ-00000004
|
Proton Pump
Potassium Channel
Na+/K+ ATPase
|
Inflammation/Immunology
|
Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H +/K +-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H +/K +-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-N0930B
-
|
|
AMPK
Bacterial
|
Infection
Metabolic Disease
|
|
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
|
-
- HY-101144
-
|
TCD-717
|
Others
|
Cancer
|
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
|
-
- HY-145628
-
|
|
Sigma Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
|
-
- HY-119980
-
|
|
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
|
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-146619
-
|
|
Amyloid-β
Serotonin Transporter
|
Neurological Disease
|
|
RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression .
|
-
- HY-120782
-
|
|
Notch
|
Neurological Disease
|
|
Yhhu-3792 enhances the self-renewal capability of neural stem cells (NSCs). Yhhu-3792 activates Notch signaling pathway and promotes the expression of Hes3 and Hes5. Yhhu-3792 expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) in mouse. Yhhu-3792 increases the spatial and episodic memory abilities of mice. Yhhu-3792 has the potential for the research of impairment of learning and memory associated DG dysfunction .
|
-
- HY-146452
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
|
-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
|
-
- HY-150562
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-150596
-
|
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-151155
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
|
-
- HY-P99163
-
|
ABBV-8E12; C2N-8E12
|
Tau Protein
|
Neurological Disease
|
|
Tilavonemab (ABBV-8E12) is a humanized anti-tau antibody that targets the extracellular form of pathological tau protein aggregates by binding to the N-terminal 25-30 amino acid residues of tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates, reduces the loss of brain volume, slows the progression of tau pathology, and improves cognitive abilities in transgenic mice expressing mutant human tau. Tilavonemab is used in Alzheimer's disease research .
|
-
- HY-129983
-
|
|
HSV
|
Infection
Cancer
|
|
5-Hydroxymethyl-2'-deoxyuridine is a nucleoside analog. 5-Hydroxymethyl-2'-deoxyuridine inhibits the replication of multiple human leukemia cell lines with IC50 values of 1.7-5.8 μM. 5-Hydroxymethyl-2'-deoxyuridine prolongs the survival of mice carrying L1210 leukemia. 5-Hydroxymethyl-2'-deoxyuridine can be used for the research of cell replication and leukemia .
|
-
- HY-152148
-
|
|
MAGL
|
Neurological Disease
|
|
JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP) .
|
-
- HY-110126
-
|
|
P2Y Receptor
|
Inflammation/Immunology
Cancer
|
|
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth .
|
-
- HY-128129
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-153369
-
|
|
Guanylate Cyclase
|
Cardiovascular Disease
Neurological Disease
|
|
BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model .
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-
- HY-P5762A
-
|
PNX-14 TFA
|
GnRH Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Phoenixin-14 (PNX-14) TFA, a BBB-penatrable neuropeptide, has anxiolytic, cardioprotective and neuroprotective effect. Phoenixin-14 TFA can regulate pituitary gonadotrophin secretion by upregulating the GnRH receptor mRNA. Phoenixin-14 TFA stimulates insulin secretion. Phoenixin-14 TFA also protects mice from ischemia/reperfusion (IR) injury. PNX-14 TFA prevents oxidative stress by reducing ROS and increasing GSH .
|
-
- HY-15791
-
|
FK-3657
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease .
|
-
- HY-155328
-
|
|
HDAC
|
Inflammation/Immunology
|
|
GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice .
|
-
- HY-116143
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
|
-
- HY-117836
-
|
|
FAK
|
Cancer
|
|
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
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-
- HY-119980B
-
|
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
|
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-120782A
-
|
|
Notch
|
Neurological Disease
|
|
Yhhu-3792 hydrochloride enhances the self-renewal capability of neural stem cells (NSCs). Yhhu-3792 hydrochloride activates Notch signaling pathway and promotes the expression of Hes3 and Hes5. Yhhu-3792 hydrochloride expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) in mouse. Yhhu-3792 hydrochloride increases the spatial and episodic memory abilities of mice. Yhhu-3792 hydrochloride has the potential for the research of impairment of learning and memory associated DG dysfunction .
|
-
- HY-B1640R
-
|
Etacrynic acid (Standard)
|
Glutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
Cancer
|
|
Ethacrynic acid (Standard) is the analytical standard of Ethacrynic acid. This product is intended for research and analytical applications. Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-161305
-
|
|
HDAC
|
Metabolic Disease
Cancer
|
|
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice .
|
-
- HY-161372
-
|
|
PARP
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
|
-
- HY-163476
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
PIP5K1C-IN-1 (Compound 30) is a potent PIP5K1C inhibitor, with an IC50 of 0.80 nM. PIP5K1C-IN-1 exhibits low total clearance in mice and high levels of kinase selectivity. PIP5K1C-IN-1 can be used for the research of cancer and chronic pain .
|
-
- HY-158204
-
|
|
Lipoxygenase
|
Neurological Disease
|
|
CNB-001 is a potent 5-lipoxygenase (5-LOX) inhibitor, decreases 5-LOX expression, and increases proteasome activity. CNB-001 also increases eIF2α phosphorylation and HSP90 and ATF4 levels in Alzheimer's disease transgenic mice, and limits the accumulation of soluble Aβ and ubiquitinated aggregated proteins. CNB-001 maintains the expression of synapse-associated proteins and improves memory. CNB-001 can be used for the research of Alzheimer's disease .
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-
- HY-106761
-
|
|
Calcium Channel
|
Cardiovascular Disease
Others
|
|
Oxodipine, a dihydropyridine-type calcium antagonist, inhibits KCl-induced aortic contraction in rabbits and reduces cardiac force in less potent rat ventricular test-paper contractions. In rat cultured neonatal ventricular myocytes, Oxodipine reduces L-type Ca currents (I) with an IC50 of 0.24 μM, and against T-type Ca currents (I) with an IC50 of 0.41 μM. Oxodipine causes constipation in mice and gingival hyperplasia in dogs .
|
-
- HY-162596
-
|
BA-1049
|
ROCK
|
Neurological Disease
|
|
NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice .
|
-
- HY-162640
-
|
|
ROR
|
Cancer
|
|
ROR1-IN-1 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. ROR1-IN-1 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. ROR1-IN-1 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-162645
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
|
-
- HY-165098
-
|
β-Aminoisobutyric acid sodium salt; BAIBA sodium salt
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
3-Aminoisobutyric acid (β-Aminoisobutyric acid) sodium salt has anti-inflammatory and antioxidant effects. 3-Aminoisobutyric acid sodium salt increases the expression of brown adipocyte-specific genes in white adipose tissue and fatty acid β-oxidation in hepatocytes. 3-Aminoisobutyric acid sodium salt attenuates insulin resistance and inflammation induced by palmitate or a high fat diet via an AMPK–PPARδ-dependent pathway in mice. 3-Aminoisobutyric acid sodium salt is a catabolic metabolite of thymine and valine in skeletal muscle .
|
-
- HY-121670
-
|
|
Others
|
Neurological Disease
|
|
Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-159120
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
|
|
ZG-2291 is a selective inhibitor targeting FIH (Factor Inhibiting HIF) with oral activity. By binding to FIH, ZG-2291 promotes a conformational flip of a catalytically important tyrosine, enabling selective inhibition of FIH without affecting other 2OG oxygenases in the JmjC subfamily. ZG-2291k enhances thermogenesis in ob/ob mice and improves obesity-related symptoms and metabolic dysfunctions. ZG-2291 holds promise for research in the field of obesity-related diseases .
|
-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-161860
-
|
|
Bacterial
|
Cancer
|
|
Antibacterial agent 233 (Compound 7c) exhibits inhibitory efficacy against Helicobacter pylori with MIC of 0.4-1.6 μg/mL. Antibacterial agent 233 inhibits jack bean urease (IC50 is 0.27 μg/mL), changes the permeability of H. pylori cell membrane, causes the leakage of cellular contents. Antibacterial agent 233 exhibits metabolic stability in whole blood and artificial gastric fluid. Antibacterial agent 233 exhibits antitumor efficacy against U2OS in mice .
|
-
- HY-162751
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
|
-
- HY-18100AR
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 (hydrochloride) (Standard) is the analytical standard of PRE-084 (hydrochloride). This product is intended for research and analytical applications. PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-B0854R
-
|
|
Fungal
Keap1-Nrf2
Apoptosis
Lactate Dehydrogenase
Cytochrome P450
|
Infection
Metabolic Disease
Cancer
|
|
Mancozeb (Standard) is the analytical standard of Mancozeb. This product is intended for research and analytical applications. Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.
|
-
- HY-163983
-
|
|
Microtubule/Tubulin
Apoptosis
PARP
Caspase
|
Cancer
|
|
Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration .
|
-
- HY-164551
-
|
|
VEGFR
STAT
ERK
Apoptosis
|
Cancer
|
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .
|
-
- HY-N13174
-
|
|
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
|
Peanut procyanidin A is a type of A-type procyanidin that can be extracted from peanut skins. Peanut procyanidin A can protect prostate DU145 cells from H2O2-induced oxidative stress damage through the MAPKs signaling pathway, alleviate cell cycle arrest, and reduce cell apoptosis. Peanut procyanidin A can also regulate gut microbiota and metabolism in mice with DSS (HY-116282)-induced ulcerative colitis .
|
-
- HY-161940
-
|
|
PCSK9
|
Cardiovascular Disease
|
|
PCSK9-IN-30 (Compound 3f) is a PCSK9 inhibitor. PCSK9-IN-30 interacts with a cryptic binding groove of PCSK9, inhibiting the binding of PCSK9 to the low-density lipoprotein receptor (LDLR) (IC50 = 537 nM), restoring the uptake of low-density lipoprotein (LDL) by liver cells, and ultimately reducing plasma cholesterol levels. PCSK9-IN-30 exhibits good bioavailability in mice and can be used for research in the field of cardiovascular diseases .
|
-
- HY-103124
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
DOI hydrochloride is a serotonin 5-HT2A/2C receptor agonist with Ki values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A, h5-HT2C and h5-HT2B receptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice .
|
-
- HY-113421
-
|
Linoleic acid monoethanolamide
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
|
-
- HY-131605
-
|
GCV-TP
|
Endogenous Metabolite
|
Cancer
|
|
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM and has good antiviral effects against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
|
-
- HY-17032
-
|
(rac)-AS1069562 free base; YM-08054 free base
|
Others
|
Neurological Disease
|
|
Indeloxazine ((rac)-AS1069562 free base) is a brain active compound with anti-amnesic activity. Indeloxazine significantly prolonged the step latency in senescence accelerated mice (SAM-P/8/Ta), indicating that it has a promoting effect on brain function. Indeloxazine has a broader pharmacology than piracetam and exhibits stronger anti-amnesic activity. Indeloxazine has also been used as an anticonvulsant compound, further supporting its potential use in neuroprotection and behavioral improvement .
|
-
- HY-121670A
-
|
|
Others
|
Neurological Disease
|
|
Ambenoxan hydrochloride is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-P10586A
-
|
MALP-2 TFA
|
Toll-like Receptor (TLR)
NO Synthase
|
Cardiovascular Disease
Metabolic Disease
|
|
Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL) .
|
-
- HY-N0307R
-
|
|
Bcl-2 Family
|
Neurological Disease
|
|
Ciwujianoside B (Standard) is the analytical standard of Ciwujianoside B. This product is intended for research and analytical applications. Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory .
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation .
|
-
- HY-B0413R
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-14393
-
|
Frangula emodin
|
SARS-CoV
Casein Kinase
Autophagy
11β-HSD
|
Cancer
|
|
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
|
-
- HY-B1400
-
|
Iodoquinol; 5,7-Diiodo-8-hydroxyquinoline; 5,7-Diiodo-8-quinolinol
|
Parasite
SARS-CoV
|
Infection
Inflammation/Immunology
|
Diiodohydroxyquinoline (Iodoquinol, 5,7-Diiodo-8-hydroxyquinoline, 5,7-Diiodo-8-quinolinol) has an orally active and satisfactory antiparasitic properties. Diiodohydroxyquinoline exhibits mutagenic potential in mice and potent anti-SARS-CoV-2 activity with an EC50 value of 1.38 μM in VeroE6 cells. Diiodohydroxyquinoline's antimutagen is ascorbic acid. Diiodohydroxyquinoline is promising for research in inflammationin, testinal amebiasis, amebic liver abscess and chronic nonspecific diarrheas .
|
-
- HY-107825
-
|
|
Endogenous Metabolite
Bacterial
Cholinesterase (ChE)
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Flavonol is a cholinesterase (ChE) inhibitor, with an IC50 value of 120 μM and a Ki value of 74 μM. Flavonol has antioxidant, free radical-scavenging, antibacterial properties, and immune modulation functions. Flavonol inhibits the PriA helicase of Staphylococcus aureus. Flavonol can suppress the production of NO in LPS-activated RAW 264.7 cells by inhibiting the expression of the iNOS enzyme. Flavonol shows protective and analgesic effects in mice through various neuronal pathways. Flavonol can be used in research related to tumors and atherosclerosis diseases .
|
-
- HY-136522
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .
|
-
- HY-111754
-
|
|
MAP4K
|
Cardiovascular Disease
|
|
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice .
|
-
- HY-130609A
-
|
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease .
|
-
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
|
-
- HY-139659
-
|
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-117081
-
|
|
Others
|
Others
|
|
C30(ω-hydroxy) Ceramide (d18:1/30:0), a sphingolipid, is an epidermis-specifically vital component of the water barrier in mammalian skin. C30(ω-hydroxy) Ceramide (d18:1/30:0) is expressed in epidermal keratinocytes and male germ cells during their differentiation and maturation. C30(ω-hydroxy) Ceramide (d18:1/30:0) deficiency in the epiderm of Elovl4 deletion or mutation mice .
|
-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
|
-
- HY-143880
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
|
-
- HY-147720
-
|
|
γ-secretase
|
Neurological Disease
|
|
5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
|
-
- HY-151153
-
|
|
HDAC
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
|
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
|
-
- HY-16936
-
|
|
LRRK2
|
Neurological Disease
|
|
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
|
-
- HY-115552
-
|
|
PARP
|
Cancer
|
|
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
|
-
- HY-17623S
-
|
CJ-12420-d6; RQ-00000004-d6
|
Proton Pump
Na+/K+ ATPase
|
Metabolic Disease
|
|
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-P99620
-
|
CT-P22; CT120
|
Influenza Virus
|
Infection
|
|
Firivumab (CT-P22; CT120) is a human IgG1 monoclonal influenza A virus hemagglutinin (Anti-IAV HA) antibody. Firivumab is capable of neutralizing H1N1, H5N1, H6N1, H6N2, H8N4, H8N8, H9N2 and H12N7. Firivumab shows protection against H1N1 virus in mice .
|
-
- HY-139192
-
|
|
iGluR
TRP Channel
ERK
|
Neurological Disease
|
|
NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss .
|
-
- HY-P4190
-
|
|
GnRH Receptor
|
Endocrinology
|
|
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .
|
-
- HY-N2673
-
|
5-n-Heptadecylresorcinol; AR-C17
|
Sirtuin
|
Cardiovascular Disease
Metabolic Disease
|
|
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity .
|
-
- HY-117006
-
E1231
1 Publications Verification
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
|
Sirtuin
|
Cardiovascular Disease
|
|
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
|
-
- HY-12756A
-
|
|
Toll-like Receptor (TLR)
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Inflammation/Immunology
|
|
E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 dihydrochloride is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 dihydrochloride also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-153810
-
|
JNJ-1802
|
Virus Protease
Flavivirus
Dengue virus
|
Infection
|
|
Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates .
|
-
- HY-155997
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 56 (Compound 9) is a selective COX-2 inhibitor (IC50: 0.54 μM). Anti-inflammatory agent 56 has anti-oxidant and anti-inflammatory effects. Anti-inflammatory agent 56 inhibits oxidative stress induced cell death. Anti-inflammatory agent 56 inhibits oxidative stress and neuroinflammation by inhibiting Keap1, COX-2 and iNOS. Anti-inflammatory agent 56 has low acute toxicity in mice (LD50: 1000 mg/kg) .
|
-
- HY-P2712
-
|
Chemerin148–156, mouse
|
Chemerin Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Chemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis .
|
-
- HY-12756
-
E6446
1 Publications Verification
|
Toll-like Receptor (TLR)
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Inflammation/Immunology
|
|
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-162033
-
|
|
Others
|
Others
|
|
PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF .
|
-
- HY-12678S
-
|
NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-164102
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
|
-
- HY-161833
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
HSP90-IN-31 (compound Be01) causes reduction of CD80 and CD86 expression on dendritic cells (DCs). HSP90-IN-31 decreases the production of pro-inflammatory cytokines (IL-6, TNF-α, and IL-1β) in BMDC and peritoneal macrophages stimulated by LPS (HY-D1056). Under the delayed-type hypersensitivity (DTH) mice model, HSP90-IN-31 reduces ear swelling and pro-inflammatory cytokines in the spleen .
|
-
- HY-162681
-
|
|
Cholinesterase (ChE)
Interleukin Related
|
Neurological Disease
|
|
eeAChE-IN-3 (compound YS3g) is an orally active, potent EeAChE and IL-6 inhibitor with IC50s of 0.54 μM, 0.49 μM, 8.54 μM and 0.57 μM for EeAChE, RatAChE, RatBuChE and IL-6, respectively. eeAChE-IN-3 improves STZ (HY-13753) (Streptozotocin; HY-13753)-induced learning and memory impairment in mice. eeAChE-IN-3 has the potential for Alzheimer's disease (AD) research .
|
-
- HY-111817A
-
|
|
Parasite
|
Infection
|
|
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.
|
-
- HY-P10586
-
|
MALP-2
|
Toll-like Receptor (TLR)
NO Synthase
|
Cardiovascular Disease
|
|
Macrophage-activating lipopeptide 2 (MALP-2) is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 can enhance endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 can enhance endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL) .
|
-
- HY-148013
-
|
|
Beta-secretase
NF-κB
|
Neurological Disease
|
|
K284-6111 is an orally active inhibitor for protein chitinase 3-like 1 (CHI3L1). K284-6111 reduces the expression of inflammatory proteins such as iNOS, COX-2, GFAP, and Iba-1, inhibits β-secretase and NF-κB, and suppresses Aβ production. K284-6111 ameliorates the Aβ1–42-induced mice memory impairment, and can be used in research about Alzheimer’s Diseases .
|
-
- HY-B1268R
-
|
|
HSV
|
Others
|
|
Docusate (Sodium) (Standard) is the analytical standard of Docusate (Sodium). This product is intended for research and analytical applications. Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
|
-
- HY-N0594R
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Deacetylasperulosidic Acid (Standard) is the analytical standard of Deacetylasperulosidic Acid. This product is intended for research and analytical applications. Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice . Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells .
|
-
- HY-163987
-
|
|
Sirtuin
|
Neurological Disease
|
|
SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 improved the thermal stability of SIRT3 in SH-SY5Y cells, indicating that it can directly bind to SIRT3, has SIRT3 dependency in SH-SY5Y to clear α-Syn. SIRT3 activator 2 improves motor function in Parkinson mice, preventing Parkinson (DA) neuron loss in the substantia nigra in a dose-dependent manner .
|
-
- HY-164495
-
|
|
FAAH
Thyroid Hormone Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Sob-AM2 is a potent substrate (Km=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice .
|
-
- HY-131527
-
|
N-Desmethyl Venlafaxine hydrochloride; Wy 45494
|
Others
|
Metabolic Disease
|
|
Wy-45494 hydrochloride (N-Desmethyl Venlafaxine hydrochloride; Wy 45494) is a minor active metabolite of the selective norepinephrine and serotonin reuptake inhibitor (SNRI) venlafaxine. It is formed from venlafaxine via the cytochrome P450 (CYP) isomer CYP3A4.2. Wy-45494 hydrochloride inhibits norepinephrine and serotonin reuptake in rat synaptosomal preparations (IC50s of 4.7 and 1.6 μM, respectively). In vivo, Wy-45494 hydrochloride reversed reserpine-induced hypothermia in mice at a minimum effective dose (MED) of 10 mg/kg.
|
-
- HY-123525
-
|
|
Others
|
Neurological Disease
|
|
COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .
|
-
- HY-167692
-
|
|
Others
|
Others
|
|
JI069 is a novel JAK-STAT inhibitor that demonstrates potent activity in suppressing Th1, Th2, and Th17 differentiation while promoting iTreg differentiation. JI069 effectively inhibits STAT3 activation as well as the activation of other STATs, including STAT1, STAT5, and STAT6. JI069 has shown significant therapeutic potential in alleviating symptoms of collagen-induced arthritis in mice while inhibiting cytokine production from T cells and the phosphorylation of STAT3 in synovial cells.
|
-
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-168301
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
CL-13 is a butyrylcholinesterase (BChE) inhibitor, with an IC50 of 1.15 μM, and a selectivity index (SI) of 9.2 for acetylcholinesterase. CL-13 shows antioxidant activity in SH-SY5Y cells (DPPH EC50 = 47.01 μM) and has the ability to chelate metals involved in Aβ aggregation and/or oxidative stress, showing no neurotoxicity at 50 μM. CL-13 can reverse cognitive impairment caused by scopolamine (HY-N0296) without affecting the mice's motor skills .
|
-
- HY-N0058
-
|
Isochlorogenic acid C
|
HBV
Endogenous Metabolite
Apoptosis
Glucosidase
|
Infection
|
|
4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
|
-
- HY-19350
-
BML-210
2 Publications Verification
|
HDAC
Apoptosis
|
Cancer
|
|
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .
|
-
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-101029A
-
|
|
NEKs
Ribosomal S6 Kinase (RSK)
DYRK
Apoptosis
|
Cancer
|
|
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-117427
-
|
|
Others
|
Metabolic Disease
|
|
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice .
|
-
- HY-N6715
-
|
|
Influenza Virus
Bacterial
Enterovirus
Photosystem II
|
Infection
Cancer
|
|
Tenuazonic acid is a nonhost-selective mycotoxin belonging to the tetramic acids family. Tenuazonic acid inhibits protein biosynthesis on ribosomes by suppressing the release of new protein. Tenuazonic acid is acutely toxic, and oral LD50 is set between 81-186 mg/kg in rats and mice. Tenuazonic acid blocks electron transport beyond the primary quinone receptor (QA) by interacting with the D1 protein and is a photosystem II (PSII) inhibitor. In addition, Tenuazonic acid has antiviral effects on measles virus, enterovirus, respiratory virus and so on. Tenuazonic acid has an inhibitory effect on skin cancer .
|
-
- HY-N1940
-
|
Cycloicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
Cancer
|
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
|
-
- HY-N0028
-
|
|
Others
|
Inflammation/Immunology
|
|
Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice. Forsythiaside A inhibits the interaction between KLRB1 and CLEC2D .
|
-
- HY-120000
-
MS402
1 Publications Verification
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice .
|
-
- HY-136182
-
|
|
Na+/Ca2+ Exchanger
|
Cardiovascular Disease
Neurological Disease
|
|
YM-244769 dihydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
|
-
- HY-110133
-
JTE-607
2 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
|
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively . Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 .
|
-
- HY-121035
-
|
7-Bromoindirubin-3-Oxime
|
CDK
GSK-3
|
Neurological Disease
|
|
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice [1].
|
-
- HY-B2181
-
|
Bismuth(III) oxynitrate
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Bismuth subnitrate (Bismuth(III) oxynitrate) is a simple and efficient catalyst for the synthesis of methyl ketone by martensitic acetylene hydration reaction. When Bismuth subnitrate is intraperitoneally injected into mice, the distribution characteristics of bismuth (Bi) in the brain are similar to those of other exogenous metals such as mercury, silver and gold. Bismuth subnitrate has antibacterial activity, which can inhibit the growth of Staphylococcus aureus and Escherichia coli. Bismuth subnitrate is effective orally and can be used for the study of gastrointestinal diseases, which has protective effect on alcoholic gastric ulcer in rats .
|
-
- HY-146293
-
|
|
HDAC
HSP
|
Cancer
|
|
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
|
-
- HY-146019
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
|
-
- HY-147678
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice . GPR40 agonist 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-136182A
-
|
|
Na+/Ca2+ Exchanger
|
Cardiovascular Disease
Neurological Disease
|
|
YM-244769 is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice .
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-
- HY-147080
-
|
ARC1905
|
Complement System
|
Others
|
|
Avacincaptad pegol (ARC1905) sodium is a 40KDa PEG-conjugated aptamer. Avacincaptad pegol sodium targets complement factor 5 (C5), inhibits the cleavage of C5 into C5a and C5b, limits inflammatory stimulation and complement membrane attack complex (MAC), and is used to study age-related macular degeneration (AMD). Avacincaptad pegol sodium limits irregular cell apoptosis by targeting downstream factors in the complement cascade while preserving the early steps of the complement system. Avacincaptad pegol sodium treats Geographic atrophy (GA) mice .
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-
- HY-130437
-
|
|
MDM-2/p53
TGF-β Receptor
Caspase
|
Infection
Metabolic Disease
|
|
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease .
|
-
- HY-119980A
-
|
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
|
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-116818
-
|
|
HDAC
|
Neurological Disease
|
|
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice .
|
-
- HY-107659
-
|
|
Na+/Ca2+ Exchanger
|
Cardiovascular Disease
Neurological Disease
|
|
YM-244769 hydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
|
-
- HY-119980S
-
|
|
Isotope-Labeled Compounds
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Others
|
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-155529
-
|
|
Pim
|
Cancer
|
|
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .
|
-
- HY-153972
-
|
|
URAT1
Xanthine Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
|
URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia .
|
-
- HY-107513
-
|
|
mGluR
|
Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
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-
- HY-156124
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
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-
- HY-155226
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
|
-
- HY-160421
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206 + and CX3CR1 + immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells .
|
-
- HY-158434
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor. IRAK1-IN-1 inhibits the release of IL-6 with the IC50 values of 4.57 μM and 6.51 μM on mouse cells J774A. 1 and human cells THP-1, respectively. IRAK1-IN-1 alleviats LPS (HY-D1056)-induced acute lung injury (ALI) and DSS(HY-116282C)-induced colitis in mice .
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-
- HY-N7545
-
|
|
Antibiotic
Reverse Transcriptase
|
Infection
|
|
Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitory activity against HIV reverse transcriptase. In vitro studies have shown that Protorubradirin also inhibits Staphylococcus aureus strains and Streptococci. In infected mice, subcutaneous injection of Protorubradirin showed in vivo inhibitory efficacy against antibiotic-resistant Staphylococcus aureus strains. However, oral administration may result in a significant reduction in the activity of Protorubradirin, possibly due to faster cleavage of its C-nitroso sugar in the acidic gastric environment compared to Rubradirin .
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-
- HY-162720
-
|
|
HIV
Potassium Channel
Reverse Transcriptase
|
Infection
|
|
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
|
-
- HY-160023
-
|
|
Ras
|
Cancer
|
|
D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
|
-
- HY-120561
-
|
|
Trk Receptor
IRAK
Pim
Apoptosis
|
Cancer
|
|
PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC50 of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC50 of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice .
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-
- HY-162760
-
|
|
COMT
Monoamine Oxidase
|
Neurological Disease
|
|
COMT-IN-1 (compound C12), a nitrophenolic analogue, is an orally active dopamine metabolic enzyme catechol-O-methyltransferase (COMT) inhibitor with IC50s of 0.37 μM, 95.58 μM and 58.82 μM for COMT, MAO-A and MAO-B, respectively. COMT-IN-1 exhibits chelation with a variety of metal ions. COMT-IN-1 exhibits good BBB permeability. COMT-IN-1 improves dopamine levels and ameliorates MPTP (HY-15608)-induced Parkinson's disease (PD) symptoms in mice .
|
-
- HY-N0028R
-
|
|
Others
|
Inflammation/Immunology
|
|
Forsythiaside A (Standard) is the analytical standard of Forsythiaside A. This product is intended for research and analytical applications. Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice .
|
-
- HY-164373
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
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-
- HY-117707
-
|
|
Raf
|
Cancer
|
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
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-
- HY-123357
-
|
|
Apoptosis
|
Neurological Disease
|
|
IMM-H004, a coumarin derivative, possesses neuroprotective and potent free radical scavenging abilities. IMM-H004 significantly inhibits amyloid-β (Aβ)-induced cytotoxicity and apoptosis, offering potential value for research into neurodegenerative diseases such as Alzheimer's disease. Additionally, IMM-H004 is also capable of effectively blocking the calcium mobilization and chemotaxis induced by CKLF1-C27 (HY-P3418), thereby alleviating asthmatic pathological changes in the lung tissue of CKLF1 transgenic mice .
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-
- HY-169019
-
|
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
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-
- HY-113421S
-
|
|
Isotope-Labeled Compounds
Cannabinoid Receptor
|
Neurological Disease
|
|
Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
|
-
- HY-135555
-
|
5-CT
|
5-HT Receptor
|
Neurological Disease
|
|
5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist . 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .
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-
- HY-122179
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
NUCC-555 is an activin antagonist. NUCC-555 interacts with Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107 in the Activin A binding pocket. NUCC-555 blocks Activin A-mediated hepatic stellate cells (HSCs) activation. NUCC-555 promotes liver regeneration and halts fibrosis progression in chronic liver disease models. NUCC-555 inhibits Activin A-mediated ovarian cell proliferation. NUCC-555 decreases FSH levels in ovariectomized mice .
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-
- HY-121621
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guinea pigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guinea pigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated .
|
-
- HY-117912
-
|
|
Others
|
Cardiovascular Disease
|
|
TRC210258 is a TGR5 agonist with activity to improve diabetes-associated hyperglycemia and dyslipidemia. TRC210258 promotes energy expenditure by enhancing the release of glucagon-like peptide-1. TRC210258 is able to improve glucose metabolic control in high-fat diet-induced obese mice. TRC210258 also showed improvement in lipid parameters in high-fat-fed hamsters, including reductions in plasma triglyceride and low-density lipoprotein cholesterol levels. TRC210258 improved emerging lipid-related cardiovascular risk parameters including remnant cholesterol and triglyceride clearance .
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-
- HY-W024365R
-
|
|
PROTAC Linkers
|
Cancer
|
|
3-tert-Butyl-4-methoxyphenol (Standard) is the analytical standard of 3-tert-Butyl-4-methoxyphenol. This product is intended for research and analytical applications. 3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system .
|
-
- HY-16561
-
|
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-12220
-
MM-102
4 Publications Verification
HMTase Inhibitor IX
|
Histone Methyltransferase
Apoptosis
NF-κB
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
|
-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
|
-
- HY-136523
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .
|
-
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-116330A
-
|
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
Cancer
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
|
-
- HY-100839
-
|
D,L-(tetrazol-5-yl)glycine; LY 285265
|
iGluR
|
Neurological Disease
|
|
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist . (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively . (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice .
|
-
- HY-18099
-
S1RA
1 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
|
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
|
-
- HY-D1065
-
|
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
NIR-H2O2 is a cell-permeable near-infrared (NIR) fluorescent turn-on sensor. NIR-H2O2 has both absorption and emission in the NIR region. NIR-H2O2 responds to H2O2 with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-H2O2 is capable of imaging endogenously produced H2O2 in living cells and mice .
|
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-108039
-
|
HE 3286; NE-3107
|
NF-κB
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis . Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-125961
-
|
|
Others
|
Cancer
|
|
T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream) .
|
-
- HY-146001
-
|
|
Influenza Virus
|
Inflammation/Immunology
|
|
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice .
|
-
- HY-139192A
-
|
|
iGluR
TRP Channel
ERK
|
Neurological Disease
|
|
NMDAR/TRPM4-IN-2 free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 free base shows neuroprotective activity. NMDAR/TRPM4-IN-2 free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss .
|
-
- HY-139439
-
|
|
Ser/Thr Protease
|
Cancer
|
|
SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity . SBI-581 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-P99048
-
|
IBI308
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Sintilimab (IBI308) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
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- HY-151799
-
|
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p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
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- HY-148572
-
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Indoleamine 2,3-Dioxygenase (IDO)
NAMPT
|
Cancer
|
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NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
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- HY-P99744
-
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TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
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- HY-P2260B
-
|
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HIV
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Infection
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Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
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- HY-P2260C
-
|
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HIV
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Infection
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Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
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-
- HY-155199
-
|
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Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD .
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- HY-125858B
-
|
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Drug-Linker Conjugates for ADC
MDM-2/p53
|
Others
|
|
(S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
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- HY-A0081R
-
|
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
|
Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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-
- HY-158138
-
|
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PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
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-
- HY-113484
-
|
LTB5
|
Others
|
Cancer
|
|
Leukotriene B5 (LTB5) is a leukotriene with diverse biological activities. It is a metabolite of eicosapentaenoic acid formed through the 5-lipoxygenase (5-LO) pathway. LTB5 increases contraction of bullfrog lung strips ex vivo in a concentration-dependent manner. In vivo, LTB5 (100 nM) reduces tumor volume in mice injected with Tm1 murine melanoma cells. LTB5 also elicits chemokinesis and lysosomal enzyme release from polymorphonuclear leukocytes (PMNLs) 20- to 30-fold less, and induces platelet aggregation 8-fold less, potently than LTB4.
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- HY-162585
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
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-
- HY-161781
-
|
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HSP
EGFR
Akt
Survivin
|
Cancer
|
|
HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
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- HY-163799
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-162729
-
|
|
Histone Demethylase
Monoamine Oxidase
TGF-beta/Smad
|
Cardiovascular Disease
|
|
LSD1-IN-34 (Compound 7d) is the orally active inhibitor for Lysine-specific demethylase (LSD) and monoamine oxidase (MAO), with IC50 of 4.51 and 18.46 nM, for LSD1 and MAO A. LSD1-IN-34 inhibits the Ang II-induced neonatal rat myocardial fibroblasts (NRCFs) activation, without significant toxicity (20 μM). LSD1-IN-34 inhibits TGFβ/Smad signaling pathway, and ameliorates heart failure in mice. LSD1-IN-34 exhibits good pharmacokinetic characteristics in rats .
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- HY-B1400R
-
|
|
Parasite
SARS-CoV
|
Infection
Inflammation/Immunology
|
Diiodohydroxyquinoline (Standard) is the analytical standard of Diiodohydroxyquinoline. This product is intended for research and analytical applications. Diiodohydroxyquinoline (Iodoquinol, 5,7-Diiodo-8-hydroxyquinoline, 5,7-Diiodo-8-quinolinol) has an orally active and satisfactory antiparasitic properties. Diiodohydroxyquinoline exhibits mutagenic potential in mice and potent anti-SARS-CoV-2 activity with an EC50 value of 1.38 μM in VeroE6 cells. Diiodohydroxyquinoline's antimutagen is ascorbic acid. Diiodohydroxyquinoline is promising for research in inflammationin, testinal amebiasis, amebic liver abscess and chronic nonspecific diarrheas .
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-
- HY-16561G
-
|
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-123237
-
|
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c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
- HY-B1005R
-
|
|
Bacterial
Antibiotic
|
Cancer
|
|
8-Hydroxyquinoline (Standard) is the analytical standard of 8-Hydroxyquinoline. This product is intended for research and analytical applications. 8-Hydroxyquinoline (8-Quinolinol) is a lipophilic metal chelator that can be used as a fungicide .8-Hydroxyquinoline shows the MIC range of 27.56-55.11 μM (4-8 μg/mL) against the clinical isolates of Neisseria gonorrhoeae. 8-Hydroxyquinoline can bind to copper form complexes and transport copper into cells. 8-Hydroxyquinoline increases in the number of micronucleated polychromatic erythrocytes and can also make hair depigmented in mice .
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-
- HY-161935
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid (Compound 2) exhibits antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Vancomycin enterococci (VRE). 6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid interfers with the integrity and function of the bacterial cell membrane, and affects metabolism in MRSA. 6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid exhibits anti-inflammatory and anti-infective efficacy, and promotes angiogenesis in mice .
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-
- HY-161953
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC50=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects .
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-
- HY-111077
-
|
|
JAK
STAT
|
Inflammation/Immunology
Cancer
|
|
INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma .
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-
- HY-164477
-
|
|
Androgen Receptor
|
Cancer
|
|
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
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-
- HY-W001925
-
|
|
Apoptosis
NF-κB
c-Met/HGFR
Akt
MMP
|
Cancer
|
|
7-Methoxy-1-tetralone is a potent antitumor agent. 7-Methoxy-1-tetralone inhibits cancer cell proliferation and migration, and induces hepatocellular carcinoma cell (HCC) apoptosis. 7-Methoxy-1-tetralone decreased the protein levels of NF-κB, matrix metallopeptidase 2 (MMP2)/MMP9, and p-AKT. 7-Methoxy-1-tetralone showed antitumor activity in nude mice and had no effect on body weight and liver, spleen and organ index .
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-
- HY-110133A
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
JTE-607 free base, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 free base inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively . Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 free base .
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-
- HY-165061
-
|
Sciadonic acid
|
Others
|
Inflammation/Immunology
|
|
5(Z),11(Z),14(Z)-Eicosatrienoic acid (Sciadonic acid), a polyunsaturated fatty acid sourced from maritime pine seed oil, gymnospermae leaves and seeds, and freshwater gastropods, has been shown to reduce high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1 when included in their diet. In vitro studies indicate that it diminishes cholesterol efflux, and when applied topically in its methyl ester form, it alleviates inflammatory processes, likely by displacing arachidonic acid from phospholipid pools and lowering concentrations of downstream inflammatory mediators such as prostaglandin E2 and leukotrienes.
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-
- HY-12443
-
|
|
Casein Kinase
|
Neurological Disease
|
|
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
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-
- HY-145774
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester proagent of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice .
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-
- HY-W007223
-
|
D-5-HTP; 5-Hydroxy-D-tryptophan
|
5-HT Receptor
|
Neurological Disease
|
|
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range .
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-
- HY-156792
-
|
|
Others
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
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-
- HY-14393R
-
|
Frangula emodin (Standard)
|
SARS-CoV
Casein Kinase
Autophagy
11β-HSD
|
Cancer
|
|
Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
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-
- HY-12678S1
-
|
NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
|
Cancer
|
|
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
|
-
- HY-122189
-
|
(-)-Akuammine; Vincamajoridine
|
Others
|
Neurological Disease
|
|
Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC50s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.
|
-
- HY-125172
-
|
Polyglutamine Aggregation inhibitor III
|
Others
|
Others
|
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s=25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2 transgenic mouse model of Huntington's disease.
|
-
- HY-W052508
-
|
N-Desalkylquetiapine
|
5-HT Receptor
|
Neurological Disease
|
|
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
|
-
- HY-15074
-
|
NS-1209
|
iGluR
|
Neurological Disease
|
|
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
|
-
- HY-163879
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
|
Neurological Disease
|
|
hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
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-
- HY-115681R
-
|
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (Standard) is the analytical standard of (2R/S)-6-PNG. This product is intended for research and analytical applications. (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
|
-
- HY-164384
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
|
-
- HY-N6715R
-
|
|
Influenza Virus
Bacterial
Enterovirus
Photosystem II
|
Infection
Cancer
|
|
Tenuazonic acid (Standard) is the analytical standard of Tenuazonic acid. This product is intended for research and analytical applications. Tenuazonic acid is a nonhost-selective mycotoxin belonging to the tetramic acids family. Tenuazonic acid inhibits protein biosynthesis on ribosomes by suppressing the release of new protein. Tenuazonic acid is acutely toxic, and oral LD50 is set between 81-186 mg/kg in rats and mice. Tenuazonic acid blocks electron transport beyond the primary quinone receptor (QA) by interacting with the D1 protein and is a photosystem II (PSII) inhibitor. In addition, Tenuazonic acid has antiviral effects on measles virus, enterovirus, respiratory virus and so on. Tenuazonic acid has an inhibitory effect on skin cancer .
|
-
- HY-103388
-
|
|
COX
TGF-β Receptor
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
NCX 466 is an orally active COX-1 and COX-2 inhibitor that exhibits anti-inflammatory and analgesic effects. Additionally, NCX 466 acts as a NO donor, exerting anti-inflammatory and antioxidant effects by improving microcirculation. NCX 466 significantly reduces the levels of transforming growth factor-β (TGF-β) and oxidative stress markers (such as thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG)), and it decreases leukocyte recruitment during inflammation by reducing myeloperoxidase (MPO) activity, thereby preventing bleomycin (HY-108345)-induced pulmonary fibrosis in mice .
|
-
- HY-164575
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
NH2-NODAGA is a NODAGA-type metal chelator that can bind to radionuclides to prepare radionuclide conjugates (RDCs). NH2-NODAGA can react with diethyl squarate in 0.5M phosphate buffer (room temperature, 2 h, pH 7-7.5) to obtain NODAGA.SA. NODAGA.SA can target L-lysine urea-L-glutamate (KuE), which is a key structure of prostate-specific membrane antigen (PSMA). NODAGA.SA.KuE can bind [68]Ga and can be used for PET examination of NMRInu/nu nude mice bearing LNCaP tumors.
|
-
- HY-W087187
-
|
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
|
Cancer
|
|
DOTAGA-anhydride is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide drug conjugates (RDCs). DOTAGA-anhydride can be used to label monoclonal antibodies (mAbs) such as trastuzumab (targeting HER2/neu receptor with an affinity of 5.5 nM) under mild conditions (PBS pH 7.4, 25 °C, 30 minutes) after chelation with indium-111. [111In-DOTAGA]-trastuzumab showed a tumor uptake of 65% ID/g in mice bearing breast cancer BT-474 xenografts 72 hours after injection, which is valuable for SPECT/CT imaging and biodistribution studies.
|
-
- HY-15076
-
|
NS-1209 sodium
|
iGluR
|
Neurological Disease
|
|
SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
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- HY-118775
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Others
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Others
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LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.
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- HY-135167
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CaMK
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Neurological Disease
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HOCPCA is a compound with neuroprotective activity that improves sensorimotor function in mice after experimental stroke. HOCPCA selectively binds to the CaMKIIα hub domain, modulates signaling of different CaMKII pools, and alleviates abnormal CaMKII signaling after cerebral ischemia. HOCPCA promotes hippocampal neuronal activity and enhances working memory. HOCPCA also normalizes Thr286 autophosphorylation in the cytoplasm after ischemia and downregulates ischemia-specific expression of active CaMKII enzymatic cleavage fragments. HOCPCA binds to the GHB binding site with 27-fold higher affinity than GHB and has good blood-brain barrier penetration ability .
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- HY-N13866
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Others
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Cancer
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Cucumarioside A2-2 is a triterpene glycoside with antitumor activity. Cucumarioside A2-2 can induce mouse macrophage polarization toward the M1 phenotype. Cucumarioside A2-2 pretreated macrophages can effectively and selectively target and kill multiple types of cancer cells. Cucumarioside A2-2-induced M1 macrophages can effectively target and penetrate tumor tissues and improve the survival rate of mice in an allogeneic model. Exogenous activation of Cucumarioside A2-2 provides a useful model for the subsequent development of antitumor cell immunosuppression .
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- HY-115314
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LG 30435
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Others
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Inflammation/Immunology
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Mequitamium iodide (LG 30435) is an antihistamine drug with antiallergic and bronchodilatory activity. Mequitamium iodide can effectively antagonize airway contraction and inflammatory responses induced by histamine and antigens. Mequitamium iodide has nanomolar affinity for the H1 and smooth muscle receptors of histamine and mequitin. Mequitamium iodide, when administered in aerosol form, significantly inhibits histamine- and antigen-induced increases in airway pressure in allergic mice. Mequitamium iodide reduces antigen-induced eosinophil accumulation in the airways. Mequitamium iodide also exhibits inhibitory effects on PAF-induced platelet aggregation and bronchoconstriction, and can be used in the study of allergic diseases such as rhinitis and asthma .
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- HY-114162B
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Others
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Cancer
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VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
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- HY-103117
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5-HT Receptor
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Neurological Disease
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S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV (Kis=6.6 and 8.9 nM, respectively). It is also an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptor (Ki=5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gαq and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2CINI receptors (EC50s=38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s=38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.
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- HY-D0186R
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Endogenous Metabolite
Thymidylate Synthase
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Infection
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2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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- HY-121659
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Others
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Cancer
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DCFBC is a prostate-specific membrane antigen (PSMA) inhibitor for small animal positron emission tomography (PET) imaging. [18F]DCFBC was prepared by reacting fluorine-18 labeled phenyl bromide with the precursor (S)-2-[3-[(R)-1-carboxy-2-thiolethyl]urea]-glutaric acid in ammonia-saturated methanol at 60°C for 10 min and then purified by C-18 reversed-phase HPLC. [18F]DCFBC was injected via the tail vein in severe combined immunodeficient mice for in vitro biodistribution or imaging. For in vitro biodistribution studies, mice were sacrificed at 5, 15, 30, 60, and 120 min after injection, and tumors, blood, and major organs were collected, weighed, and radioactivity was counted. Imaging was performed using a GE eXploreVista small animal PET scanner, collecting 12 consecutive 10-min frames. Results showed that the radiochemical yield of [18F]DCFBC averaged 16±6% (n=8) from 4-[18F]fluorophenyl bromide. Specific radioactivity ranged from 13 to 133 GBq/Amol (350-3600 Curie/mmol) with an average of 52 GBq/Amol (1392 Curie/mmol; n=6). Biodistribution and imaging studies showed high uptake of [18F]DCFBC in PIP tumors and almost no uptake in FLU tumors. High radiopharmaceutical uptake was also seen in the kidney and bladder; however, radioactivity washout from these organs was faster than from the PIP tumors. Maximum PIP tumor uptake was reached at 60 min post-injection at 8.16±2.55% injected dose/g and decreased to 4.69±0.89 at 120 min post-injection. The PIP tumor-to-muscle ratio was 20 at 120 min post-injection. Based on mouse biodistribution, the dose-limiting organ was the kidney (estimated human absorbed dose: 0.05 mGy/MBq; 0.2 rad/mCi). Conclusions: [18F]DCFBC localizes specifically to PSMA+ expressing tumors in mice and is suitable for small animal PET imaging. This novel radiopharmaceutical is an attractive candidate for further study in PET imaging of prostate cancer.
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- HY-N0394
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Endogenous Metabolite
Ferroptosis
ROS Kinase
Keap1-Nrf2
Reactive Oxygen Species
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Metabolic Disease
Inflammation/Immunology
Cancer
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L-Cystine is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-cystine reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and kidney stones
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- HY-N1441
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Afzelin
4 Publications Verification
Kaempferol-3-O-rhamnoside
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Mitochondrial Metabolism
PTEN
Autophagy
Bacterial
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin .
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- HY-B1941
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Endogenous Metabolite
Apoptosis
DNA/RNA Synthesis
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
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4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
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- HY-116330
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Calcium Channel
TRP Channel
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Neurological Disease
Inflammation/Immunology
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Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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- HY-16561R
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trans-Resveratrol (Standard); SRT501 (Standard)
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IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
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Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-149401
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EGFR
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Cancer
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EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
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- HY-123789
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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T-5342126 is a toll-like receptor 4 (TLR4) antagonist. It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50=27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s=110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.
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- HY-161887
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Epigenetic Reader Domain
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Cancer
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SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
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- HY-162895
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Polo-like Kinase (PLK)
Akt
CDK
Caspase
Apoptosis
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Cancer
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NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC50 value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC50 values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth .
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- HY-169059
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Ferroptosis
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Inflammation/Immunology
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Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
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- HY-165484
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Interleukin Related
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Inflammation/Immunology
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AVP-13358 is an orally active IgE inhibitor that effectively suppresses immunoglobulin E (IgE)-mediated immune responses, with IC50 values of 8 and 3 nM for IgE inhibition in vivo and in vitro in BALB/c mice, respectively. AVP-13358 acts directly on T cells, inhibiting the production and release of IL-4, IL-5, and IL-13. It also targets other markers critical for the development of allergic responses, including the B cell IgE receptor (CD23) in human monocytes and the CD23 and IL-4 receptors in mouse B cells. AVP-13358 can be used in research related to anti-allergic responses .
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- HY-169135
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PROTACs
Proteasome
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Cancer
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PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for 20S proteasome subunit β5, with a DC50 of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC50 of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models . (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))
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- HY-123189
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Dopamine Receptor
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Neurological Disease
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LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guinea pigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .
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- HY-168166
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Others
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Neurological Disease
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CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .
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- HY-123882
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Others
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Others
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IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
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- HY-159897
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PAK
LIM Kinase (LIMK)
Apoptosis
Reactive Oxygen Species
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Cancer
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PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.) .
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- HY-W009356
-
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Endogenous Metabolite
Ferroptosis
ROS Kinase
Keap1-Nrf2
Reactive Oxygen Species
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Others
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L-Cystine hydrochloride is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine hydrochloride elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-Cystine hydrochloride reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine hydrochloride combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine hydrochloride is promising for research of cystinuria and kidney stones
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-
- HY-131527R
-
|
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Others
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Metabolic Disease
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Wy-45494 (hydrochloride) (Standard) is the analytical standard of Wy-45494 (hydrochloride). This product is intended for research and analytical applications. Wy-45494 hydrochloride (N-Desmethyl Venlafaxine hydrochloride; Wy 45494) is a minor active metabolite of the selective norepinephrine and serotonin reuptake inhibitor (SNRI) venlafaxine. It is formed from venlafaxine via the cytochrome P450 (CYP) isomer CYP3A4.2. Wy-45494 hydrochloride inhibits norepinephrine and serotonin reuptake in rat synaptosomal preparations (IC50s of 4.7 and 1.6 μM, respectively). In vivo, Wy-45494 hydrochloride reversed reserpine-induced hypothermia in mice at a minimum effective dose (MED) of 10 mg/kg.
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- HY-16561S1
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trans-Resveratrol-13C6; SRT501-13C6
|
Isotope-Labeled Compounds
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
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- HY-16561S
-
|
trans-Resveratrol-d4; SRT501-d4
|
Isotope-Labeled Compounds
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
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Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
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- HY-W017540
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ATP Synthase
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
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Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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- HY-149091
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|
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Others
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Cancer
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KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
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-
- HY-153808
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|
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Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
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Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
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- HY-149521
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|
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PI3K
|
Cancer
|
|
PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
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- HY-116330AR
-
|
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TRP Channel
Calcium Channel
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Neurological Disease
|
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Hyperforin (dicyclohexylammonium salt) (Standard) is the analytical standard of Hyperforin (dicyclohexylammonium salt). This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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-
- HY-N0058R
-
|
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HBV
Endogenous Metabolite
Apoptosis
Glucosidase
|
Infection
|
|
4,5-Dicaffeoylquinic acid (Standard) is the analytical standard of 4,5-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
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- HY-124110
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nAChR
|
Neurological Disease
|
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TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ∗ and α4β2 ∗ nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ∗ nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ∗ nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .
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- HY-W241345
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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DOTA-bis(tert-butyl)ester is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide conjugates (RDCs). DOTA-bis(tert-butyl)ester can be conjugated with different salts to form different metal chelators, such as (HY-B1244) hydrochloride to obtain DOTA-MN2. DOTA-MN2 can be reacted with [67]Ga-citrate to obtain radiolabeling. When (67)Ga-DOTA-MN2 is incubated in phosphate buffer solution or mouse plasma for 24 hours, it does not undergo significant decomposition. In the biodistribution experiment of NFSa tumor mice, it has high tumor uptake and rapid plasma clearance, and is a good material for SPECT and PET studies.
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- HY-169177
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JNK
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Inflammation/Immunology
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JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
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- HY-117881
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Opioid Receptor
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Neurological Disease
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CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
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- HY-159898
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Cholinesterase (ChE)
Amyloid-β
Tau Protein
NOD-like Receptor (NLR)
Reactive Oxygen Species
Mitochondrial Metabolism
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Neurological Disease
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AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model .
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- HY-B0561
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SC9420
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Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
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Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
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Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
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- HY-15800A
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LRRK2
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Neurological Disease
Inflammation/Immunology
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CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases .
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- HY-15800
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LRRK2
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Neurological Disease
Inflammation/Immunology
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CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases .
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- HY-145836
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FGFR
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Cancer
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FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
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-
- HY-N0976
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11b-Hydroxy-11b,1-dihydromedicarpin
|
Interleukin Related
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Inflammation/Immunology
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1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative . Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
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- HY-155156
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Endogenous Metabolite
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Cardiovascular Disease
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PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .
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-
- HY-155157
-
|
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Endogenous Metabolite
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Cardiovascular Disease
|
|
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .
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-
- HY-156798
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ADS032
1 Publications Verification
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NOD-like Receptor (NLR)
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Inflammation/Immunology
|
|
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation. ADS032 can reduce NLPR1 and NLRP3 activation of human macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduce NLRP3-induced ASC speck formation. ADS032 protected mice against the deadly influenza A virus, reducing inflammation in the lungs and improving survival. ADS032 inhibits Nigericin (HY-127019)-induced IL-1β secretion with IC50s of 94.6 μM (No wash out) and 354 μM (Wash out) respectively .
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-
- HY-123929
-
|
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MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
|
Cancer
|
|
PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
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- HY-118243
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|
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Others
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Others
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KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
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- HY-163816
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Cytochrome P450
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Cancer
|
|
Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
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-
- HY-161863
-
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Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
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- HY-N1441R
-
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Mitochondrial Metabolism
PTEN
Autophagy
Bacterial
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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Afzelin (Standard) is the analytical standard of Afzelin. This product is intended for research and analytical applications. Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin .
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- HY-126969
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|
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Others
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Metabolic Disease
|
|
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
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-
- HY-167939
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|
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Others
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Inflammation/Immunology
|
|
(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
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- HY-168555
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|
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CDK
PROTACs
Apoptosis
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Cancer
|
|
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
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- HY-101448
-
|
WAY-171318
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MMP
Apoptosis
Interleukin Related
TNF Receptor
Caspase
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .
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- HY-P1925A
-
|
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PI3K
Reactive Oxygen Species
Apoptosis
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Cancer
|
|
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
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- HY-144668
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|
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Influenza Virus
|
Infection
|
|
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
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- HY-151852
-
|
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Endogenous Metabolite
|
Cardiovascular Disease
|
|
9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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- HY-116282
-
|
DSS (MW 5000); DXS (MW 5000)
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HIV
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Dextran sulfate sodium salt (MW 5000) is a polymer of anhydroglucose with a molecular weight of 5000. Dextran sulfate sodium salt (MW 5000) can be used to induce acute colitis and cause apoptosis of colonic epithelial cells in mice. The concentration dose used in the study was 5% (in feed, w/w). The sulfated polysaccharide dextran sulfate is also an effective inhibitor of HIV. Dextran sulfate sodium salt (MW 5000) can significantly inhibit HIV-1 replication at a concentration that does not significantly inhibit the blood coagulation process. Dextran sulfate sodium salt (MW 5000) protects MT-4 cells from HIV-1-induced cellular pathogenicity. Dextran sulfate-induced colitis can be inhibited by Puerarin (HY-N0145), Baicalein (HY-N0196), β-Caryophyllene (HY-N1415).
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-
- HY-124187
-
|
Ethyl pinolenate
|
Biochemical Assay Reagents
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Others
|
|
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
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-
- HY-N8501
-
|
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Others
|
Infection
|
|
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities. It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s=3.94, 0.6, 2.21, 4.55, and 2.21 μg/mL, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50=5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg/mL) induces apoptosis in HL-60 cells. It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.
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- HY-138232
-
|
LTNAM
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Others
|
Neurological Disease
|
|
Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
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- HY-B1941R
-
|
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Endogenous Metabolite
Apoptosis
DNA/RNA Synthesis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
4-tert-Octylphenol (Standard) is the analytical standard of 4-tert-Octylphenol. This product is intended for research and analytical applications. 4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
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- HY-N0092R
-
|
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR .
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation .
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes .
In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
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- HY-B0612B
-
|
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Others
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Neurological Disease
|
|
(S)-Lercanidipine is a calcium channel blocker with antihypertensive and neuroprotective activities. (S)-Lercanidipine reduces oxidative stress and protects auditory sensory hair cells from noise-induced damage. (S)-Lercanidipine showed significant protective effects on cell viability in in vitro experiments, especially at low concentrations. (S)-Lercanidipine has been found to effectively reduce the hearing threshold of mice after noise stimulation and protect the survival of outer hair cells. The antioxidant properties of (S)-Lercanidipine are reflected in its increased expression of antioxidant enzyme genes and decreased expression of oxidative enzyme genes. (S)-Lercanidipine administration is effective in reducing noise-induced hearing loss both before and after noise exposure. (S)-Lercanidipine may alleviate noise-induced hearing loss and protect the survival of outer hair cells through its antioxidant mechanism .
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- HY-B0824A
-
|
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Others
|
Others
|
|
(1R)-cis-Bifenthrin is a widely used pyrethroid pesticide with activity that reduces motor coordination. (1R)-cis-Bifenthrin has a significant impact on the motor function of ParKin-/- mice, as shown by increased pole climbing time and wheel running Time decreases. Exposure of (1R)-cis-Bifenthrin resulted in a significant reduction in tyrosine hydroxylase-positive cell counts and protein expression. (1R)-cis-Bifenthrin caused increased expression of mitophagy-related proteins LC3B and p62. (1R)-cis-Bifenthrin has a lower binding energy with transferrin and transferrin receptor 2, showing stronger interactions. The biological effects of (1R)-cis-Bifenthrin show relationships with mitophagy and ferroptosis-related pathways .
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-
- HY-N6972
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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-
- HY-116282A
-
|
DSS (MW 4500-5500); DXS (MW 4500-5500)
|
HIV
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Dextran sulfate sodium salt (MW 4500-5500) is a polymer of anhydroglucose with a molecular weight of 4500-5500. Dextran sulfate sodium salt (MW 4500-5500) can be used to induce acute colitis and cause apoptosis of colonic epithelial cells in mice. The recommended molecular weight in the study is 5000 (HY-116282) and the use concentration is 5% (in feed, W/W). The sulfated polysaccharide dextran sulfate is also an effective inhibitor of HIV. Dextran sulfate sodium salt (MW 4500-5500) can significantly inhibit HIV-1 replication at concentrations that do not significantly inhibit the blood coagulation process. Dextran sulfate sodium salt (MW 4500-5500) protects MT-4 cells from HIV-1-induced cellular pathogenicity. Dextran sulfate-induced colitis can be inhibited by Puerarin (HY-N0145), Baicalein (HY-N0196), β-Caryophyllene (HY-N1415).
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-
- HY-A0139
-
|
NSC 108165; Navan; Navane
|
Others
|
Others
|
|
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
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-
- HY-159606
-
|
|
MDM-2/p53
|
Cancer
|
|
MS182 (compound 11) is an acetylation targeting chimera (AceTAC) designed based on p53 Y220C stabilizer and targeting p53 Y220C. MS182 is composed of p53 Y220C and p300/CBP binders, respectively, coupled by a linker. MS182 forms a ternary complex with p300/CBP acetyltransferase and p53 Y220C in a time- and concentration-dependent manner, effectively acetylating lysine at position 382 of p53 Y220C (ACE50: 1.52 μM). MS182 also exhibited considerable bioavailability in mice, with GI50 values of 2.16 μM and 1.83 μM for BxPC3 (p53 Y220C/-) and NUGC (p53 Y220C/+), respectively .
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-
- HY-12882
-
|
RC 61-91; NP-120
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iGluR
|
Neurological Disease
|
|
Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
|
-
- HY-W017113
-
|
|
Endogenous Metabolite
Aryl Hydrocarbon Receptor
|
Metabolic Disease
|
|
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
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-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
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-
- HY-14608R
-
|
|
Endogenous Metabolite
iGluR
Ferroptosis
Apoptosis
|
Neurological Disease
|
L-Glutamic acid (Standard) is the analytical standard of L-Glutamic acid. This product is intended for research and analytical applications. L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases .
IC50 & Target:DA .
In Vitro: L-Glutamic acid (120, 500, 750, 1000 mg/dL) can reduce the harmful effect of lithium on the embryonic development of Xenopus Xenopus .
L-Glutamic acid (2, 5, 10, 20 mM, 24-48 h) can induce neuroexcitotoxicity in neuroblastoma .
In Vivo: L-Glutamic acid (3 g/kg, subcutaneous injection) can promote excitotoxic degeneration of retinal ganglion cells in mice .
L-Glutamic acid (750 mg/kg, intraperitoneal injection) can reduce and inhibit oxidative stress induced by chlorpyrifos (CPF) in rats .
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-
- HY-N6972R
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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-
- HY-163345
-
|
|
5-HT Receptor
|
Neurological Disease
|
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
Pharmacokinetic Analysis ICR Male Mice
药代动力学分析
| Plasma |
Intravenous Administration |
Intraperitoneal Administration |
| Tmax (h) |
0.08 |
0.25 |
| T1/2 (h) |
0.77 |
1.06 |
| Cmax (ng/mL) |
33.07 |
156.44 |
| AUClast (ng·h/mL) |
28.31 |
143.27 |
| CL (L/h/kg) |
41.61 |
- |
| Vss (L/kg) |
32.43 |
- |
| MRT (h) |
0.79 |
0.93 |
| F (%) |
50.60 |
|
|
-
- HY-125726
-
|
(3'-sulfo)Galβ-Cer(d18:1/24:1); N-Nervonoyl Sulfatide; C24:1 Sulfatide
|
Others
|
Inflammation/Immunology
|
|
Sulfo galactosylceramide (N-Nervonoyl Sulfatide; C24:1 Sulfatide) is a member of the sulfatide class of glycolipids. It is the predominate sulfatide species in mature myelin, and it accumulates at a higher rate than C24 3’-sulfo galactosylceramide in rat cerebellum from seven to 32 days of age when active myelination occurs. It interacts with C-type lectins and immunoglobulin-like receptors with the highest affinity for LMIR5. It induces production of MCP-1 in basophils but not mast cells and increases the activation of NFAT in a reporter assay via LMIR5. Sulfo galactosylceramide is an immunodominant species in myelin, is bound by CD1d in vitro, and increases proliferation in isolated mouse splenocytes. It reduces symptoms and increases survival in a mouse model of chronic relapsing-remitting experimental autoimmune encephalomyelitis (EAE) when used at a dose of 20 μg. It also decreases the number of inflammatory lesions and infiltrating mononuclear cells in the lumbar spinal cord of EAE mice. As this product is derived from a natural source, there may be variations in the sphingoid backbone.
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-
- HY-N0394R
-
|
|
Endogenous Metabolite
Ferroptosis
ROS Kinase
Keap1-Nrf2
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
L-Cystine (Standard) is the analytical standard of L-Cystine. This product is intended for research and analytical applications. L-Cystine, the extracellular form of L-Cysteine (HY-Y0337), is a nutritionally dispensable semiessential sulfur-containing amino acid, occurring in proteins of plants and animals. L-Cystine induces Nrf2 protein elevation in a Keap1 (HY-P75897)-dependent manner and activates Nrf2 transcription factor. L-cystine can elicit cytoprotection by reducing ROS generation and protecting against oxidant- or doxorubicin-induced apoptosis. The reduced reabsorption of L-Cystine in renal tubules and its poor solubility in urine are the important causes of cystine precipitation and cystine crystal formation eventually leading to kidney stones. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and cystinosis
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-
- HY-B2176R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
ATP (Standard) is the analytical standard of ATP. This product is intended for research and analytical applications. ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation .
In Vitro: ATP (5 mM; 1 hour) co-treatment with LPS (1 μg/mL) has a synergistic effect on the activation of the NLRP3 inflammasome in HGFs .
ATP (2 mM; 0.5-24 hours) induces secretion of IL-1β, KC and MIP-2 from BMDMs in a caspase-1 activation-dependent manner .
ATP promotes neutrophil chemotaxis in vitro .
In Vivo: ATP (50 mg/kg; i.p.) protects mice against bacterial infection in vivo .
ATP induces the secretion of IL-1β, KC and MIP-2 and neutrophils recruitment in vivo .
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-
- HY-117087
-
|
|
Others
|
Cancer
|
|
K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-N2037
-
|
Norcoclaurine; Demethyl-Coclaurine
|
MAP3K
MDM-2/p53
Adrenergic Receptor
ROS Kinase
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
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-
- HY-N0469R
-
|
|
Endogenous Metabolite
Virus Protease
HSV
|
Infection
Metabolic Disease
Inflammation/Immunology
|
L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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-
- HY-B2167R
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
|
-
- HY-117811
-
|
L-680574
|
Others
|
Others
|
|
(R,R)-MK 287 is a tetrahydrofuran derivative that effectively inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with K1 values of 6.1 ± 1.5, 3.2 ± 0.7, and 5.49 ± 2.3 nM, respectively. The inhibition is stereospecific and competitive. Its racemate, L-668,750, is less potent, and its enantiomer, L-680574, is only 1/20 as potent as MK 287. MK 287 inhibits the binding of [3H]C18-PAF to human PMN membranes, reducing the affinity of the radioligand without changing the number of receptor sites. The binding of other radioligands (e.g., LTB4, LTC4, C5a, FMLP) to their specific receptors is unchanged at 1-10 microM MK 287. [3H]MK 287 binds to human platelet and PMN membranes with KD values of 2.1 ± 0.6 and 2.9 ± 1.2 nM. When tested on isolated human cells, MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50 = 56 ± 38 nM or ED50 = 1.5 ± 0.5 nM for gel-filtered platelets) and elastase release from PMNs (ED50 = 4.4 ± 2.6 nM). In vivo studies, MK 287 inhibited PAF-induced lethality in mice (ED50 = 0.8 mg/kg oral) and PAF-induced bronchospasm in guinea pigs (ED50 = 0.18 mg/kg intraduodenally and 0.19 mg/kg intravenously). The inhibition of PAF-induced bronchospasm was accompanied by a rightward shift in the concentration-response curve for PAF-induced platelet aggregation measured in vitro.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D0211
-
|
|
Fluorescent Dyes/Probes
|
|
Phenolphthalein is an acid-base indicator that is colorless in an acidic environment and pink in an alkaline environment. Phenolphthalein is genotoxic and potentially carcinogenic to mice. In addition, phenolphthalein is also a blood indicator .
|
-
- HY-150236
-
|
|
Dyes
|
|
FITC-labeled Tominersen (sodium) is the Tominersen labeled with FITC. Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
|
-
- HY-15096
-
|
FJ-776
|
Dyes
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-D2203
-
|
|
Fluorescent Dyes/Probes
|
|
BODIPY BDP4 has ssuperb sonosensitivity and high SDT efficiency against cancer cells and tumors in tumor-bearing mice .
|
-
- HY-D1535
-
|
|
Fluorescent Dyes/Probes
|
|
IR 813 perchlorate is a near-infrared (NIR) fluorescent dye (Ex=815 nm, Em=840 nm) and can be used for visualizing regional lymph nodes in mice .
|
-
- HY-D2095
-
|
|
Fluorescent Dyes/Probes
|
|
Medical fluorophore 33 is a novel quinoline-isoquinoline salt. Medical fluorophore 33 exhibits a strong fluorescent signal, good microsomal stability and high biocompatibility in vivo. Medical fluorophore 33 has antitumor activity in colorectal cancer mice .
|
-
- HY-D1066
-
|
|
Fluorescent Dyes/Probes
|
|
NIR-Thiol dinitrobenzenesulfonate has both absorption and emission in the NIR region. NIR-Thiol dinitrobenzenesulfonate responds to thiol with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-Thiol dinitrobenzenesulfonate is capable of imaging endogenously produced thiol in living cells and mice .
|
-
- HY-D2279
-
|
|
Fluorescent Dyes/Probes
|
|
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively .
|
-
- HY-D1460
-
|
|
Fluorescent Dyes/Probes
|
|
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies .
|
-
- HY-149696
-
|
|
Dyes
|
|
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
|
-
- HY-D1065
-
|
|
Fluorescent Dyes/Probes
|
|
NIR-H2O2 is a cell-permeable near-infrared (NIR) fluorescent turn-on sensor. NIR-H2O2 has both absorption and emission in the NIR region. NIR-H2O2 responds to H2O2 with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-H2O2 is capable of imaging endogenously produced H2O2 in living cells and mice .
|
-
- HY-16561G
-
|
trans-Resveratrol (GMP); SRT501 (GMP)
|
Fluorescent Dye
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
| Cat. No. |
Product Name |
Type |
-
- HY-NP003
-
|
Collagen
|
Native Proteins
|
|
Collagen, Type II, from bovine snout membrane is a type II collagen that can induce osteoarthritis by eliciting a strong and sustained T cell response. Type II collagen can be used to model collagen-induced arthritis in mice .
|
-
- HY-40156
-
|
|
Biochemical Assay Reagents
|
|
5-Fluoroindole is an antibacterial agent, that inhibits Mycobacterium tuberculosis with a MIC of 4.7 μM. 5-Fluoroindole exhibits metabolic stability in rat liver microsomes. 5-Fluoroindole exhibits anti-tuberculosis efficacy in mice .
|
-
- HY-D0873
-
|
EPPS
|
Buffer Reagents
|
|
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier .
|
-
- HY-B2241A
-
|
Aluminum potassium sulfate dodecahydrate, for cell culture
|
Cell Assay Reagents
|
|
Potassiumalum, for cell culture (Aluminum potassium sulfate dodecahydrate, for cell culture) is an egg white adjuvant that can induce allergic reactions in mice; it can also be used for bacterial staining. Potassiumalum, for cell culture is a biomaterial or organic compound that can be used in life science research .
|
-
- HY-109506
-
DPPC
5 Publications Verification
129Y83
|
Drug Delivery
|
|
DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
|
-
- HY-N1428A
-
|
|
Buffer Reagents
|
|
Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
-
- HY-W250113
-
|
Zymosan A from Saccharomyces cerevisiae
|
Carbohydrates
|
|
Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury .
|
-
- HY-B2201
-
|
Sodium citrate; Trisodium citrate anhydrous
|
Buffer Reagents
|
|
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice .
|
-
- HY-W100403
-
|
Choline p-toluenesulfonate
|
Enzyme Substrates
|
|
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) .
|
-
- HY-158272
-
|
|
Biochemical Assay Reagents
|
|
Penicillin/OVA is a conjugate of penicillin and Ovalbumins (HY-W250978), that is utilized as an antigen in immunological research. Penicillin/OVA causes IgE-dependent anaphylactic response to penicillin in mice .
|
-
- HY-109506R
-
|
|
Drug Delivery
|
|
DPPC (Standard) is the analytical standard of DPPC. This product is intended for research and analytical applications. DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
|
-
- HY-N1428AR
-
|
|
Buffer Reagents
|
|
Citric acid (monohydrate) (Standard) is the analytical standard of Citric acid (monohydrate). This product is intended for research and analytical applications. Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice .
|
-
- HY-157252
-
|
|
Drug Delivery
|
|
CL4F8-6 is an ionizable cationic lipid with a pKa of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice .
|
-
- HY-16561G
-
|
trans-Resveratrol (GMP); SRT501 (GMP)
|
Biochemical Assay Reagents
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-W001925
-
|
|
Biochemical Assay Reagents
|
|
7-Methoxy-1-tetralone is a potent antitumor agent. 7-Methoxy-1-tetralone inhibits cancer cell proliferation and migration, and induces hepatocellular carcinoma cell (HCC) apoptosis. 7-Methoxy-1-tetralone decreased the protein levels of NF-κB, matrix metallopeptidase 2 (MMP2)/MMP9, and p-AKT. 7-Methoxy-1-tetralone showed antitumor activity in nude mice and had no effect on body weight and liver, spleen and organ index .
|
-
- HY-116282
-
|
DSS (MW 5000); DXS (MW 5000)
|
Carbohydrates
|
|
Dextran sulfate sodium salt (MW 5000) is a polymer of anhydroglucose with a molecular weight of 5000. Dextran sulfate sodium salt (MW 5000) can be used to induce acute colitis and cause apoptosis of colonic epithelial cells in mice. The concentration dose used in the study was 5% (in feed, w/w). The sulfated polysaccharide dextran sulfate is also an effective inhibitor of HIV. Dextran sulfate sodium salt (MW 5000) can significantly inhibit HIV-1 replication at a concentration that does not significantly inhibit the blood coagulation process. Dextran sulfate sodium salt (MW 5000) protects MT-4 cells from HIV-1-induced cellular pathogenicity. Dextran sulfate-induced colitis can be inhibited by Puerarin (HY-N0145), Baicalein (HY-N0196), β-Caryophyllene (HY-N1415).
|
-
- HY-124187
-
|
Ethyl pinolenate
|
Drug Delivery
|
|
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P6083
-
|
|
Peptides
|
Others
Cancer
|
|
RTSPSSR is synthesized peptide, which binds specifically to claudin-1 and visulizes the CRC tumor in mice, through near-infrared fluorescence imaging .
|
-
- HY-P1823
-
|
|
Akt
mTOR
Caspase
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
C-Reactive Protein (CRP) is an anti-pneumococcal plasma protein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma .
|
-
- HY-P0194
-
-
- HY-P0194A
-
-
- HY-P1438A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide S(Rat) TFA is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) TFA also reduces anxiety-like behavior in mice.
|
-
- HY-P10110
-
|
|
Autophagy
|
Neurological Disease
|
|
retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice .
|
-
- HY-P1437A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
|
-
- HY-P5724
-
|
|
Bacterial
|
Infection
|
|
Nv-CATH is an antibacterial peptide of frog origin. Nv-CATH has broad-spectrum antibacterial activity against gram-positive and gram-negative bacteria. Nv-CATH significantly protects mice from fatal infections caused by Staphylococcus aureus. Nv-CATH protects mice from bacterial infection through antimicrobial immunoregulatory duality .
|
-
- HY-P10746
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
EB1002 is a selective NK2R agonist. EB1002 significantly raises the expression levels of mitochondrial biosynthesis-related genes (like PGC-1α) in obese mice, indicating that it promotes energy expenditure by boosting mitochondrial activity. EB1002 also increases the insulin sensitivity and improves glycolipid metabolism of the mice. EB1002 is promising for research of obesity and type 2 diabetes .
|
-
- HY-P1726A
-
|
|
Melanocortin Receptor
|
Cancer
|
|
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
|
-
- HY-P0286
-
|
|
Peptides
|
Inflammation/Immunology
|
|
OVA Peptide (323-339) represents a T and B cell epitope of Ovalbumin (Ova), which is important in the generation and development of immediate hypersensitivity responses in BALB/c mice.
|
-
- HY-P4650
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Tyrosylhistidine is a dipeptide consisting of tyrosine and histidine (Tyr-His). Tyrosylhistidine is an orally active antihypertensive peptide. Tyrosylhistidine reduces blood pressure in mice in a model of spontaneous hypertension .
|
-
- HY-103290
-
|
|
Bradykinin Receptor
|
Others
|
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- HY-P5521
-
|
|
Peptides
|
Cardiovascular Disease
|
|
mLR12 is a Trem1 inhibitory peptide. mLR12 decreases aortic rupture rate in BAPN-induced Thoracic aortic aneurysm and dissection (TAAD) mice model .
|
-
- HY-P10721
-
|
|
Antibiotic
Bacterial
|
Infection
|
Plectasin is a peptide antibiotic derived from saprophytic fungi. Plectasin can kill pneumococcus in vitro. Plectasin can alleviate experimental peritonitis and pneumonia caused by pneumococcus in mice .
|
-
- HY-P10312
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models .
|
-
- HY-P5890
-
-
- HY-P5448
-
|
|
Peptides
|
Others
|
|
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
|
-
- HY-P1910
-
|
|
Peptides
|
Metabolic Disease
|
|
BDC2.5 mimotope 1040-51 is a mimotope peptide for diabetogenic T cell clone BDC2.5. isolated from non-obese diabetic mice .
|
-
- HY-P0107
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-P5003
-
|
|
MMP
|
Inflammation/Immunology
|
|
Collagen Type II Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen Type II Fragment can be used for research on inflammation and immunity .
|
-
- HY-P6053
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
|
-
- HY-P0009
-
|
SB-75
|
GnRH Receptor
|
Endocrinology
|
|
Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist. Cetrorelix inhibits the endogenous luteinizing hormone surge during ovarian stimulation. Cetrorelix reduces cyclophosphamide induced ovarian follicular destruction in mice .
|
-
- HY-P3856
-
|
|
Peptides
|
Neurological Disease
|
|
Endokinin C is a peptide component of endokinin. Endokinin C works as a neurotransmitter or modulator in the pain system. Pretreatment with endokinin C prevents induction of scratching behavior and thermal hyperalgesia of endokinin A/B in mice .
|
-
- HY-P2203
-
SAHM1
1 Publications Verification
|
Notch
|
Inflammation/Immunology
|
|
SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice .
|
-
- HY-P0107A
-
|
|
Bombesin Receptor
|
Inflammation/Immunology
|
|
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist . RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
|
-
- HY-P1624
-
|
ALX-0600
|
Nuclear Hormone Receptor 4A/NR4A
FXR
|
Inflammation/Immunology
|
|
Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
|
-
- HY-P1624A
-
|
ALX-0600 TFA
|
Nuclear Hormone Receptor 4A/NR4A
FXR
|
Inflammation/Immunology
|
|
Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
|
-
- HY-P1587
-
|
|
Peptides
|
Inflammation/Immunology
|
|
IRBP (1-20), human contains a major epitope for the H-2 b haplotype. IRBP (1-20), human induces experimental autoimmune uveoretinitis (EAU) in H-2 b mice .
|
-
- HY-P1241
-
-
- HY-P4094
-
CTP
1 Publications Verification
|
Peptides
|
Cardiovascular Disease
|
|
CTP is a cardiac targeting peptide. CTP transduces cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be used to deliver therapeutic peptides, proteins and nucleic acid specifically to the heart .
|
-
- HY-P4835
-
|
|
Peptides
|
Others
|
|
pTH (2-34) (human) (80 μg/kg) slightly increases serum osteocalcin levels and alkaline phosphatase activity of bone extract (markers of bone formation) in mice. pTH (2-34) is not as effective as pTH (1-34) .
|
-
- HY-P5437
-
|
|
PKC
|
Others
|
|
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
|
-
- HY-P10032
-
-
- HY-162396
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .
|
-
- HY-P1241A
-
-
- HY-P3707
-
|
|
Apoptosis
|
Cancer
|
|
Tumor targeted pro-apoptotic peptide (CNGRC-GG-D(KLAKLAK)2) is an anti-tumor peptide. Tumor targeted pro-apoptotic peptide disrupts mitochondrial membranes and promotes apoptosis, showing anticancer activity in mice .
|
-
- HY-P10102
-
|
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury .
|
-
- HY-P10136
-
|
human TREM-2 182-190
|
Peptides
|
Inflammation/Immunology
|
|
IA9 (human TREM-2 182-190) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model .
|
-
- HY-P1587A
-
|
|
Peptides
|
Inflammation/Immunology
|
|
IRBP (1-20), human TFA contains a major epitope for the H-2 b haplotype. IRBP (1-20), human TFA induces experimental autoimmune uveoretinitis (EAU) in H-2 b mice .
|
-
- HY-P1290A
-
|
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice .
|
-
- HY-P0085
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Splenopentin diacetate is a synthetic immunomodulating pentapeptide corresponding to the residues 32-36 of the splenic hormone splenin. Splenopentin diacetate influences both early T and B cell differentiation, to increase the number of antibody-forming cells in mice after gamma irradiation .
|
-
- HY-P5883
-
|
tatM2NX
|
TRP Channel
|
Neurological Disease
|
|
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. TAT-M2NX can be used to study ischemic neuronal damage .
|
-
- HY-P4885
-
|
AβpE3-40
|
Amyloid-β
|
Neurological Disease
|
|
Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice .
|
-
- HY-P5762
-
|
PNX-14
|
GnRH Receptor
|
Neurological Disease
|
|
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia .
|
-
- HY-P3134
-
|
|
Peptides
|
Metabolic Disease
|
|
CPN-267 (compound 7b) is a selective neuromedin U receptor 1 (NMUR1) agonist with the EC50 of 0.25 nM. CPN-267 suppresses body weight gain in mice and can be used for study of obesity .
|
-
- HY-P10612
-
|
|
Peptides
|
Metabolic Disease
|
|
Tetanus toxin peptide is a specific peptide isolated from the toxin produced by Clostridium tetani. Tetanus toxin peptide can be used as an immunogen to induce diabetes in mice. Tetanus toxin peptide can be used in the study of type 1 diabetes .
|
-
- HY-P1290
-
|
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice .
|
-
- HY-P1149
-
|
Epithalon; Epithalamin
|
Telomerase
|
Neurological Disease
Cancer
|
|
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa .
|
-
- HY-P10136A
-
|
human TREM-2 182-190 TFA
|
Peptides
|
Inflammation/Immunology
|
|
IA9 TFA (human TREM-2 182-190 TFA) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model .
|
- HY-P10200
-
|
|
Bacterial
|
Infection
|
|
CP7-FP13-2 is a peptide with antivirulence factor and antibacterial activity. CP7-FP13-2 inhibits the formation of Staphylococcus aureus biofilm and has good antibacterial efficacy in mice .
|
- HY-P10029
-
|
|
Peptides
|
Neurological Disease
|
|
Sakura-6 is a SERT-nnos interaction promoter that significantly increases the SERT-nnos complex, but reduces the level of SERT on the cell surface. Acute injection of Sakura-6 into the dorsal raphe nucleus (DRN) causes depression-like behavior in mice .
|
- HY-P1149A
-
|
Epithalon TFA; Epithalamin TFA
|
Telomerase
|
Neurological Disease
Cancer
|
|
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa .
|
- HY-P3304
-
|
|
GHSR
|
Neurological Disease
Cancer
|
|
MR 409 is a selected growth hormone-releasing hormone (GHRH) agonist. MR 409 has remarkable neuroprotective effects through enhancing endogenous neurogenesis in cerebral ischemic mice. MR 409 also inhibits the in vivo growth of lung cancer .
|
- HY-P5117
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice .
|
- HY-P10032A
-
- HY-P5742
-
|
|
Peptides
|
Cancer
|
|
ELAAWCRWGFLLALLPPGIAG (P5) is derived from rat HER2/neu protein with 21 amino acid length (aa 5-25). ELAAWCRWGFLLALLPPGIAG can induce cytotoxic T lymphocyte (CTL) responses in mice bearing HER2-positive tumours .
|
- HY-P10057
-
|
|
Apoptosis
|
Cancer
|
|
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC50 value of 130 nM. cpm-1285 reduces tumor burden in mice .
|
- HY-P2210A
-
|
|
Peptides
|
Neurological Disease
|
|
BigLEN(mouse) TFA is a GPR171 agonist. BigLEN(mouse) TFA is a proSAAS-derived neuropeptide. BigLEN(mouse) TFA regulates food intake in mice. BigLEN(mouse) inhibits the release of glutamate onto parvocellular neurons of the paraventricular nucleus in a process dependent upon activation of postsynaptic G proteins.
|
- HY-P2251
-
|
|
HIV
Microtubule/Tubulin
|
Infection
Inflammation/Immunology
Cancer
|
|
T-peptide, a Tuftsin analog, can be used for the research of human immunodeficiency virus (HIV) infection. T-peptide prevents cellular immunosuppression and improves survival rate in septic mice. T-peptide also can inhibit the growth of residual tumor cells after surgical resection .
|
- HY-P1949
-
|
|
Peptides
|
Cardiovascular Disease
Cancer
|
|
Cyclic MKEY is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY also protects against stroke-induced brain injury in mice .
|
- HY-105063
-
|
|
Peptides
|
Metabolic Disease
Inflammation/Immunology
|
|
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes .
|
- HY-P5878
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
|
- HY-P5578
-
|
|
GCGR
|
Metabolic Disease
|
|
A8SGLP-1 is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 reduces blood glucose in db/db mice without affecting its function .
|
- HY-P5975
-
|
Z-LLL-FMK
|
Cathepsin
SARS-CoV
|
Infection
|
|
Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge .
|
- HY-P3102
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
|
- HY-P5742A
-
|
|
Peptides
|
Cancer
|
|
ELAAWCRWGFLLALLPPGIAG TFA (P5) is derived from rat HER2/neu protein with 21 amino acid length (aa 5-25). ELAAWCRWGFLLALLPPGIAG TFA can induce cytotoxic T lymphocyte (CTL) responses in mice bearing HER2-positive tumours .
|
- HY-P10039
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) rat is a β-amyloid peptide (Abeta), a metal-binding domain fragment of amyloid. Three amino acid substitutions in β-Amyloid (1-16) rat that differ from humans render rats and mice less susceptible to AD-like neurodegeneration .
|
- HY-P1949A
-
|
|
Peptides
|
Cardiovascular Disease
Cancer
|
|
Cyclic MKEY TFA is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY TFA also protects against stroke-induced brain injury in mice .
|
- HY-13589
-
|
LU103793 free base
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer .
|
- HY-P5489
-
|
|
Peptides
|
Others
|
|
IGRP(206-214) is a biological active peptide. (This peptide corresponds to residues 206–214 of murine islet-specific glucose-6-phosphatase catalytic subunit–related protein (IGRP). This peptide is T cells specific for proinsulin and IGRP induces diabetes in non-obese diabetic (NOD) mice.)
|
- HY-P5578A
-
|
|
GCGR
|
Metabolic Disease
|
|
A8SGLP-1 TFA is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 TFA reduces blood glucose in db/db mice without affecting its function .
|
- HY-P5130
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
|
- HY-13589A
-
|
LU103793 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) hydrochloride is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin hydrochloride blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin hydrochloride can be used to research anticancer .
|
- HY-P1422
-
Spadin
1 Publications Verification
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research .
|
- HY-P3102A
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice .
|
- HY-108742
-
|
BA 058; BIM 44058
|
PTHR
Arrestin
|
Metabolic Disease
Cancer
|
|
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis .
|
- HY-P1136B
-
- HY-P1434
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
[Pro3]-GIP (mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (mouse) can be used for research of type 2 diabetes .
|
- HY-P10382
-
|
|
Peptides
|
Inflammation/Immunology
|
|
M133 peptide is a coronavirus-specific CD4 T cell epitope. M133 peptide is immunodominant in mice infected with the neurotropic coronavirus (the JHM strain of mouse hepatitis virus). M133 peptide forms a complex with MHC II molecules, which is recognized by specific TCRs, thereby activating CD4 T cells .
|
- HY-P0119
-
|
|
GCGR
MEK
Akt
MMP
JNK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe −/− Irs 2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .
|
- HY-P1422A
-
|
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research .
|
- HY-P1136C
-
- HY-P5550
-
|
|
Influenza Virus
|
Infection
|
|
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection .
|
- HY-108742A
-
|
BA 058 TFA; BIM 44058 TFA
|
Arrestin
PTHR
|
Metabolic Disease
Endocrinology
Cancer
|
|
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis .
|
- HY-P1089
-
|
PCC 88-104
|
Peptides
|
Inflammation/Immunology
|
|
Cytochrome c-pigeon (88-104) (PCC 88-104) has full stimulatory activity for pigeon cytochrome c-primed T cells from B10.A mice. The I-E k-restricted T cell response to Cytochrome c pigeon (pcyt c) is specific for the COOH-terminal sequence 88-104 .
|
- HY-P4154
-
|
ALM-488
|
Fluorescent Dye
|
Neurological Disease
Cancer
|
|
Bevonescein (ALM-488) is a novel, intravenously-administrated fluorescein-conjugated peptide that binds nerve-associated connective tissue, labels peripheral nerves under real-time fluorescence imaging (FL) in living mice and human ex vivo nerve tissue. Bevonescein is a peptide-linked tracer which fluorescently labeled both intact and degenerated nerves .
|
- HY-P10707
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Tpp-CAQK can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK, with excellent bioactivity. Mito-Tpp-CAQK can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury .
|
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
- HY-P5452
-
|
|
Peptides
|
Others
|
|
PKCd (8-17) is a biological active peptide. (This peptide is derived from the V1 domain of protein kinase C (PKC)d. It inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Inhibition of PKCd reduces ischemia damage in cardiac and cerebral cells, induces proliferation of fibroblasts, and inhibits graft coronary artery disease in mice.)
|
- HY-P3248
-
|
Myelin basic protein (85-99) antagonist
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
|
- HY-P1173
-
|
Myristoylated L 803; GSK-3β Inhibitor XIII
|
GSK-3
Amyloid-β
|
Neurological Disease
|
|
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
|
- HY-12557
-
|
|
CaSR
Wnt
TNF Receptor
|
Inflammation/Immunology
|
|
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation .
|
- HY-P10554
-
|
|
Peptides
|
Cardiovascular Disease
Others
Inflammation/Immunology
|
|
Myhc-α(334–352) is a sequence fragment of amino acid residues 334 to 352 of cardiac myosin heavy chain α. Myhc-α(334–352) is an immunodominant epitope that can induce autoimmune reactions in A/J mice, leading to the occurrence of myocarditis. Myhc-α(334–352) can be used to study the autoimmune pathways of myocarditis and dilated cardiomyopathy .
|
- HY-P5451
-
|
|
Peptides
|
Others
|
|
PLP (178-191) is a biological active peptide. (This is amino acids 178 to 191 fragment of the proteolipid protein (PLP), an immunodominant encephalitogenic epitope in SJL mice, one of two major encephalitogenic epitopes. PLP peptide 178 to 191 was compared with another encephalitogenic peptide, 139 to 151. The day of onset of disease induced by PLP 178 to 191 was earlier, but the incidence, severity, and histologic features were indistinguishable.)
|
- HY-P2260
-
|
|
Autophagy
HIV
|
Infection
|
|
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
|
- HY-P1259
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
- HY-P10653
-
|
|
HCV
HIV
|
Infection
|
|
C5A is a microbicidal peptide, anti-hepatitis C virus (HCV), and anti-HIV agent. C5A disrupts the membrane integrity of the HIV virion as well as the integrity of the conical capsid core that surrounds the viral genome. C5A inhibits in vitro infectivity of a broad range of primary HIV isolates in various primary target cells. C5A protects mice against vaginal and rectal HIV challenges .
|
- HY-P1302
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice .
|
- HY-P1259A
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
- HY-P2260A
-
|
|
Autophagy
HIV
|
Infection
|
|
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
|
- HY-P5581
-
|
|
Peptides
|
Infection
Inflammation/Immunology
Cancer
|
|
Alloferon 1 is an antiviral and antitumoral peptide. Alloferon 1 stimulates natural cytotoxicity of human peripheral blood lymphocytes. Alloferon 1 also induces IFN synthesis, and enhances antiviral and antitumor resistance in mice. Alloferon 1 also shows anti-inflammatory activity in λ-carrageenan-induced paw edema model. Alloferon 1 can be isolated from the blood of the blow fly Calliphora vicina (Diptera) .
|
- HY-P1617
-
|
|
Peptides
|
Neurological Disease
|
|
LY 190388 is a penicillamine-containing enkefa peptide analog with μ receptor agonist activity. LY 190388 showed analgesic effect in inhibiting the writhing response in mice after intracerebroventricular administration. The analgesic effect of LY 190388 is not caused by its δ receptor agonist action, but by its μ receptor agonist activity. When LY 190388 is used together with the δ receptor antagonist ICI 174864, an additive analgesic effect is produced .
|
- HY-P1302A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice .
|
- HY-P2264
-
|
|
Ephrin Receptor
|
Inflammation/Immunology
|
|
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
|
- HY-P10109A
-
|
hG6PI (325-339) hydrochloride
|
Peptides
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) hydrochloride is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) hydrochloride primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) hydrochloride induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
- HY-P10109
-
|
|
Peptides
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
- HY-P4641
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
- HY-P5121
-
|
|
Peptides
|
Cardiovascular Disease
|
|
γ-Fibrinogen377-395 is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in mice in vivo. γ-Fibrinogen377-395 can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation .
|
- HY-P5875
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
- HY-P5121A
-
|
|
Peptides
|
Cardiovascular Disease
|
|
γ-Fibrinogen377-395 TFA is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 TFA blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in mice in vivo. γ-Fibrinogen377-395 TFA can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation .
|
- HY-P5762A
-
|
PNX-14 TFA
|
GnRH Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Phoenixin-14 (PNX-14) TFA, a BBB-penatrable neuropeptide, has anxiolytic, cardioprotective and neuroprotective effect. Phoenixin-14 TFA can regulate pituitary gonadotrophin secretion by upregulating the GnRH receptor mRNA. Phoenixin-14 TFA stimulates insulin secretion. Phoenixin-14 TFA also protects mice from ischemia/reperfusion (IR) injury. PNX-14 TFA prevents oxidative stress by reducing ROS and increasing GSH .
|
- HY-P10567
-
|
|
Peptides
|
Others
|
|
Pip6a is an arginine-rich cell-penetrating peptide. Pip6a has the ability to deliver associated cargoes across the plasma and endosomal membranes and is stable to serum proteolysis. Pip6a is composed of a hydrophobic core region flanked on each side by arginine-rich domains containing β-alanine and aminohexanoyl spacers. Pip6a-conjugated morpholino phosphorodiamidate oligomer (PMO) dramatically enhanced antisense oligonucleotide (ASO) delivery into striated muscles of myotonic dystrophy (DM1) mice .
|
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
- HY-P10586A
-
|
MALP-2 TFA
|
Toll-like Receptor (TLR)
NO Synthase
|
Cardiovascular Disease
Metabolic Disease
|
|
Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL) .
|
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
|
- HY-P4190
-
|
|
GnRH Receptor
|
Endocrinology
|
|
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .
|
- HY-P2712
-
|
Chemerin148–156, mouse
|
Chemerin Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Chemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis .
|
- HY-P10586
-
|
MALP-2
|
Toll-like Receptor (TLR)
NO Synthase
|
Cardiovascular Disease
|
|
Macrophage-activating lipopeptide 2 (MALP-2) is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 can enhance endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 can enhance endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL) .
|
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
- HY-P2260B
-
|
|
HIV
|
Infection
|
|
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
|
- HY-P2260C
-
|
|
HIV
|
Infection
|
|
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
|
- HY-P5396
-
|
|
Peptides
|
Others
|
|
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
|
- HY-W007223
-
|
D-5-HTP; 5-Hydroxy-D-tryptophan
|
5-HT Receptor
|
Neurological Disease
|
|
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range .
|
- HY-W009356
-
|
|
Endogenous Metabolite
Ferroptosis
ROS Kinase
Keap1-Nrf2
Reactive Oxygen Species
|
Others
|
|
L-Cystine hydrochloride is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine hydrochloride elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-Cystine hydrochloride reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine hydrochloride combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine hydrochloride is promising for research of cystinuria and kidney stones
|
- HY-P1925A
-
|
|
PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
|
- HY-P5502
-
|
|
Peptides
|
Others
|
|
Influenza NP (311-325) is a biological active peptide. (This peptide is amino acids 311 to 325 fragment of the influenza virus nucleoprotein (NP). This bona fide MHC class II restricted epitope from influenza virus was used to study the host immunoresponse during the infection. This peptide elicits the strongest gamma interferon (IFN-gamma) production in the intracellular cytokine assays. It does not stimulate CD8 T-cells in mice.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
|
-
- HY-K6013
-
|
|
|
MCE Organoid Dissociation Solution is versatile and suitable for routine dissociation and passaging of organoids derived from various mammals (including humans, mice, pigs, cows, and more).
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99797
-
|
JR-141
|
Transferrin Receptor
|
Neurological Disease
|
|
Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice .
|
-
- HY-P9960
-
|
|
CD20
|
Inflammation/Immunology
|
|
Ocrelizumab (Ocrevus) is a humanized anti-CD20 monoclonal antibody. Ocrelizumab can induce B cell depletion and inhibit multiple sclerosis lesions in mice through antibody dependent cytotoxicity (ADCC) .
|
-
- HY-P99199
-
|
NI-0401
|
CD3
|
Inflammation/Immunology
|
|
Foralumab (NI-0401) is a potent, orally active human monoclonal antibody targeting the CD3. Foralumab modulates immune responses by human cells in NSG mice that were reconstituted with human hematopoietic stem cells .
|
-
- HY-P9944
-
|
MEDI 493
|
RSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Palivizumab (MEDI 493) is a humanized monoclonal antibody against respiratory syncytial virus (RSV). Palivizumab can bind to RSV F protein with a Kd value of 1.4 nM. Palivizumab can prevent respiratory syncytial virus infection in cotton mice .
|
-
- HY-P99216
-
|
PF-04360365; RN 1219
|
EGFR
|
Neurological Disease
|
|
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease .
|
-
- HY-P99908
-
|
NT-17
|
Interleukin Related
|
Cancer
|
|
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4 + and CD8 + cells in both human and mice. Efineptakin alfa can be used for glioblastoma research .
|
-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-P99708
-
|
ABBV-151; ARGX-115
|
TGF-beta/Smad
|
Cancer
|
|
Livmoniplimab (ABBV-151) is a monoclonal antibody against GARP/TGF-β1 that can inhibit the release of active TGF-β1. Livmoniplimab has anti-tumor activity in colon cancer mice. Livmoniplimab can be used for the study of locally advanced or metastatic solid tumors .
|
-
- HY-P99554
-
|
PRX-302
|
Inhibitory Antibodies
|
Cancer
|
|
Topsalysin is a PSA-activated protoxin, a pore-forming protein (synthetic proaerolysin) fusion protein with human prostate-specific antigen. Topsalysin has tumor suppression effect in mice modle .
|
-
- HY-P99354
-
|
Anti-Human CTLA4xLAG3
|
LAG-3
|
Inflammation/Immunology
Cancer
|
|
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activates T cells in NSG mice. Bavunalimab can be used for the research of cancer .
|
-
- HY-P99194
-
|
REGN1500
|
ANGPTL
Inhibitory Antibodies
|
Cardiovascular Disease
Metabolic Disease
|
|
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia .
|
-
- HY-108786
-
|
ENB-0040
|
Inhibitory Antibodies
|
Metabolic Disease
|
|
Asfotase alfa (ENB-0040) is a bone-targeted genetically engineered glycoprotein. Asfotase alfa increases the survival rate, bone mineralization and bone length and prevents mineralization defects of the feet, rib cage, lower limbs, jaw bones in Akp2 ?/? knockout mice. Asfotase alfa can be used for the research of perinatal, infantile, and juvenile-onset hypophosphatasia (HPP) .
|
-
- HY-P99588
-
|
MYO-029
|
TGF-β Receptor
|
Metabolic Disease
|
|
Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research .
|
-
- HY-P99583
-
|
MEDI4893
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
|
-
- HY-P99156
-
|
BMS-986016
|
LAG-3
|
Cancer
|
|
Relatlimab (BMS-986016) is a human monoclonal antibody anti-LAG-3 antibody generated by immunization of transgenic mice bearing human immunoglobulin miniloci with recombinant LAG-3 protein. Relatlimab blocks LAG-3/MHC II interaction with an IC50 value of 0.67 nM and LAG-3/FGL1 interaction with an IC50 value of 0.019 nM. Relatlimab can be used in research of cancer .
|
-
- HY-P99341
-
|
REGN10933
|
SARS-CoV
|
Infection
|
|
Casirivimab (REGN10933) is a human monoclonal antibody that targets the SARS-CoV-2 virus, which causes COVID-19. Casirivimab is ineffective against COVID-19 variants. Casirivimab can be used in combination with Imdevimab (HY-P99342), which alters the lung response of K18-hACE2 mice to the SARS-CoV-2 δ variant, effectively reducing viral load and improving symptoms .
|
-
- HY-P9983
-
|
HuM-195
|
Inhibitory Antibodies
Radionuclide-Drug Conjugates (RDCs)
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR? and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
|
-
- HY-P99163
-
|
ABBV-8E12; C2N-8E12
|
Tau Protein
|
Neurological Disease
|
|
Tilavonemab (ABBV-8E12) is a humanized anti-tau antibody that targets the extracellular form of pathological tau protein aggregates by binding to the N-terminal 25-30 amino acid residues of tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates, reduces the loss of brain volume, slows the progression of tau pathology, and improves cognitive abilities in transgenic mice expressing mutant human tau. Tilavonemab is used in Alzheimer's disease research .
|
-
- HY-P99620
-
|
CT-P22; CT120
|
Influenza Virus
|
Infection
|
|
Firivumab (CT-P22; CT120) is a human IgG1 monoclonal influenza A virus hemagglutinin (Anti-IAV HA) antibody. Firivumab is capable of neutralizing H1N1, H5N1, H6N1, H6N2, H8N4, H8N8, H9N2 and H12N7. Firivumab shows protection against H1N1 virus in mice .
|
-
- HY-P99048
-
|
IBI308
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Sintilimab (IBI308) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-N0031
-
-
- HY-N3312
-
-
- HY-N7944
-
-
- HY-133800
-
-
- HY-N5106
-
-
- HY-121271
-
-
- HY-B0430B
-
|
(±)-Pantothenate; (±)-Vitamin B5
|
Other disease
Disease markers
Endogenous metabolite
|
Others
|
|
(±)-Pantothenic acid ((±)-Pantothenate), a B-vitamin, is an essential vitamin required for the biosynthesis of coenzyme A (CoA) in mammalian cells. Pantothenic acid has protective activity against valproic acid (VPA)-induced neural tube defects (NTD) in CD-1 mice .
|
-
- HY-N2867
-
-
- HY-126645
-
-
- HY-N0700R
-
-
- HY-122365
-
-
- HY-N9173
-
-
- HY-N12127
-
-
- HY-N2953
-
-
- HY-121182
-
-
- HY-B0892
-
-
- HY-N4063
-
-
- HY-134579
-
-
- HY-N0546R
-
-
- HY-120912
-
-
- HY-B2194
-
-
- HY-N3522
-
-
- HY-121431
-
-
- HY-N7047
-
-
- HY-N0506
-
-
- HY-N7514
-
-
- HY-N9536
-
-
- HY-N12141
-
-
- HY-N1472
-
-
- HY-N3015
-
-
- HY-N6608
-
-
- HY-N4024
-
-
- HY-N11911
-
-
- HY-W345885
-
-
- HY-N6857
-
-
- HY-N0592
-
-
- HY-N1388
-
-
- HY-N0592A
-
-
- HY-N12016
-
-
- HY-113412AR
-
-
- HY-N7272
-
-
- HY-149101
-
-
- HY-19839
-
-
- HY-N0901AR
-
-
- HY-113354
-
-
- HY-109506
-
-
- HY-N7026
-
-
- HY-D0887
-
-
- HY-N11286
-
|
TG-DHA; Meganol D
|
Structural Classification
Natural Products
Animals
Source classification
|
Others
|
|
Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases .
|
-
- HY-121111
-
|
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Others
|
|
Agaritine is a compound isolated from the commonly cultivated commercial mushroom Agaricus bisporus. Agaritine is hydrolyzed by an enzyme system present in the mushroom into 4-(hydroxymethyl)benzenediazonium ion, which is a carcinogen in mice. Agaritine is structurally similar to some known carcinogens and can be used for research in cancer and food safety .
|
-
- HY-N0031R
-
-
- HY-N3312R
-
-
- HY-124717
-
-
- HY-N10390
-
-
- HY-B1192
-
-
- HY-N0219
-
-
- HY-N1428
-
-
- HY-N0278
-
-
- HY-119789
-
-
- HY-N12249
-
-
- HY-124941
-
-
- HY-N1570R
-
-
- HY-N5106R
-
-
- HY-W654264
-
-
- HY-66005
-
-
- HY-N6869
-
-
- HY-119347
-
-
- HY-113314
-
-
- HY-N11872
-
-
- HY-129297
-
-
- HY-N12353
-
-
- HY-B0892R
-
-
- HY-N0506R
-
-
- HY-N0088
-
-
- HY-N2342
-
-
- HY-N5097
-
-
- HY-Z0283
-
-
- HY-N2573
-
-
- HY-N12042
-
-
- HY-N7741
-
-
- HY-N1388R
-
-
- HY-N6857R
-
-
- HY-107818
-
-
- HY-126477
-
-
- HY-W024365
-
-
- HY-119678
-
-
- HY-N7272R
-
-
- HY-N11286R
-
|
|
Structural Classification
Natural Products
Animals
Source classification
|
Others
|
|
Tridocosahexaenoylglycerol (Standard) is the analytical standard of Tridocosahexaenoylglycerol. This product is intended for research and analytical applications. Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases .
|
-
- HY-109506R
-
-
- HY-N0283
-
-
- HY-N6967
-
|
(-)-α-Bisabolol
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Apoptosis
|
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-N7515
-
-
- HY-N11020
-
-
- HY-N0307
-
-
- HY-122920
-
-
- HY-N0278A
-
-
- HY-120657
-
-
- HY-N0219R
-
-
- HY-113365
-
-
- HY-N2787
-
-
- HY-112234
-
-
- HY-119347R
-
-
- HY-N6869R
-
|
|
Structural Classification
Microorganisms
other families
Terpenoids
Source classification
Diterpenoids
Plants
|
Antibiotic
PPAR
Bacterial
Fungal
|
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-N1428R
-
-
- HY-N0594
-
-
- HY-N9481
-
-
- HY-N11728
-
-
- HY-N0088R
-
-
- HY-N1369R
-
-
- HY-Z0283R
-
-
- HY-N0401A
-
-
- HY-N6962
-
-
- HY-108485
-
-
- HY-N2877
-
-
- HY-N2199
-
-
- HY-126170
-
-
- HY-N12124
-
-
- HY-126477R
-
-
- HY-N2342R
-
-
- HY-N6967R
-
|
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Apoptosis
|
|
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-N8818
-
-
- HY-B1350A
-
-
- HY-W012974
-
-
- HY-59291
-
-
- HY-N1420
-
-
- HY-125130
-
-
- HY-N0930B
-
-
- HY-N13174
-
-
- HY-113421
-
|
Linoleic acid monoethanolamide
|
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
|
Cannabinoid Receptor
|
|
Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
|
-
- HY-N0307R
-
|
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Acanthopanax senticosus (Rupr. et Maxim.) Harms
Plants
Araliaceae
|
Bcl-2 Family
|
|
Ciwujianoside B (Standard) is the analytical standard of Ciwujianoside B. This product is intended for research and analytical applications. Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory .
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation .
|
-
- HY-14393
-
-
- HY-107825
-
-
- HY-117081
-
-
- HY-N2673
-
|
5-n-Heptadecylresorcinol; AR-C17
|
Structural Classification
Gramineae
Source classification
Secale cereale
Phenols
Polyphenols
Plants
|
Sirtuin
|
|
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity .
|
-
- HY-N0594R
-
|
|
Structural Classification
Iridoids
Terpenoids
Source classification
Rubiaceae
Plants
Morinda officinalis How
|
Interleukin Related
|
|
Deacetylasperulosidic Acid (Standard) is the analytical standard of Deacetylasperulosidic Acid. This product is intended for research and analytical applications. Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice . Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells .
|
-
- HY-N0058
-
-
- HY-N6715
-
-
- HY-N1940
-
-
- HY-N0028
-
-
- HY-N7545
-
|
|
Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
|
Antibiotic
Reverse Transcriptase
|
|
Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitory activity against HIV reverse transcriptase. In vitro studies have shown that Protorubradirin also inhibits Staphylococcus aureus strains and Streptococci. In infected mice, subcutaneous injection of Protorubradirin showed in vivo inhibitory efficacy against antibiotic-resistant Staphylococcus aureus strains. However, oral administration may result in a significant reduction in the activity of Protorubradirin, possibly due to faster cleavage of its C-nitroso sugar in the acidic gastric environment compared to Rubradirin .
|
-
- HY-N0028R
-
|
|
Structural Classification
Oleaceae
Simple Phenylpropanols
Source classification
Phenols
Polyphenols
Phenylpropanoids
Forsythia suspensa (Thunb.) Vahl
Plants
|
Others
|
|
Forsythiaside A (Standard) is the analytical standard of Forsythiaside A. This product is intended for research and analytical applications. Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice .
|
-
- HY-W024365R
-
|
|
Structural Classification
Monophenols
Source classification
Jatropha curcas Linn.
Phenols
Euphorbiaceae
Plants
|
PROTAC Linkers
|
|
3-tert-Butyl-4-methoxyphenol (Standard) is the analytical standard of 3-tert-Butyl-4-methoxyphenol. This product is intended for research and analytical applications. 3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system .
|
-
- HY-16561
-
Resveratrol
Maximum Cited Publications
94 Publications Verification
trans-Resveratrol; SRT501
|
Structural Classification
Classification of Application Fields
Anti-aging
Source classification
Vitis vinifera cv. Zalema
Plants
Vitaceae
Infection
Microorganisms
Functional Molecules
Sunscreen
Research of Health Products
Phenols
Polyphenols
Cosmetic Research
Inflammation/Immunology
Disease Research Fields
Cancer
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-161935
-
-
- HY-W001925
-
-
- HY-14393R
-
-
- HY-N6715R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Influenza Virus
Bacterial
Enterovirus
Photosystem II
|
|
Tenuazonic acid (Standard) is the analytical standard of Tenuazonic acid. This product is intended for research and analytical applications. Tenuazonic acid is a nonhost-selective mycotoxin belonging to the tetramic acids family. Tenuazonic acid inhibits protein biosynthesis on ribosomes by suppressing the release of new protein. Tenuazonic acid is acutely toxic, and oral LD50 is set between 81-186 mg/kg in rats and mice. Tenuazonic acid blocks electron transport beyond the primary quinone receptor (QA) by interacting with the D1 protein and is a photosystem II (PSII) inhibitor. In addition, Tenuazonic acid has antiviral effects on measles virus, enterovirus, respiratory virus and so on. Tenuazonic acid has an inhibitory effect on skin cancer .
|
-
- HY-N13866
-
|
|
Triterpenes
Structural Classification
Animals
Terpenoids
Source classification
|
Others
|
|
Cucumarioside A2-2 is a triterpene glycoside with antitumor activity. Cucumarioside A2-2 can induce mouse macrophage polarization toward the M1 phenotype. Cucumarioside A2-2 pretreated macrophages can effectively and selectively target and kill multiple types of cancer cells. Cucumarioside A2-2-induced M1 macrophages can effectively target and penetrate tumor tissues and improve the survival rate of mice in an allogeneic model. Exogenous activation of Cucumarioside A2-2 provides a useful model for the subsequent development of antitumor cell immunosuppression .
|
-
- HY-D0186R
-
|
|
Structural Classification
Natural Products
Immune System Disorder
Microorganisms
Source classification
Disease markers
Endogenous metabolite
|
Endogenous Metabolite
Thymidylate Synthase
|
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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- HY-N0394
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- HY-N1441
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- HY-B1941
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- HY-116330
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- HY-16561R
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trans-Resveratrol (Standard); SRT501 (Standard)
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Infection
Functional Molecules
Classification of Application Fields
Sunscreen
Anti-aging
Source classification
Research of Health Products
Cosmetic Research
Plants
Inflammation/Immunology
Disease Research Fields
Cancer
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IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
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Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-116330AR
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Structural Classification
Natural Products
Guttiferae
Source classification
Hyperlcurn perforatum L.
Plants
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TRP Channel
Calcium Channel
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Hyperforin (dicyclohexylammonium salt) (Standard) is the analytical standard of Hyperforin (dicyclohexylammonium salt). This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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- HY-N0058R
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Structural Classification
Ketones, Aldehydes, Acids
Source classification
Phenols
Polyphenols
Bowdichia virgilioides
Plants
Compositae
Endogenous metabolite
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HBV
Endogenous Metabolite
Apoptosis
Glucosidase
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4,5-Dicaffeoylquinic acid (Standard) is the analytical standard of 4,5-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
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- HY-N0976
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- HY-155156
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- HY-155157
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- HY-N1441R
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Flavonols
Structural Classification
Flavonoids
Saururaceae
Houttuynia cordata Thunb.
Source classification
Phenols
Polyphenols
Plants
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Mitochondrial Metabolism
PTEN
Autophagy
Bacterial
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Afzelin (Standard) is the analytical standard of Afzelin. This product is intended for research and analytical applications. Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin .
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- HY-151852
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Cardiovascular Disease
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
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9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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- HY-B1941R
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Monophenols
Source classification
Phenols
Endogenous metabolite
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Endogenous Metabolite
Apoptosis
DNA/RNA Synthesis
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4-tert-Octylphenol (Standard) is the analytical standard of 4-tert-Octylphenol. This product is intended for research and analytical applications. 4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology .
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- HY-N0092R
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Structural Classification
Natural Products
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
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Adenosine Receptor
Endogenous Metabolite
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Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR .
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation .
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes .
In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
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- HY-N6972
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- HY-W017113
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Structural Classification
Natural Products
Classification of Application Fields
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
Aryl Hydrocarbon Receptor
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2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
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- HY-14608R
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Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
Cardiovascular System Disorder
Cancer
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Endogenous Metabolite
iGluR
Ferroptosis
Apoptosis
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L-Glutamic acid (Standard) is the analytical standard of L-Glutamic acid. This product is intended for research and analytical applications. L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases .
IC50 & Target:DA .
In Vitro: L-Glutamic acid (120, 500, 750, 1000 mg/dL) can reduce the harmful effect of lithium on the embryonic development of Xenopus Xenopus .
L-Glutamic acid (2, 5, 10, 20 mM, 24-48 h) can induce neuroexcitotoxicity in neuroblastoma .
In Vivo: L-Glutamic acid (3 g/kg, subcutaneous injection) can promote excitotoxic degeneration of retinal ganglion cells in mice .
L-Glutamic acid (750 mg/kg, intraperitoneal injection) can reduce and inhibit oxidative stress induced by chlorpyrifos (CPF) in rats .
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- HY-N6972R
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Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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- HY-N0394R
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Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Amino acids
Endogenous metabolite
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Endogenous Metabolite
Ferroptosis
ROS Kinase
Keap1-Nrf2
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L-Cystine (Standard) is the analytical standard of L-Cystine. This product is intended for research and analytical applications. L-Cystine, the extracellular form of L-Cysteine (HY-Y0337), is a nutritionally dispensable semiessential sulfur-containing amino acid, occurring in proteins of plants and animals. L-Cystine induces Nrf2 protein elevation in a Keap1 (HY-P75897)-dependent manner and activates Nrf2 transcription factor. L-cystine can elicit cytoprotection by reducing ROS generation and protecting against oxidant- or doxorubicin-induced apoptosis. The reduced reabsorption of L-Cystine in renal tubules and its poor solubility in urine are the important causes of cystine precipitation and cystine crystal formation eventually leading to kidney stones. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and cystinosis
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- HY-B2176R
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Structural Classification
Alkaloids
Human Gut Microbiota Metabolites
Microorganisms
other families
Animals
Other Alkaloids
Source classification
Plants
Endogenous metabolite
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Endogenous Metabolite
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ATP (Standard) is the analytical standard of ATP. This product is intended for research and analytical applications. ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation .
In Vitro: ATP (5 mM; 1 hour) co-treatment with LPS (1 μg/mL) has a synergistic effect on the activation of the NLRP3 inflammasome in HGFs .
ATP (2 mM; 0.5-24 hours) induces secretion of IL-1β, KC and MIP-2 from BMDMs in a caspase-1 activation-dependent manner .
ATP promotes neutrophil chemotaxis in vitro .
In Vivo: ATP (50 mg/kg; i.p.) protects mice against bacterial infection in vivo .
ATP induces the secretion of IL-1β, KC and MIP-2 and neutrophils recruitment in vivo .
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- HY-N6871
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Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
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Bacterial
IKK
Ferroptosis
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Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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- HY-N2037
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- HY-N0469R
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Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
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Endogenous Metabolite
Virus Protease
HSV
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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- HY-B2167R
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Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endogenous metabolite
Cardiovascular System Disorder
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Endogenous Metabolite
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Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-109506S1
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DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
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- HY-109506S
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DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
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- HY-B1002S
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Oxolinic acid-d5 is the deuterium labeled Oxolinic acid. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice[1][2][3].
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- HY-113354S
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Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
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- HY-109506S3
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DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
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- HY-B0448S1
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Phenytoin- 15N2, 13C is the 13C and 15N labeled Phenytoin[1]. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[2][3].
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- HY-B1198S
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Piperonyl butoxide-d9 is the deuterium labeled Piperonyl butoxide.Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice .
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- HY-N1428S3
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Citric acid- 13C3 is the 13C labeled Citric acid[1]. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[2][3][4].
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- HY-124412S
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Paynantheine-d3 is a deuterium labeled Paynantheine. Paynantheine is an alkaloid that can be isolated from Mitragyna speciosa. Paynantheine can decrease alcohol intake in mice .
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- HY-D0195S
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Acesulfame-d4 potassiumis the deuterium labeledAcesulfame (potassium)(HY-D0195) . Acesulfame potassium is an artificial sweetener. Acesulfame potassium (long-term) affects cognitive functions, potentially via altering neuro-metabolic functions in mice .
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- HY-14393S
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Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
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- HY-B0534S1
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Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
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- HY-145119S
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GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
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- HY-109120S
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Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-B0534S
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Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
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- HY-N6608S
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Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
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- HY-109120S1
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Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-100442S
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Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
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- HY-100442S1
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Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
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- HY-109506S2
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(Rac)-DPPC-d6 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
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- HY-101064S2
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Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
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- HY-101064S3
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Fmoc-leucine-d10 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
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- HY-113354S1
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Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-109506S9
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DPPC-13C2 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
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- HY-N1428S6
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Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
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- HY-N9484S
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Menthofuran- 13C2 is 13C labeled Menthol (HY-N1369). Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca ++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice .
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- HY-17623S
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Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
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- HY-12678S
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Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
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- HY-119980S
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Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-113421S
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Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
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- HY-12678S1
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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- HY-16561S1
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Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
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- HY-16561S
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Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
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- HY-163816
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Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
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| Cat. No. |
Product Name |
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Classification |
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- HY-W001538
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SPRC
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Alkynes
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S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca 2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties .
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- HY-16361A
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CGP3466B; CGP3446 maleate; TCH346 maleate
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Alkynes
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Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease . Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD) . Omigapil (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-108039
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HE 3286; NE-3107
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Alkynes
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Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis . Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-151852
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Labeling and Fluorescence Imaging
Azide
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9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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- HY-118950
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Alkynes
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J 628 is an estrogen derivative used to study antifertility effects after sexual intercourse in mice, rats, and rabbits .
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- HY-120171
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Alkynes
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DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice . DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-150725C
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CpG ODNs
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ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
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- HY-B0892
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Benzenemethanol
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Preservatives
Solvents
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Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice .
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- HY-145721A
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GED-0301 sodium
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Antisense Oligonucleotides
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Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
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- HY-109506
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DPPC
5 Publications Verification
129Y83
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Phospholipids
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DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice .
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- HY-RS08425
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siRNAs
Pre-designed siRNA Sets
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MICAL1 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS08426
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siRNAs
Pre-designed siRNA Sets
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MICAL2 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS08427
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siRNAs
Pre-designed siRNA Sets
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MICAL3 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-156936
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Cationic Lipids
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RCB-02-4-8 is an ionizable cationic lipid that is used to form lipid nanoparticles (LNPs) to deliver mRNA. RCB-02-4-8 can improve the efficiency of lung transfection in mice .
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- HY-150725
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CpG ODNs
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ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
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- HY-145721
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GED-0301
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Antisense Oligonucleotides
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Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
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- HY-132579A
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RG6042 sodium; IONIS-HTTRx sodium
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Antisense Oligonucleotides
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Tominersen sodium is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen sodium can be used for the research of Huntington’s disease (HD) .
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- HY-154974
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Cationic Lipids
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LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model .
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- HY-13859
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L-FMAU
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Nucleosides and their Analogs
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Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
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- HY-148413
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ISIS 3521 sodium
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Antisense Oligonucleotides
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Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
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- HY-132579
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RG6042; IONIS-HTTRx
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Antisense Oligonucleotides
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Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD) .
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- HY-153834
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Aptamers
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GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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- HY-153834A
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Aptamers
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GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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- HY-160554
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Cationic Lipids
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C12-113 is a lipidoid delivery agent that can be used to transfect siRNA into cells. C12-113 can also be combined with other lipids to form lipid nanoparticles (LNPs) for the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice .
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- HY-150236
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Antisense Oligonucleotides
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FITC-labeled Tominersen (sodium) is the Tominersen labeled with FITC. Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
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- HY-157252
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Cationic Lipids
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CL4F8-6 is an ionizable cationic lipid with a pKa of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice .
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- HY-147080
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ARC1905
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Aptamers
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Avacincaptad pegol (ARC1905) sodium is a 40KDa PEG-conjugated aptamer. Avacincaptad pegol sodium targets complement factor 5 (C5), inhibits the cleavage of C5 into C5a and C5b, limits inflammatory stimulation and complement membrane attack complex (MAC), and is used to study age-related macular degeneration (AMD). Avacincaptad pegol sodium limits irregular cell apoptosis by targeting downstream factors in the complement cascade while preserving the early steps of the complement system. Avacincaptad pegol sodium treats Geographic atrophy (GA) mice .
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- HY-153808
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Adjuvant
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Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
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