Search Result
Results for "
DOR
" in MedChemExpress (MCE) Product Catalog:
32
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P1334A
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- HY-P1333
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
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-
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- HY-105343
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BW-180C
1 Publications Verification
[D-Ala2, D-Leu5]-Enkephalin; DADLE
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Opioid Receptor
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Neurological Disease
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BW-180C ([D-Ala2, D-Leu5]-Enkephalin; DADLE) is an δ opioid receptor (DOR) agonist, which belongs to the enkephalin family. Neuroprotective agent. BW-180C reversibly inhibits cellular transcription in neurons without causing cell injury .
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- HY-136208
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Opioid Receptor
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Neurological Disease
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TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
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- HY-162850
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- HY-162552
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Opioid Receptor
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Neurological Disease
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KOR/DOR agonist 2 is a KOR and DOR opioid receptors agonist with Ki values of 0.14 nM, and 0.93 nM, respectively. KOR/DOR agonist 2 shows significant antinociceptive effects. KOR/DOR agonist 2 penetrates the blood-brain barrier .
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- HY-P2669
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- HY-P10203
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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- HY-P1333A
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
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- HY-W283556
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Biochemical Assay Reagents
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Cancer
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DO2A-tert-butyl ester is a bifunctional chelator (BFC) that can be used for the coupling of peptides and radionuclides. DO2A-tert-butyl ester can be used in the development of radionuclide imaging tracers .
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- HY-114157
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DO-264
1 Publications Verification
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MAGL
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Neurological Disease
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DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
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- HY-N12992
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Others
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Others
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(3R)-3′,8-Dihydroxyvestitol (compound DO-9) is an isoflavonoid monomer that can be isolated from Dalbergia odorifera. I .
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- HY-W726767
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Biochemical Assay Reagents
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Others
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DO2Ais a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. DO2A can be used for conjugation of peptides and radionuclides.
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- HY-W250844A
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Biochemical Assay Reagents
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Others
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DO3A (trisodium)is a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. DO3A (trisodium) can be used for conjugation of peptides and radionuclides.
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- HY-108419
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JNK
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Cancer
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WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM .
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- HY-D1629
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Fluorescent Dye
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Others
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Calcium Orange AM is an intracellular calcium reporter. Specific fluorescence can be detected when free calcium binds to Calcium Orange AM (Ex/Em=549/576 nm). Calcium Orange AM does not enter the vacuoles and does not compartmentalize into acidic vesicles .
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- HY-W782081
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Biochemical Assay Reagents
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Others
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p-SCN-Bn-oxo-DO3Ais a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. p-SCN-Bn-oxo-DO3A can be used for conjugation of peptides and radionuclides.
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- HY-N8659
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Uzarigenin 3-β-sophoroside
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Others
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Others
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Uzarin is a steroid glycoside. Uzarin does not
inhibit cell proliferation or induce apoptosis .
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- HY-50683S
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c-Met/HGFR
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Cancer
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JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
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- HY-163975
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Glucosidase
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Cancer
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α-Glucosidase-IN-72 (compound 5i) is a 2,4-dichloro-N-phenylacetamide derivative and an α-glucosidase inhibitor (IC50: 6 μM). α-Glucosidase-IN-72 does not follow Lipinski's "rule of five" and does not induce cancer .
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- HY-145115
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Others
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Infection
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Adeninobananin, a negative control tool, does not show any inhibitory activity of the SARS Coronavirus helicase.
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- HY-123220
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Others
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Inflammation/Immunology
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S 1592 is a compound that possesses bronchodilating and antianaphylactic properties and does not affect gastrointestinal propulsion .
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- HY-P2021
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- HY-P1334
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- HY-P10672
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- HY-W782080
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Biochemical Assay Reagents
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Others
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p-NH2-Bn-oxo-DO3Ais a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. p-NH2-Bn-oxo-DO3A can be used for conjugation of peptides and radionuclides.
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- HY-103329
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MM22; Biotinylated N-arachidonoylethanolamine
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Cannabinoid Receptor
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Others
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b-AEA (MM22) is a biotinylated endocannabinoid analog with probe activity. b-AEA is able to accumulate intracellularly in a similar manner to the parent compound AEA. b-AEA does not interact with other components of the endocannabinoid system and therefore does not interfere with their function. b-AEA can be used to visualize the accumulation and intracellular distribution of endocannabinoids .
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- HY-115756
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Others
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Others
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4-Maleimidosalicylic acid is a polar maleimide, and does not suppress IL-2 production in JURKAT T cells .
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- HY-16560B
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(R)-Campathecin; (R)-(+)-Camptothecin; (R)-CPT
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Others
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Others
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(R)-Camptothecin is an enantiomer of Camptothecin (CPT), is inactive as an inhibitor of the DNA religation reaction and consequently do not poison Top1 .
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- HY-11051
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Opioid Receptor
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Inflammation/Immunology
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JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
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- HY-117771A
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DAGL
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Metabolic Disease
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DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
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- HY-139709
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- HY-139710
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- HY-122367
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Bacterial
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Neurological Disease
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Neoxaline is an alkaloid produced by Aspergillus japonicus. Neoxaline does not possess antimicrobial activities, but weakly stimulates the central nervous system .
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- HY-117818
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Antibiotic DC 116
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Antibiotic
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Cancer
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Sapurimycin is an antitumor antibiotic isolated from Streptomyces DO-116 and belongs to the capramycin family. Sapurimycin exhibits potent activity against Gram-positive bacteria and exhibits significant antitumor effects against leukemia P388 and sarcoma 180 in mouse models. In vitro studies have shown that Sapurimycin can induce single-strand breaks in supercoiled plasmid DNA .
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- HY-15615
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ONC201 isomer
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Others
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Others
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TIC10 isomer is the isomer of TIC10. TIC10 isomer does not possess the reported biological activity of inducing TRIAL expression.
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- HY-107744
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Opioid Receptor
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Neurological Disease
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Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence .
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- HY-157335
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- HY-B1485
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Opioid Receptor
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Neurological Disease
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Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .
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- HY-121548
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Others
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Infection
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Drimentine A is a terpenylated diketopiperazine originally isolated from Actinomycete bacteria.nlike Drimentine B and Drimentine C, Drimentine A does not have anticancer activity.
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- HY-137279
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Opioid Receptor
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Inflammation/Immunology
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Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier .
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- HY-B0019
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(Rac)-SENS-401 free base
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Others
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Neurological Disease
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Azasetron ((Rac)-SENS-401 free base) is an antiemetic drug with 5-HT3 receptor antagonist activity. Azasetron is often used as a preventive measure for postoperative nausea and vomiting or chemotherapy-induced nausea and vomiting. Azasetron does not impair neutrophil chemotaxis or phagocytosis and does not scavenge O(-)(2) or H(2)O(2) generated by cell-free systems .
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- HY-138887
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DMNG
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Others
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Others
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Decyl maltose neopentyl glycol (DMNG) is the neopentyl glycol detergent that does not disrupt the AlkB oligomeric state. AlkB is a nonheme di-iron alkane hydroxylase .
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- HY-P1854
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Amyloid-β
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Neurological Disease
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β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
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- HY-114990
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- HY-130538
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HDAC
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Cancer
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1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity .1-Naphthohydroxamic acid can induce tubulin acetylation .
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- HY-161539
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Opioid Receptor
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Neurological Disease
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KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
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- HY-10281
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Factor Xa
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Cardiovascular Disease
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YM-60828 is an FXa inhibitor with antithrombotic properties. In the rat arteriovenous shunt model, YM-60828 does not prolong coagulation time but reduces the levels of thrombin-antithrombin III complex (TAT) in a dose-dependent manner. YM-60828 exhibits only anti-FXa activity and does not show anti-thrombin activity, indicating that its antithrombotic effect is independent of thrombin. Therefore, the antithrombotic effect of YM-60828 can be monitored by TAT .
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- HY-P0233
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- HY-117765
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- HY-117771
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DO34
2 Publications Verification
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DAGL
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Metabolic Disease
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DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
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- HY-N1272
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Endogenous Metabolite
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Others
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Secaubryenol is a class of 3,4-secocycloartane triterpenes isolated from Coussarea macrophylla. Secaubryenol does not display any cytotoxic effect at a dose of 10 μg/mL .
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- HY-100815B
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(±)-AMPA
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iGluR
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Neurological Disease
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(RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors .
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- HY-P0233A
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Phospholipase
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Infection
Cancer
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Melittin TFA is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2 .
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- HY-100815D
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(±)-AMPA monohydrate
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iGluR
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Neurological Disease
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(RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors .
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- HY-122208
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Others
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Inflammation/Immunology
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SGA360 suppress inflammatory SAA1 signaling in an AHR-dependent manner through a mechanism that does not require AHR binding to its cognate response element (partial antagonist) .
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- HY-117200
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Nec-7
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Necroptosis
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Cancer
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Necrotatin-7 (Nec-7) is a potent necroptosis inhibitor with an EC50 of 10.6 μM. Necrotatin-7 does not inhibit recombinant RIP1 kinase .
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- HY-115731
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Desmethyltocopherol; DL-Tocol; rac-Tocol
|
Endogenous Metabolite
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Metabolic Disease
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(±)-Tocol is a synthetic vitamin E derivative.nlike (±)-α-tocopherol, (±)-tocol does not suppress retinol-induced erythrocyte hemolysis or increase microviscosity of rat liver phosphatidylcholine (PC) liposomes.
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- HY-122029
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Mitochondrial Metabolism
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Metabolic Disease
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BRD6897 is a mitochondrial content inducer. BRD6897 does not alter the percent of cytoplasmic area occupied by mitochondria, but instead, induces a striking increase in the electron density of existing mitochondria .
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- HY-137252
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Ivermectin Impurity G
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Parasite
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Infection
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22,23-Dihydroavermectin B1a aglycon is an acid degradation product produced by hydrolysis of the disaccharide unit of ivermectin. It can inhibit nematode larval development, but does not cause paralytic activity.
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- HY-141551
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Estrogen Receptor/ERR
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Cancer
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GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
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- HY-16639
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- HY-131443
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Phosphatase
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Others
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TRC-766 is a negative control of RTC-5 (TRC-382). TRC-766 binds protein phosphatase 2A (PP2A) and does not activate the phosphatase .
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- HY-137989
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Voriconazole oxynitride
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Fungal
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Infection
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Voriconazole N-oxide (Voriconazole oxynitride) is a potent antifungal agent. Voriconazole N-oxide has phototoxicity and photocarcinogenicity. Voriconazole N-oxide does not sensitize keratinocytes to ultraviolet B (UVB) .
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- HY-126198
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McN-3935
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Antibiotic
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Metabolic Disease
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Linogliride (MCN-3935) is an antidiabetic agent. Linogliride (100 μM) does not affect insulin secretion in the absence of glucose, but has a significant insulinotropic effect in the presence of 5.5 mM glucose .
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- HY-126198A
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McN-3935 fumarate
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Antibiotic
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Metabolic Disease
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Linogliride (MCN-3935) fumarate is an antidiabetic agent. Linogliride fumarate (100 μM) does not affect insulin secretion in the absence of glucose, but has a significant insulinotropic effect in the presence of 5.5 mM glucose .
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- HY-100815E
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(±)-AMPA hydrochloride
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iGluR
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Neurological Disease
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(RS)-AMPA ((±)-AMPA) hydrochloride is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
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- HY-13802
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SC-514
5 Publications Verification
GK 01140
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IKK
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Cancer
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SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
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- HY-U00441
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DPBQ
1 Publications Verification
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MDM-2/p53
Apoptosis
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Cancer
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DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells .
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- HY-N7091
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Others
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Metabolic Disease
Cancer
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Atrazine, a triazine herbicide, is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term .
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- HY-103348
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Boc-Asp(OMe)-FMK
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Caspase
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Inflammation/Immunology
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Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8 .
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- HY-141724
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PCSK9
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Cancer
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PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. PCSK9 ligand 1 does not affect PCSK9 function .
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- HY-107603
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iGluR
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Neurological Disease
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NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors .
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- HY-P99706
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AK 117
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CD47
Interleukin Related
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Cancer
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Ligufalimab (AK 117) is a humanized IgG4 anti-CD47 monoclonal antibody. Ligufalimab does not induce RBC hemagglutination, and induces phagocytosis. Ligufalimab shows anti-tumor activity .
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- HY-100815C
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(±)-AMPA hydrobromide
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iGluR
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Neurological Disease
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(RS)-AMPA ((±)-AMPA) hydrobromide is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
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- HY-P10008
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Cathepsin
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Cancer
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Cathepsin D/E Substrate, Fluorogenic, 11 amino acid peptide, is a selective substrate for cathepsins D and E. Cathepsin D/E Substrate, Fluorogenic does not act as a substrate for cathepsins B, H, or L .
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- HY-158195
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Others
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Cancer
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DPP23 exerts antitumor activity through ROS-mediated apoptosis in cancer cells, but does not play a role in healthy cells. DPP23 can up-regulate the expression of ATF4 .
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- HY-129207
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GHSR
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Endocrinology
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Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 μg/kg.
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- HY-N1745
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-
- HY-P3278
-
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Proton Pump
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Metabolic Disease
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Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
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- HY-123070
-
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Phospholipase
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Inflammation/Immunology
|
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ONO-RS-082 is an inhibitor of phospholipase A (PLA) . ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM, but does not inhibit PLC even at 100 μM .
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- HY-P5074
-
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GCGR
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Metabolic Disease
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GRPP (human) is a 30 amino acid Gcg-derived peptide. GRPP (human) causes slight increases in plasma insulin and decreases in plasma glucagon. GRPP (human) does not affect insulin secretion in rat islets .
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- HY-123154
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Others
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Others
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PDE10A-IN-4 (compound 38) is a compound used to inhibit schizophrenia. As a PDE10A inhibitor, it is less effective than placebo in inhibiting acute schizophrenia and does not show antipsychotic effect.
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- HY-118534A
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BRN-2209058 sodium
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Others
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Endocrinology
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Cyclobutyrol sodium is a potent choleretic agent. Cyclobutyrol sodium also inhibits biliary lipid secretion. Cyclobutyrol sodium induces choleretic is unrelated to bile acids. Cyclobutyrol sodium and bile acids do not compete for the hepatobiliar transport mechanisms[1]
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- HY-119874
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Pyruvate Kinase
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Inflammation/Immunology
Cancer
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Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent .
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- HY-152214
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Sirtuin
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Cancer
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SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor .
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- HY-110145
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TRP Channel
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Cancer
|
|
MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis .
|
-
- HY-W373206
-
|
|
Others
|
Metabolic Disease
|
|
Triampizine is an effective gastric antisecretory agent. Triampizine does not have the side effects commonly associated with anticholinergic agents. Triampizine may react with the excipient magnesium stearate. Triampizine can be used in the research of hyperacidity .
|
-
- HY-P10210
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Paenilagicin is a Gram-positive active antibiotic with a unique diphosphorylated prenyl binding mechanism that does not induce drug resistance. Paenilagicin exhibits a MIC value of 2 μg/mL against multidrug-resistant Gram-positive bacteria .
|
-
- HY-122370A
-
|
|
Aurora Kinase
|
Cancer
|
|
Tripolin B is an ATP-competitive Aurora kinase inhibitor with IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. Tripolin B does not inhibit Aurora kinase in cells .
|
-
- HY-112715
-
|
|
ATP Synthase
|
Cardiovascular Disease
|
|
ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels .
|
-
- HY-P2222
-
-
- HY-136194
-
-
- HY-136195
-
-
- HY-P3278A
-
|
|
Proton Pump
|
Metabolic Disease
|
|
Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
- HY-D0333
-
|
Sirius Red
|
Amyloid-β
|
Others
|
|
Direct Red 80 (Sirius Red) is a polyazo dye used principally in staining methods for collagen and amyloid. Direct Red 80 does not release benzidine upon degradation and is safer than many traditional direct dyes .
|
-
- HY-P0190A
-
|
|
Potassium Channel
|
Others
|
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .
|
-
- HY-134340
-
|
8-(4-Methoxyphenylthio)-2'-O-Me-cAMP
|
Others
|
Others
|
|
8-pMeOPT-2'-O-Me-cAMP is an analogue of the signal molecule cAMP and a potent stimulator of exchange factors activated by cAMP (Epac), while it doesn't activate PKA as cAMP does .
|
-
- HY-119018
-
|
|
Others
|
Inflammation/Immunology
|
|
AHR-6293 is an orally effective and potent anti-inflammatory agent. AHR-6293 has a better anti-inflammatory effect than AHR-5850, but does not have the activity of inhibiting platelet aggregation .
|
-
- HY-15451
-
MDA 19
1 Publications Verification
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
|
-
- HY-B1410
-
|
MP-328
|
Others
|
Others
Cancer
|
|
Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal .
|
-
- HY-128918
-
|
|
HDAC
|
Cancer
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM. SIS17 inhibits the demyristoylation of serine hydroxymethyltransferase 2, a substrate of HDAC 11, but does not inhibit other HDACs .
|
-
- HY-14406A
-
|
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent .
|
-
- HY-131015
-
|
|
Others
|
Others
|
|
HaXS8 is a dimerizer that can promote a covalent and irreversible intracellular dimerization of HaloTag and SNAP-tagged proteins of interest. HaXS8 does not interfere with PI3K/mTOR signaling .
|
-
- HY-107621
-
|
|
MEK
|
Cancer
|
|
U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM .
|
-
- HY-155941
-
|
|
Potassium Channel
|
Neurological Disease
|
|
5-Hydroxydecanoic acid (5-HD） is a KATP channel antagonist，which has the effect of blocking the K KATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic KATP channels .
|
-
- HY-110335
-
|
|
ROCK
|
Cancer
|
|
OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
|
-
- HY-16658B
-
|
Z-VAD(OH)-FMK
|
Caspase
Apoptosis
|
Cancer
|
|
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM .
|
-
- HY-112554
-
|
|
Others
|
Others
|
|
PDM11 is a derivative of antioxidant resveratrol. PDM11 do not exhibit any significant protective effect against oxidation of linoleate micelles initiated by radiolysis-generated hydroxyl radicals. PDM11 is inactive in resveratrol activity assays .
|
-
- 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-N7091S2
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
Atrazine-d5 is deuterium labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
- HY-P2222A
-
-
- HY-112543
-
|
|
Influenza Virus
|
Infection
|
|
S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV) .
|
-
- HY-N7091S
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
Atrazine- 15N is the 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
- HY-123604A
-
|
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .
|
-
- HY-149258
-
-
- HY-W717329
-
|
|
Aminopeptidase
|
Cardiovascular Disease
|
|
EC33 is a selective aminopeptidase A (APA) inhibitor. EC33 blocks the pressor response of exogenous Ang II. EC33 does not cross the blood-brain barrier. EC33 has the potential for salt-dependent model of hypertension research .
|
-
- HY-134451
-
|
DEUP
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Diethylumbelliferyl phosphate (DEUP), a selective and potent inhibitor of cholesterol esterase, does not inhibit protein kinase activity A in vitro, and it effectively disrupts steroidogenesis by blocking the transport of cholesterol into the mitochondria of steroidogenic cells, with an IC50 of 11.6 μM, potentially limiting dietary cholesterol absorption.
|
-
- HY-18963
-
|
RG-14355
|
EGFR
|
Cancer
|
|
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .
|
-
- HY-123604
-
TH1834
1 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .
|
-
- HY-120951
-
|
|
Endonuclease
|
Cancer
|
|
PFM39, a Mirin analog, is a potent and selective MRE11 exonuclease inhibitor. PFM39 inhibits phosphate rotation for dsDNA exonuclease activity. PFM39 does not inhibit TmMre11 or human MRE11/MRN endonuclease activity .
|
-
- HY-111014
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum Ca 2+release but does not block the β-receptor.VK-II-36 inhibits triggered activities evoked by both early and delayed after depolarizations .
|
-
- HY-133787
-
|
|
Drug Metabolite
|
Infection
|
|
Levofloxacin N-oxide is a minor metabolite of Levofloxacin (HY-B0330). Levofloxacin N-oxide does not exhibit significantly genotoxic risks. Levofloxacin is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria .
|
-
- HY-125143
-
|
|
MAGL
|
Metabolic Disease
|
|
ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122 .
|
-
- HY-153540
-
|
|
Others
|
Others
|
|
AP-C4 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.2. AP-C3 does not inhibit cGKII-dependent anion secretion .
|
-
- HY-10250A
-
|
TCN-P sodium
|
ATP Synthase
|
Metabolic Disease
Cancer
|
|
Triciribine phosphate sodium inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate sodium also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity .
|
-
- HY-N7091R
-
|
|
Others
|
Metabolic Disease
|
|
Atrazine (Standard) is the analytical standard of Atrazine. This product is intended for research and analytical applications. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term .
|
-
- HY-N6861
-
|
|
Apoptosis
|
Cancer
|
|
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells .
|
-
- HY-110249
-
CINPA1
1 Publications Verification
|
Constitutive Androstane Receptor
|
Metabolic Disease
|
|
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
|
-
- HY-100444
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 free base does not affect the phosphorylation of Smad2 .
|
-
- HY-P4114
-
|
|
HIV
|
Others
|
|
TAT-NSF700scr consists the intact TAT domain and glycine linker, followed by the NSF amino acids in a random order. TAT-NSF700scr is used as a control peptide that does not inhibit SNAREmediated exocytosis .
|
-
- HY-B1978S
-
|
|
Fungal
Reactive Oxygen Species
|
Infection
|
|
Iprodione-d5 is the deuterium labeled Iprodione[1]. Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective[2].
|
-
- HY-14751
-
|
SCH619734
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-114405
-
|
|
PROTACs
p38 MAPK
Autophagy
|
Cancer
|
|
SJFδ is a 10-atom linker PROTAC based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ .
|
-
- HY-P0190
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels .
|
-
- HY-18832
-
|
|
Others
|
Cancer
|
|
AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf .
|
-
- HY-142619
-
|
|
Bacterial
|
Infection
|
|
TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk. TP0586352 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-14751A
-
|
SCH619734 hydrochloride
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-16436
-
|
SCH619734 hydrochloride hydrate
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .
|
-
- HY-10250
-
|
TCN-P
|
ATP Synthase
|
Metabolic Disease
Cancer
|
|
Triciribine phosphate (TCN-P) inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity .
|
-
- HY-D2182
-
|
|
Fluorescent Dye
|
Others
|
|
Preactivated PE-Cy5 Maleimide is a sulfhydryl reactive dye that reacts with free sulfhydryl groups on proteins. Preactivated APC-Cy5.5 Maleimide binds easily to proteins or antibodies, and does not change the spectral characteristics of APC-Cy/YF after activation.
|
-
- HY-131842
-
|
N6-Benzyladenosine-3',5'-cyclic monophosphate
|
PKA
|
Cancer
|
|
6-Bn-cAMP is a site-selective activator of cAMP-dependent protein kinase (PKA) which does not activate Epac. 6-Bn-cAMP increases hydrolytic stability against PDE, esterases, amidases and considerably higher membrane permeability compared to cAMP .
|
-
- HY-14833
-
|
TP300
|
Topoisomerase
|
Cancer
|
|
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
|
-
- HY-124257
-
|
D-Citronellol; (R)-(+)-β-Citronellol
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
(R)-Citronellol (D-Citronellol) is an alcoholic monoterpene found in geranium essential oil. (R)-Citronellol inhibits degranulation of mast cells and does not affect caffeine bitterness perception. (R)-Citronellol can be used in decorative cosmetics, toiletries as well as in non-cosmetic products .
|
-
- HY-142981
-
|
DODA
|
Liposome
|
Others
|
|
Dioctadecylamine (DODA) is a secondary amine that has been shown to self-organize in plate-like structures in aqueous solution. Dioctadecylamine exhibits sufficiently hydrophobic properties of nanoparticles and good dispersibility in nonpolar solvent. Dioctadecylamine does not form a monolayer above pH 3.9 .
|
-
- HY-149810
-
|
|
Bacterial
Parasite
|
Infection
|
|
AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-P5786
-
-
- HY-D2180
-
|
|
Fluorescent Dye
|
Others
|
|
Preactivated APC-Cy5.5 Maleimide is a sulfhydryl reactive dye that reacts with free sulfhydryl groups on proteins. Preactivated APC-Cy5.5 Maleimide binds easily to proteins or antibodies, and does not change the spectral characteristics of APC-Cy/YF after activation.
|
-
- HY-121256
-
|
|
Thymidylate Synthase
Antifolate
Dihydrofolate reductase (DHFR)
|
Others
|
|
Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents .
|
-
- HY-135238
-
|
PD-117302
|
Others
|
Others
|
|
(rel)-RSD 921 (PD-117302) is a κ agonist that is more sensitive to its initial food-inducing effect in obese and lean Zucker rats, but ultimately reduces food intake. The compound does not enhance food intake more in obese Zucker rats than in lean rats.
|
-
- HY-128579
-
|
|
Histone Methyltransferase
|
Cancer
|
|
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity .
|
-
- HY-116304
-
1G244
3 Publications Verification
|
Dipeptidyl Peptidase
Apoptosis
|
Cancer
|
|
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects .
|
-
- HY-110114
-
|
|
Others
|
Others
|
|
Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ .
|
-
- HY-155909
-
|
mPEG-SC (MW 3400); mPEG-Succinimidyl ester (MW 3400)
|
Biochemical Assay Reagents
|
Others
|
|
m-PEG-NHS ester (MW 3400) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-155909A
-
|
mPEG-SC (MW 1000); mPEG-Succinimidyl ester (MW 1000)
|
Biochemical Assay Reagents
|
Others
|
|
m-PEG-NHS ester (MW 1000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-155909B
-
|
mPEG-SC (MW 550); mPEG-Succinimidyl ester (MW 550)
|
Biochemical Assay Reagents
|
Others
|
|
m-PEG-NHS ester (MW 550) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-155909C
-
|
mPEG-SC (MW 350); mPEG-Succinimidyl ester (MW 350)
|
Biochemical Assay Reagents
|
Others
|
|
m-PEG-NHS ester (MW 350) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-W591424
-
|
mPEG-SC (MW 2000); mPEG-Succinimidyl ester (MW 2000)
|
Biochemical Assay Reagents
|
Others
|
|
m-PEG-NHS ester (MW 2000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-107626
-
|
|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 does not exhibits significant activity for MCHR2. ATC0065 has anxiolytic and antidepressant activities .
|
-
- HY-163918
-
|
|
Others
|
Cancer
|
|
N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells .
|
-
- HY-163895
-
|
|
Fluorescent Dye
Opioid Receptor
|
Neurological Disease
|
|
δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception .
|
-
- HY-131589
-
|
Atenolol acid
|
Endogenous Metabolite
|
Others
|
|
Metoprolol acid (Atenolol acid) is a urinary metabolite with no pharmacological activity. Metoprolol acid does not exert its pharmacological effects in vivo. Metoprolol acid can be detected by solid phase extraction and reversed phase high performance liquid chromatography. The analysis of metoprolol acid requires specific conditions, such as the use of fluorescence detection and specific eluents .
|
-
- HY-12290
-
|
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
|
-
- HY-126326
-
|
|
Epoxide Hydrolase
|
Metabolic Disease
|
|
SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH .
|
-
- HY-136172
-
ESI-08
1 Publications Verification
|
Ras
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation .
|
-
- HY-19384
-
|
E 6087
|
COX
|
Inflammation/Immunology
|
|
Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2).?Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models .
|
-
- HY-N8278
-
|
|
Thrombin
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Dermatan sulphate sodium is a glycosaminoglycan and thrombin inactivator with antithrombotic activity. Dermatan sulphate sodium selectively catalyzes the inactivation of thrombin by heparin cofactor II and does not interact with antithrombin III. Dermatan sulphate sodium is highly bioavailable and also reduces Bleomycin (HY-108345)-induced pulmonary fibrosis damage .
|
-
- HY-157745
-
|
mPEG-SC (MW 40000); mPEG-Succinimidyl ester (MW 40000)
|
Biochemical Assay Reagents
|
Others
|
|
m-PEG-NHS ester (MW 40000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects .
|
-
- HY-113960
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1 .
|
-
- HY-19747
-
HPOB
3 Publications Verification
|
HDAC
Apoptosis
|
Cancer
|
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
|
-
- HY-10403
-
-
- HY-W127739
-
|
Zinc ethylene-1, 2-bisdithiocarbamate
|
Biochemical Assay Reagents
|
Others
|
|
Zineb is an agricultural fungicide of the dithiocarbamate class. Its toxicity is relatively low, and there is little evidence of human harm from exposure. Oxidative stress is one of the main factors contributing to diseases caused by Zineb. Zineb does not alter the activity of any superoxide dismutase enzymes. Catalase (CAT) activity was reduced only by Zineb.
|
-
- HY-149811
-
|
|
Bacterial
Parasite
|
Infection
|
|
Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-149812
-
|
|
Bacterial
Parasite
|
Infection
|
|
Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-156736
-
|
|
17β-HSD
|
Cancer
|
|
HSD17B13-IN-3 (compound 2) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor. HSD17B13-IN-3 does not have cell experimental activity .
|
-
- HY-113628
-
|
VML-530
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
ABT-080 is an orally active inhibitor of leukotriene biosynthesis. ABT-080 simultaneously blocks the leukotriene pathways leading to the synthesis of LTB4 and LTC4, but does not inhibit PGH2 biosynthesis. ABT-080 can block bronchoconstriction and be used in the research of asthma and related inflammations
|
-
- HY-14157
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms .
|
-
- HY-14157A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms .
|
-
- HY-116211
-
|
WIN-25978
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mouse brain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
|
-
- HY-13642
-
|
N-Phthalyl-L-tryptophan
|
DNA Methyltransferase
|
Cancer
|
|
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .
|
-
- HY-101096
-
|
MK-8998; CX-8998; JZP385
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-110150
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
|
-
- HY-109785A
-
|
|
Bacterial
|
Infection
|
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-N8537
-
|
|
Fungal
|
Infection
|
|
Enfumafungin, a triterpene glycoside, is isolated from extracts derived from fungus Hormonema carpetanum. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis .
|
-
- HY-N7091S1
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
Atrazine- 13C3, 15N3 is the 13C-labeled and 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
- HY-151691
-
|
|
ADC Linker
|
Others
|
|
Trisulfo-Cy3 Methyltetrazine is a click chemistry reagent containing an methyltetrazine group. Methyltetrazine-activated Cy3 probe reacts with TCO-containing compounds via an Inverse-Electron-Demand Diels-Alder reaction to form a stable covalent bond and does not require Cu-catalyst or elevated temperatures .
|
-
- HY-149919
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 23 is an antimalarial benzimidazole with IC50s of 0.08 μM and 0.10 μM for PfNF54 and PfK1, respectively. Antimalarial agent 23 has potent β-hematin inhibition activity. Antimalarial agent 23 does not directly inhibit the conversion of heme to hemozoin .
|
-
- HY-126224
-
|
|
Others
|
Others
|
|
Driselase, Basidiomycetes sp, a complex mixt. of wall-digesting enzymes, is a specific commercial fungal protoplasting enzyme preparation. Driselase is by far the most potent of the enzymes tested for polysaccharide digestion and greatly increases both tensile and indentation compliances, yet it does not induce wall creep, even after 6 h of digestion .
|
-
- HY-108058A
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research .
|
-
- HY-157068
-
|
|
Ferroptosis
|
Cancer
|
|
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
|
-
- HY-14356
-
-
- HY-116893
-
|
|
Others
|
Cancer
|
|
Diethyl bipy55'DC is an inhibitor of collagen proline 4-hydroxylases (CP4Hs) with antifibrotic and anti-metastatic activities. Diethyl bipy55'DC can inhibit CP4H activity in cultured cells at concentrations that do not cause iron deficiency .
|
-
- HY-B1410R
-
|
|
Others
|
Others
Cancer
|
|
Ioversol (Standard) is the analytical standard of Ioversol. This product is intended for research and analytical applications. Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal [4].
|
-
- HY-17491
-
|
RU 43-715; Sandoz-43-715
|
Others
|
Inflammation/Immunology
|
|
Proquazone (RU 43-715) is a chemically distinctive non-steroidal anti-inflammatory agent (NSAID). unlike most other NSAIDs, Proquazone does not have a free acid group in its structure. Proquazone may inhibit or arrest progression of bone erosions. Proquazone is an orally active anti-inflammatory, analgesic and anti-pyretic agent .
|
-
- HY-13044
-
-
- HY-13521
-
|
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-111759
-
|
7-CN-7-C-Ino
|
PKA
Parasite
|
Infection
|
|
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity .
|
-
- HY-12290A
-
|
RGDS peptide TFA; Fibronectin tetrapeptide TFA
|
Integrin
|
Inflammation/Immunology
|
|
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1 .
|
-
- HY-13521A
-
|
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 hydrochloride is a selective inhibitor of?TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with?IC50s?of 129 nM and 47 nM for?ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-P1136B
-
-
- HY-136658
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects .
|
-
- HY-100536
-
|
|
Wnt
|
Cancer
|
|
IWP-3 is an potent inhibitor of Wnt production with an IC50 of 40 nM. IWP-3 inhibits Porcupine (Porcn) function thereby blocking palmitoylation of Wnt proteins. IWP-3 inhibits CK1γ3 and CK1ε only moderately and does not inhibit CK1α .
|
-
- HY-152108
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
|
-
- HY-P5422
-
|
|
Calcium Channel
|
Others
|
|
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
|
-
- 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-W685943
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Heptaminol is a fatty amine with pressor properties and a potential antihypotension agent. Heptaminol is also a competitive inhibitor of norepinephrine uptake and an inhibitor of nicotine-induced catecholamine release (IC50: 650 μM). Heptaminol does not inhibit norepinephrine release induced by 59 mM K + but rather inhibits high-affinity Na +-dependent norepinephrine uptake .
|
-
- HY-120547
-
|
|
Others
|
Neurological Disease
Metabolic Disease
|
|
UCB-11056 is a modulator of cyclic AMP generation. UCB-11056 can rapidly increase cyclic AMP levels in the rat brain in vivo and potentiate stimulated cyclic AMP formation in vitro. UCB-11056 does not stimulate cAMP formation on its own. UCB-11056 is a potential nootropic drug .
|
-
- HY-135222
-
|
5-Methoxy-6-methyl-2-aminoindan hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
MMAI (5-Methoxy-6-methyl-2-aminoindan) hydrochloride is a selective serotonin releaser that does not produce psychoactive or hallucinogenic effects in the context of drug discrimination in rats. MMAI hydrochloride induces a behavioral syndrome in rats, including hypokinesia with freezing, spinning, Straub tail, flat posture, and reduced sleep time .
|
-
- HY-P10536
-
|
|
Bacterial
|
Infection
|
|
Temporin SHF is a broad-spectrum antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria and yeasts, but does not have hemolytic activity. Temporin SHF disrupts the acyl chain stacking of anionic lipid bilayers, leading to cracks and disintegration of microbial membranes. Temporin SHF can be used in the development of antimicrobial drugs .
|
-
- HY-138222
-
|
WHI-P131 hydrochloride; Jak3 inhibitor I hydrochloride
|
JAK
|
Cancer
|
|
JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3 inhibitor (Ki=2.3 μM). JANEX-1 hydrochloride shows potent JAK3 inhibitory activity (IC50=78 μM), does not inhibit JAK1 and JAK2 .
|
-
- HY-121700
-
|
|
5 alpha Reductase
|
Others
|
|
L-751788 is a selective inhibitor of type I of 5α-reductase. L-751788 does not have a significant impact on the differentiation of the external genitalia in animals. When administered orally to pregnant rhesus monkeys, L-751788 (2, 10 mg/kg) did not cause abnormalities in fetal external genitalia .
|
-
- HY-15451R
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 (Standard) is the analytical standard of MDA 19. This product is intended for research and analytical applications. MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
|
-
- HY-W322573
-
|
|
Others
|
Inflammation/Immunology
|
|
(R)-Ketoprofen is an orally active nonsteroidal anti-inflammatory drug (NSAID) with analgesic properties. (R)-Ketoprofen does not significantly amplify the increase of inflammatory cytokines (such as tumor necrosis factor (TNF) and interleukin-1 (IL-1)) induced by LPS, but it can inhibit the anti-inflammatory activity of (S)-Ketoprofen .
|
-
- HY-19517
-
|
|
Others
|
Cardiovascular Disease
|
|
R1663 is a factor Xa inhibitor with anticoagulant activity. R1663 does not affect bleeding time. The pharmacodynamic effects (such as inhibition of thrombin generation) and plasma concentrations of R1663 are dose-dependent. R1663 prolongs clotting time in a concentration-dependent manner and inhibits the peak height of thrombin generation and endogenous thrombin potential .
|
-
- HY-15643
-
|
|
TNF Receptor
Potassium Channel
|
Cancer
|
|
LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
|
-
- HY-15508
-
JANEX-1
4 Publications Verification
WHI-P131; Jak3 inhibitor I
|
JAK
|
Cancer
|
|
JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
|
-
- HY-10439
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX .
|
-
- HY-15643A
-
|
|
TNF Receptor
Potassium Channel
|
Cancer
|
|
LY 303511 hydrochloride is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
|
-
- HY-111501
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .
|
-
- HY-12150
-
CCMI
1 Publications Verification
AVL-3288; UCI-4083
|
nAChR
|
Neurological Disease
|
|
CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
|
-
- HY-122051
-
AC1903
1 Publications Verification
|
TRP Channel
|
Metabolic Disease
|
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
|
-
- HY-P1136C
-
-
- HY-126972A
-
|
|
RAD51
|
Cancer
|
|
RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC50 of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC50 of 3.0 μM) .
|
-
- HY-111226
-
GSK5182
2 Publications Verification
|
Estrogen Receptor/ERR
Reactive Oxygen Species
|
Cardiovascular Disease
Cancer
|
|
GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC) .
|
-
- HY-137457
-
|
IDX-1197
|
PARP
|
Cancer
|
|
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research .
|
-
- HY-139308
-
T0467
1 Publications Verification
|
PINK1/Parkin
Mitochondrial Metabolism
|
Neurological Disease
|
|
T0467 activates parkin mitochondrial translocation in a PINK1-dependent manner in vitro. T0467 do not induce mitochondrial accumulation of PINK1in dopaminergic neurons. T0467 is a potential compound for PINK1-Parkin signaling activation, and can be used for parkinson's disease and related disorders research .
|
-
- HY-114252
-
|
|
Na+/K+ ATPase
|
Cardiovascular Disease
|
|
Strophanthidin is a naturally available cardiac glycoside . Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal . Strophanthidin increases both diastolic and systolic intracellular Ca 2+ concentration .
|
-
- HY-146025
-
|
|
Others
|
Cancer
|
|
Antitumor agent-F10 (Compound F10) is a camptothecin derivative. Antitumor agent-F10 is an orally–bioavailable and potent antitumor agent. Antitumor agent-F10 displays lower acute toxicity than SN-38 does and the solubility of F10 reached 9.86 μg/mL .
|
-
- HY-P3463
-
|
GLP-1 (human)
|
GCGR
|
Metabolic Disease
Inflammation/Immunology
|
|
Beinaglutide is a human GLP-1 polypeptide that shares almost 100% homology with human GLP-1 (7–36). Beinaglutide displays does-dependent effects in glycemic control, inhibiting food intake and gastric empty and promoting weight loss. Beinaglutide has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH) .
|
-
- HY-114785
-
|
|
MMP
|
Cancer
|
|
BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects .
|
-
- HY-10131
-
|
|
Caspase
|
Others
|
|
Procaspase-3/6 activator 1 (compound 1541) is a highly specific and robust activator of executioner procaspases-3 and -6, with EC50 values of 2.4 ± 0.2 and 2.8 ± 0.3 μM, respectively. Procaspase-3/6 activator 1 does not activate procaspases-1 or -7 .
|
-
- HY-149665
-
|
|
DGK
|
Cancer
|
|
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
|
-
- HY-N12540
-
|
MGDG
|
Others
|
Others
|
|
Monogalactosyldiacylglycerol (MGDG) is a polar lipid that does not form a bilayer and is found, for example, in the chloroplast thylakoid of aerobic photosynthetic organisms. Monogalactosyldiacylglycerol lacks charge and is highly unsaturated, which provides a fluid environment that facilitates the diffusion process of electron transfer in photosynthesis and may be used in the packaging of natural proteins. The galactolipid Monogalactosyldiacylglycerol has anti-inflammatory effects in vivo ..
|
-
- HY-147071
-
|
DAPE
|
Liposome
|
Metabolic Disease
|
|
1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine (DAPE) is a phospholipid phosphatidylethanolamine. Unlike other phospholipid phosphatidylethanolamines, 1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine has no significant effect on protein phosphatase PP2A activity and does not inhibit insulin-stimulated GLUT4 translocation .
|
-
- 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 .
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-
- HY-111180
-
|
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Endogenous Metabolite
|
Metabolic Disease
|
|
ML-262 is an inhibitor of hepatic lipid droplet formation (IC50=6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease.1 ML-262 does not induce cytotoxicity (up to 33 μM) or inhibit fatty acid uptake (up to 50 μM).
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-
- HY-19111
-
|
TIBO-R 82150
|
HIV
Reverse Transcriptase
|
Infection
|
|
R-82150 (TIBO-R 82150) is an HIV-1 reverse transcriptase inhibitor that blocks the reverse transcription of viral RNA by binding to the non-substrate binding site of reverse transcriptase, thereby inhibiting viral replication. R-82150 does not inhibit the replication of HIV-2, other RNA viruses, and DNA viruses .
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-
- HY-15643B
-
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TNF Receptor
Potassium Channel
|
Cancer
|
|
LY 303511 dihydrochloride is a structural analogue of LY294002. LY 303511 dihydrochloride does not inhibit PI3K. LY 303511 dihydrochloride enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY 303511 dihydrochloride reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
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-
- HY-107626A
-
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|
MCHR1 (GPR24)
5-HT Receptor
|
Neurological Disease
|
|
ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities .
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-
- HY-159895
-
|
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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 .
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-
- HY-14751R
-
|
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
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-
- HY-15290
-
AIM-100
3 Publications Verification
|
Ack1
|
Cancer
|
|
AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect .
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-
- HY-100360
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
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-
- HY-129056
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia . Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion .
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-
- 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 .
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-
- HY-100360A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-145287
-
|
|
DNA/RNA Synthesis
Parasite
|
Infection
|
|
S-MGB-234 is a minor groove binder of Animal African Trypanosomiasis (AAT). S-MGB-234 displays excellent in vitro activities against the principal causative organisms of AAT; Trypanosoma congolense, and Trypanosoma vivax. S-MGB-234 does not show cross-resistance with the current diamidine agents and are not internalized via the transporters used by diamidines .
|
-
- HY-103347
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia .
|
-
- HY-103381
-
|
|
CDK
GSK-3
|
Cancer
|
|
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways .
|
-
- HY-150502
-
|
pSAT
|
Biochemical Assay Reagents
|
Others
|
|
Poly(styrenyl acetal trehalose) (pSAT) is composed of trehalose side chains linked to a polystyrene backbone via acetals. Poly(styrenyl acetal trehalose) stabilizes a variety of proteins and enzymes against fluctuations in temperature, and does not trigger the innate immune response. Poly(styrenyl acetal trehalose) can be used in synthesis of protein-polymer conjugates for reduced renal clearance of the biomolecule .
|
-
- HY-160045
-
|
|
Cholecystokinin Receptor
|
Cancer
|
|
AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
|
-
- HY-116051
-
|
16,16-Dimethyl-PGF2α
|
Others
|
Cardiovascular Disease
|
|
16,16-Dimethylprostaglandin F2α (16,16-Dimethyl-PGF2α) is a potent analog of PGF2α (HY-12956), which exhibits similar binding potency as PGF2α does. 16,16-Dimethylprostaglandin F2α serves as a bronchoconstrictor .
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-
- HY-145522
-
|
MEM; 1,3-Myristin-2-Eicosapentaenoin; 14:0/20:5/14:0-TG
|
Others
|
Metabolic Disease
|
|
1,3-Dimyristoyl-2-eicosapentaenoyl glycerol (MEM) is a triacylglycerol that contains myristic acid (HY-N2041) at the sn-1 and sn-3 positions and eicosapentaenoic acid at the sn-2 position. The myristoyl groups in MEM do not affect the oxidative stability of eicosapentaenoic acid (EPA) during long-term storage at 25°C.
|
-
- HY-163742
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-22 (compound 4), a hydrolysable tannin, is a potent SARS-CoV-2 main protease (Mpro) inhibitor with an IC50 value of 1.2 µg/mL. SARS-CoV-2 Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
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-
- HY-P10640
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
[Sar1,Thr8]-Angiotensin II is a potent angiotensin II antagonist. [Sar1,Thr8]-Angiotensin II does not alter cardiac performance. [Sar1,Thr8]-Angiotensin II might be safe for patients with cardiac disease .
|
-
![[Sar1,Thr8]-Angiotensin II](//file.medchemexpress.eu/product_pic/hy-p10640.gif)
- HY-19917
-
|
|
Others
|
Neurological Disease
|
|
JNJ-39220675 is a selective and brain-penetrating histamine H3 receptor antagonist with activity in regulating alcohol stimulation and reward. JNJ-39220675 is effective in reducing alcohol intake and preference in alcohol-preferring rats. JNJ-39220675 does not affect the ataxic effects of alcohol, the rate of alcohol elimination, or alcohol-induced nucleocapsid dopamine release .
|
-
- HY-W012264
-
|
3-Methoxy-L-tyrosine monohydrate; 3-O-Methyl-L-DOPA monohydrate
|
Others
|
Neurological Disease
|
|
3-O-Methyldopa monohydrate (3-Methoxy-L-tyrosine monohydrate) is a significant metabolite of L-DOPA produced through the action of catechol O-methyltransferase (COMT). Unlike its precursor, 3-O-Methyldopa does not serve as a substrate or inhibitor of L-amino acid decarboxylase activity. Additionally, the inhibition of COMT can amplify the anti-Parkinson effects of L-DOPA.
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-
- HY-118222
-
|
|
Others
|
Others
|
|
KBR 2822 is an esterase inhibitor used to inhibit neuropathic target esterase (NTE), the target of delayed organophosphate-induced neuropathy. Experiments have shown that chronic oral administration of KBR-2822 (0.2 or 0.4 mg/kg/day) to chickens does not induce neuropathy and does not exacerbate toxic or traumatic axonopathy, even in the absence of intentional axonal injury. In the control group, administration of non-neuropathic Paraoxon (0.05 mg/kg/day orally) showed a mean AChE inhibition of 45% and no NTE inhibition. After chronic administration of KBR-2822, PMSF (120 mg/kg subcutaneously, 24 hours after the last KBR-2822 dose) was given, and KBR-2822-treated chickens did not develop neuropathy, while chickens treated with neuropathic DFP did. This suggests that sustained facilitatory "stress" is harmless to chicken axons in the absence of concurrent biochemical or neurotoxic insults.
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-
- HY-148611
-
|
|
Others
|
Neurological Disease
|
|
NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases .
|
-
- HY-15681
-
|
|
CDK
|
Cancer
|
|
Senexin A is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters .
|
-
- HY-114404
-
|
|
PROTACs
p38 MAPK
Autophagy
|
Cancer
|
|
SJFα is a 13-atom linker PROTAC based on von Hippel-Lindau ligand. SJFα degrades p38α with a DC50 of 7.16 nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM .
|
-
- HY-N2574
-
|
|
Glucosidase
|
Metabolic Disease
|
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
- HY-135841
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Metabolic Disease
Cancer
|
|
CM010 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM010 does not inhibit any of the other ALDH family members. CM010 can regulate metabolism and has anti-cancer activity .
|
-
- HY-133016
-
|
|
MetAP
|
Cardiovascular Disease
Cancer
|
|
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
|
-
- HY-139188
-
|
|
PI5P4K
|
Metabolic Disease
Cancer
|
|
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research .
|
-
- HY-144261
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-3 (compound 35) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-3 shows high activity against VIM-1 and NDM-1, with IC50 of 0.6 and 1.0 μM, respectively. Metallo-β-lactamase-IN-3 does not show inhibition of IMP-7 .
|
-
- HY-143202
-
|
|
Liposome
|
Others
|
|
DPhPC is a derivative of phosphatidylcholine (PC) used to synthesize bilayer vesicle phospholipids. DPhPC bilayer membranes do not leak ions in the absence of pores or ion channels, so they are often used to study the activity of ion channels and the regulation of membrane potential. Nanoliposomes (NTG) prepared based on DPhPC can improve the bioavailability of nitric oxide (NO) and have effective anti-inflammatory effects .
|
-
- HY-N8264
-
|
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities .
|
-
- HY-107345
-
|
Ombolan
|
Others
|
Inflammation/Immunology
|
|
Droxicam (Ombolan) is a non-steroidal anti-inflammatory agent, with strong analgesic activity. Droxicam acts by inhibiting PGE2 varies, and is characterised by being a pro-drug of Piroxicam (HY-B0253). Droxicam is well tolerated with slight side effects in the said mucosa. Droxicam does not show cardiovascular or respiratory effects in cats, and inhibits peritoneal capillary permeability in mouse .
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-
- HY-15681A
-
|
|
CDK
|
Cancer
|
|
Senexin A hydrochloride is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters .
|
-
- HY-156205
-
|
|
Phosphodiesterase (PDE)
|
Infection
|
|
CdnP-IN-1 (compound c82) is a potent and selective non-nucleotide MTB CDN PDE (CdnP; Mycobacterium tuberculosis cyclic dinucleotide phosphodiesterase) inhibitor with an IC50 of 18 μM. CdnP-IN-1 does not inhibit the enzymatic activities of three other bacterial CDN PDEs (Yybt, RocR, and GBS-CdnP), a viral CDN PDE (poxin) or mammalian ENPP1 .
|
-
- HY-P10579
-
|
|
Ephrin Receptor
|
Cancer
|
|
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .
|
-
- HY-137635
-
|
|
PKA
|
Neurological Disease
|
|
Sp-6-Phe-cAMPS is a potent, site-selective and membrane-permeable activator of cAMP-dependent protein kinase. Sp-6-Phe-cAMPS does not activate exchange factors directly activated by cAMP and can therefore be used as an Epac negative control. Sp-6-Phe-cAMPS can be used in the study of neurodegenerative diseases .
|
-
- HY-118316
-
|
|
Others
|
Inflammation/Immunology
|
|
GSK223 is a quinazolinone NOD1 pathway inhibitor with potential anti-inflammatory activity. GSK223 can selectively inhibit IL-8 release under iE-DAP stimulation without affecting IL-8 secretion caused by TNF receptor, TLR2 or NOD2 agonists. GSK223 does not directly inhibit RIP2 kinase activity.
|
-
- HY-111073
-
|
Y101
|
HBV
|
Infection
Inflammation/Immunology
|
|
Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
|
-
- HY-153663
-
|
|
Ras
|
Cancer
|
|
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
|
-
- HY-12646
-
|
|
Ras
Apoptosis
|
Cancer
|
|
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
|
-
- 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-12646A
-
|
|
Ras
Apoptosis
|
Cancer
|
|
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
|
-
- HY-111518
-
|
|
PROTACs
CDK
|
Cancer
|
|
JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19 .
|
-
- HY-124811
-
|
|
c-Myc
|
Cancer
|
|
IRES-C11 is a spectfic c-MYC internal ribosome entry site (IRES) translation inhibitor. IRES-C11 blocks the interaction of a requisite c-MYC IRES trans-acting factor, heterogeneous nuclear ribonucleoprotein A1, with its IRES. IRES-C11 does not inhibits BAG-1, XIAP and p53 IRESes .
|
-
- HY-145953
-
|
|
Others
|
Cancer
|
|
VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer .
|
-
- HY-146459
-
|
|
Akt
|
Cancer
|
|
Akt1-IN-1 (compound 5b) is a potent and selective Akt1 inhibitor with an IC50 value of 18.79 nM in MIA Paca-2 cells. Akt1-IN-1 does not exhibit obvious teratogenicity, hepatotoxicity and cardiotoxicity (No Observed Adverse Effect Level > 100 µM). Akt1-IN-1 can be used for researching anticancer .
|
-
- HY-137975
-
|
|
Others
|
Endocrinology
|
|
Exo2 is a secretion inhibitor. Exo2 perturbs trafficking of Shiga toxin between endosomes and the trans-Golgi network. Exo2 blocks secretory cargo exit from the ER (endoplasmic reticulum) and disrupts the Golgi apparatus, but does not affect the morphology of the TGN (trans-Golgi network) Exo2 can stimulate calcium-dependent exocytosis in permeabilized adrenal chromaff in cells .
|
-
- HY-151361
-
|
|
AMPK
|
Cancer
|
|
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer .
|
-
- HY-126833
-
|
|
Endogenous Metabolite
|
Infection
Cancer
|
|
Myristoyl coenzyme A is a myristoylated coenzyme A (CoA). Myristoylation is an essential process in viruses and is generally controlled by N-myristoyltransferase (NMT). And NMT is more active in colon epithelial tumors than in normal cells. Reduced Ccoenzyme A (CoA) is known to be a key regulator of NMT activity, whereas oxidized CoA does not allow NMT to promote myristoylation. Myristoyl coenzyme A blocks the demyristoylation process and has potential anticancer and antiviral mechanisms.
|
-
- HY-128439
-
|
|
DYRK
|
Cancer
|
|
BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway .
|
-
- HY-116871
-
|
|
CDK
|
Cancer
|
|
YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
|
-
- HY-E70393J
-
|
|
Others
|
Others
|
|
Bovine Factor XIa is an enzyme, which is involved in the intrinsic pathway of blood coagulation. Bovine Factor XIa is highly selective and exhibits a minimal extended substrate recognition site of at least five residues long. Bovine Factor XIa is reactive as Bovine Factor IXa (HY-E70393I) does, that it cleaves all the peptides bearing factor IX activation site sequences .
|
-
- HY-19012
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
N-1518 is an α and β adrenergic receptor blocker that has competitive antagonism against β1 and α1 receptors, but does not show selectivity for β1 receptors, but shows about 20-fold selectivity for α1 receptors. N-1518 has vasodilatory effects and can be used in the research field of hypertension treatment .
|
-
- HY-145287A
-
|
|
DNA/RNA Synthesis
Parasite
|
Infection
|
|
S-MGB-234 TFA is a minor groove binder used for African Animal Trypanosomiasis (AAT). S-MGB-234 exhibits excellent in vitro activity against the primary pathogens of AAT: Trypanosoma congolense and Trypanosoma vivax. S-MGB-234 TFA does not show cross-resistance with current diamidine active molecules and is not internalized via the transporters used by diamidines .
|
-
- HY-136720
-
|
|
Others
|
Others
|
|
ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
|
-
- HY-15648A
-
GSK-J2
2 Publications Verification
|
Others
|
Cancer
|
|
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
|
-
- HY-110261
-
|
|
IKK
E1/E2/E3 Enzyme
NF-κB
|
Inflammation/Immunology
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|
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect .
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-
- HY-129937
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .
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-
- HY-110077
-
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Akt
Apoptosis
|
Cancer
|
|
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL) .
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-
- HY-146564
-
|
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NF-κB
|
Inflammation/Immunology
|
|
R-HP210 acts on the NF-κB mediated tethered transrepression function (IC50=3.80 μM). R-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. R-HP210 does not induce the transactivation functions of Glucocorticoids (GCs) .
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-
- HY-144724
-
|
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HSP
Apoptosis
|
Cancer
|
|
HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis .
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-
- HY-N0990
-
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Others
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Cancer
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|
1,5,15-Trimethylmorindol is an anthraquinone isolated from the leaves of Morinda citrifolia. 1,5,15- trimethylmorindol (25 μg/mL) does not show significant cytotoxic activity on the human T-cell leukemia cell line, Jurkat, by itself but it shows cytotoxicity (IC50 14.5-15.0 μg/mL) when combined with 0.5-1.5 μg/mL of TRAIL in the cell proliferation assay .
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-
- HY-118668
-
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Others
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Others
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|
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.
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- HY-122464
-
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Others
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Others
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|
(±)-Jasmonic acid is an endogenous growth regulator closely related to plant resistance to abiotic stresses, used to activate defense responses to wounding, herbivory, and pathogen attacks. (±)-Jasmonic acid does not play an independent regulatory role, but works in a complex signaling network with other plant hormone signaling pathways. In addition, (±)-Jasmonic acid can also reduce chlorophyll levels in green and etiolated barley leaf segments and inhibit the elongation of rice seedlings .
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-
- HY-133033
-
|
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Mitochondrial Metabolism
|
Metabolic Disease
|
|
COQ7-IN-1, a highly potent inhibitor of human coenzyme Q (COQ7), interferes with ubiquinone (UQ) synthesis. COQ7-IN-1 does not disturb physiological cell growth of human normal culture cells. COQ7-IN-1 can be used for the research of the balance between UQ supplementation pathways: de novo UQ synthesis and extracellular UQ uptake .
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-
- HY-145827
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity .
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- HY-126833A
-
|
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Endogenous Metabolite
|
Infection
Cancer
|
|
Myristoyl coenzyme A lithium is lithium-labeled myristoylated coenzyme A (CoA). Myristoylation is an essential process in viruses and is generally controlled by N-myristoyltransferase (NMT). And NMT is more active in colon epithelial tumors than in normal cells. Reduced Ccoenzyme A (CoA) is known to be a key regulator of NMT activity, whereas oxidized CoA does not allow NMT to promote myristoylation. Myristoyl coenzyme A blocks the demyristoylation process and has potential anticancer and antiviral mechanisms.
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-
- HY-110056
-
|
|
CRFR
|
Neurological Disease
|
|
NBI 35965 hydrochloride is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects .
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-
- HY-120255
-
|
17(R)-HDoHE
|
Others
|
Inflammation/Immunology
|
|
17(R)-HDHA (17(R)-HDoHE) is a pro-resolving mediator (SPM). 17(R)-HDHA enhances the differentiation of B cells toward the CD27(+)CD38(+) antibody-secreting cell phenotype, thereby strongly increasing IgM and IgG production by activated B cells. 17(R)-HDHA does not affect cell proliferation and is non-toxic to cells .
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-
- HY-162266
-
|
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Others
|
Cancer
|
|
C3TD879 is an inhibitor of citron kinase (CITK), an AGC family serine/threonine kinase that regulates cytokinesis. C3TD879 inhibits CITK catalytic activity with an IC50 of 12 nM. C3TD879 does not induce CITK knockdown effects on cell proliferation, cell cycle progression, or cytokinesis, but rather reduces the activity by directly binding full-length human CITK (NanoBRET Kd< 10 nM) .
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-
- HY-161296
-
|
|
Bacterial
HIV
|
Infection
|
|
TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .
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-
- HY-134264
-
|
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Others
|
Cardiovascular Disease
Neurological Disease
|
|
8-Br-2'-O-Me-cAMP is an analogue of the signal molecule cyclic AMP (cAMP). 8-Br-2'-O-Me-cAMP is an agonist of exchange factors activated by cAMP (Epac), while it doesn't activate PKA as cAMP do. 8-Br-2'-O-Me-cAMP can be used in cardiovascular disease research .
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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-114252R
-
|
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Na+/K+ ATPase
|
Cardiovascular Disease
|
|
Strophanthidin (Standard) is the analytical standard of Strophanthidin. This product is intended for research and analytical applications. Strophanthidin is a naturally available cardiac glycoside . Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal . Strophanthidin increases both diastolic and systolic intracellular Ca2+ concentration .
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-
- HY-B1116A
-
|
(-)-Metaraminol; (-)-erythro-Metaraminol; (-)-m-Hydroxynorephedrine
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Others
|
Neurological Disease
|
|
Metaraminol ((-)-Metaraminol) is a sympathomimetic compound with activity that acts primarily at alpha-1 adrenergic receptors. Metaraminol is used to inhibit hypotension due to vasodilation, particularly in critically ill patients who do not respond well to volume resuscitation. Metaraminol may also be used as an adjunct to help improve cardiac contractility. The use of metaraminol may be supported by less evidence, but its effectiveness in specific situations remains of interest .
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-
- HY-106005
-
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Parasite
PI4K
|
Infection
|
|
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
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-
- HY-100277
-
|
SR-202
|
PPAR
|
Metabolic Disease
|
|
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
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-
- HY-16576A
-
SMI-4a
1 Publications Verification
TCS-PIM-1-4a
|
Pim
|
Cancer
|
|
SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity .
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-
- HY-115644
-
|
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Melanocortin Receptor
|
Inflammation/Immunology
|
|
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties .
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-
- HY-P9924
-
|
LY2439821
|
Interleukin Related
|
Inflammation/Immunology
|
|
Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis .
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-
- HY-103520
-
|
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GABA Receptor
|
Neurological Disease
|
|
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
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-
- HY-155077
-
|
|
JNK
|
Cancer
|
|
JNK-IN-12 (compound P2) is a mitochondrial-targeted JNK inhibitor (IC50=66.3 nM), consisting of a mitochondrial-specific cell-penetrating peptide and a specific inhibitor of JNK, SP600125 (HY-12041). JNK-IN-12 doesn't inhibit nuclear JNK signaling, but does inhibit mitochondrial JNK phosphorylation. JNK-IN-12 helps to improve the Parkinson's disease (PD) both in vitro and in vivo .
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-
- HY-163145
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
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-
- HY-125066
-
|
|
Bacterial
|
Infection
|
|
Reveromycin B is a spiroketal bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells (IC50=6 μg/mL) and exhibits pH-dependent antifungal activity against C. albicans (MICs=15.6 and >500 μg/mL at pH 3.0 and 7.4, respectively). Unlike reveromycin A and reveromycin C, reveromycin B does not inhibit proliferation of KB and K562 cells.
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-
- 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) .
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-
- HY-12172
-
|
ACT-077825
|
Others
|
Cardiovascular Disease
|
|
MK-8141 (ACT-077825) is a renin inhibitor that significantly increases levels of immunoreactive renin (ir-AR) by sevenfold but does not result in sustained reductions in blood renin activity (PRA). This study evaluated the antihypertensive efficacy of MK-8141 in hypertensive disease. Despite its effects on ir-AR, MK-8141 (ACT-077825) did not produce significant blood pressure-lowering effects in the absence of sustained PRA inhibition.
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-
- HY-13766
-
|
VX-853
|
Others
|
Others
|
|
Timcodar is a macrolide agent, and studies have shown that during adipogenesis, timcodar can significantly inhibit fat accumulation, with an effect similar to that of rapamycin. However, unlike rapamycin, timcodar does not cause immunosuppression and glucose resistance. In addition, timcodar can effectively inhibit the adipogenic transcriptional regulators PPAR?? and C/EBP??, thereby inhibiting genes involved in fat accumulation. These studies lay the foundation for timcodar as a potential anti-obesity therapy, as obesity is becoming a global epidemic.
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-
- HY-D2365
-
|
|
Fluorescent Dye
|
Others
|
|
QSY 21 NHS, a dark quencher is an efficient energy transfer acceptor of the far red and NIR fluorescent probes. QSY 21 NHS works in
the wavelength range of 540-750 nm, and is frequently used in FRET applications. QSY 21 NHS does not emit fluorescence in normal conditions. NHS esters can be used to label the primary amines (R-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules .
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-
- HY-N13248
-
|
|
Others
|
Metabolic Disease
|
|
Mulberry Leaf Extract is a mulberry leaf extract, and its components include: 1-Deoxynojirimycin. Mulberry Leaf Extract can effectively alleviate the adverse effects of high-fat diet on blood lipids and renal function, regulate lipid metabolism abnormalities, and significantly inhibit the accumulation of glycosylated substances in glomeruli. Mulberry Leaf Extract can regulate the key signaling pathways of diabetic nephropathy, but does not directly affect blood glucose levels. .
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-
- 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 .
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-
- HY-115827
-
|
|
Others
|
Others
|
|
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.
|
-
- HY-162390
-
|
|
Amylases
Glucosidase
|
Endocrinology
|
|
α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase (IC50 = 30.39 μM) and α-glucosidase (IC50 = 65.1 μM), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier .
|
-
- HY-128341
-
|
|
ERK
|
Cardiovascular Disease
Cancer
|
|
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
|
-
- HY-N6701
-
|
|
Arp2/3 Complex
|
Cancer
|
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport . Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis . Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings .
|
-
- HY-14521
-
|
DDATHF
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-14521B
-
|
DDATHF hydrate
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-126396
-
|
|
CaMK
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicans, C. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae) .
|
-
- HY-110282
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Metabolic Disease
|
|
S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation .
|
-
- HY-P9948
-
|
Campath-IH
|
Apoptosis
|
Cancer
|
|
Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research .
|
-
- HY-P2434
-
|
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
Cancer
|
|
AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research .
|
-
- HY-P2988A
-
|
|
Others
|
Metabolic Disease
|
|
α2-3,6 Neuraminidase, Bifidobacterium infantis is a highly specific exoglycosidase that catalyzes the hydrolysis of non-reducing terminal α2-3 and α2-6 unbranched sialic acid residues from complex carbohydrates and glycoproteins. α2-3,6 Neuraminidase does not exhibit activity on α2-8 or branched sialic acids .
|
-
- HY-157131
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+ influx in macrophages, and inhibits macrophage phagocytosis .
|
-
- HY-103378
-
|
|
CRFR
|
Neurological Disease
|
|
NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects .
|
-
- HY-N2574R
-
|
|
Glucosidase
|
Metabolic Disease
|
|
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
- HY-402410
-
|
|
TET Protein
|
Cancer
|
|
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research .
|
-
- HY-117730
-
|
Antibiotic 1063Z
|
Antibiotic
|
Infection
|
|
Pulvomycin (Antibiotic 1063Z) is an antibiotic with protein biosynthesis inhibitory activity. Pulvomycin is able to block protein biosynthesis in Bacillus brevis grown in cells. Pulvomycin is highly sensitive to poly(Phe) synthesis in cell-free systems. Pulvomycin does not affect the transfer of phenylalanine to tRNA. Studies have shown that the target of Pulvomycin is the elongation of the polypeptide chain. Pulvomycin can also prevent the formation of a ternary complex between the elongation factor Tu, GTP and aminoacyl-tRNA .
|
-
- HY-135730
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
Aglepristone is a synthetic steroidal antiprogestin with abortifacient activity. Aglepristone is used exclusively as an abortifacient in pregnant animals. Aglepristone has been shown to be a safe and effective abortifacient in the second trimester of pregnancy. Aglepristone causes termination of pregnancy and does not cause fetal resorption. During aglepristone treatment, an increase in plasma concentrations of prolactin was observed, while progesterone levels remained unchanged. The use of aglepristone also resulted in early arrest of corpus luteum function and a shortening of the estrus interval .
|
-
- HY-129407
-
|
Ala-ala-phe-chloromethylketone tfa; N-Ala-Ala-Phe-CMK; Tripeptidyl Peptidase inhibitor II
|
Others
|
Infection
|
|
AAF-CMK TFA (Ala-ala-phe-chloromethylketone tfa; N-Ala-Ala-Phe-CMK) is a subtilisin-type serine peptidase that removes tripeptides from the free NH2 termini of oligopeptides. AAF-CMK TFA is an irreversible inhibitor of TPPII and is typically used at concentrations of 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at a concentration of 50 μM.
|
-
- HY-125026
-
|
|
Others
|
Others
|
|
MyomiRs-IN-1 is a myomiRs inhibitor with activity to inhibit myoD translation in C2C12 cells. MyomiRs-IN-1 does not change the expression level of myoD mRNA, while downregulating the expression of differentiation markers. MyomiRs-IN-1 affects the expression of myomiRs in muscle cells by regulating the regulatory pathway between miR-221/222 and myoD. The application of MyomiRs-IN-1 can facilitate research on muscle development and related diseases .
|
-
- HY-163514
-
|
|
Cholinesterase (ChE)
DYRK
|
Neurological Disease
|
|
hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research .
|
-
- HY-123076
-
|
PFN-α
|
MDM-2/p53
|
Neurological Disease
|
|
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue .
|
-
- HY-A0170
-
|
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
|
-
- HY-103399
-
|
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
|
-
- HY-P2294
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
|
-
- HY-P2294A
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
|
-
- HY-18944
-
|
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-136250
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity .
|
-
- HY-100953
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research .
|
-
- HY-123981
-
|
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
- HY-145102
-
|
|
HSP
Apoptosis
|
Cancer
|
|
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
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-
- HY-14521A
-
|
DDATHF disodium
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-129047B
-
|
|
Others
|
Others
|
|
Recombinant Trypsin Solution is an animal-free trypsin solution used to digest cells or tissues. Recombinant Trypsin Solution has high stability at room temperature and gentle digestion, and can be used to digest weakly adherent cells or stem cells under low serum or serum-free culture conditions. Compared with traditional trypsin digestion solution, Recombinant Trypsin Solution does not contain any animal-derived ingredients, is gentle and effective, and can replace the application of animal-derived trypsin in cell digestion .
|
-
- HY-136855
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
MitoPBN is a mitochondria-targeted antioxidant. It accumulates in the mitochondria following the generation of a mitochondrial membrane potential by succinate, an effect that is blocked by addition of the mitochondrial membrane potential uncoupler FCCP. MitoPBN inhibits superoxide activation of mitochondrial uncoupling protein 1 (UCP1), UCP2, and UCP3 when used at a concentration of 250 nM in vitro but does not react with superoxide. It traps hydroxyl (IC50=~77 μM) and carbon-centered radicals and inhibits the initiation of lipid peroxidation in isolated bovine heart mitochondria.
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-
- 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-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 .
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-
- 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-167922
-
|
|
Others
|
Neurological Disease
|
|
(R,R,S)-GAT107 is a fully agonistic positive modulator of α7 nicotinic receptors with significant biological activity. Its activity is entirely present in its (+)-isomer 1b, while (-)-isomer 1a does not affect its activity when used together. Studies have shown that (R,R,S)-GAT107 is the most potent ago-PAM for α7 nicotinic receptors currently known and has the potential for further in vivo evaluation .
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-
- HY-136625
-
|
|
Others
|
Neurological Disease
|
|
LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT). Its cardiovascular activity was studied in anesthetized spontaneously hypertensive rats (SHR). Acute intraperitoneal injection of 10 and 20 mg/kg of LY134046 caused minimal cardiovascular changes, while 40 mg/kg resulted in a sustained decrease in mean arterial blood pressure and heart rate. This hypotension and bradycardia occurred rapidly and occurred when brain NMT activity was significantly inhibited. However, norepinephrine concentrations in rat brains were not significantly reduced at the time when LY134046-induced blood pressure and heart rate effects were maximal. The acute cardiovascular activity of LY134046 was not significantly affected by pretreatment of SHR with phentolamine, propranolol, or atropine, and LY134046 reduced heart rate in suspended SHR. In addition, acute or chronic administration of LY134046 did not antagonize the vasoconstrictor responses induced by sympathetic nerve stimulation or exogenous norepinephrine. These observations suggest that LY134046 does not interact with adrenergic or cholinergic receptors and that its hypotensive and bradycardic effects do not require neurogenic tension. Chronic intraperitoneal administration of LY134046 (40 mg/kg/day) resulted in a sustained and significant inhibition of hypothalamic and brainstem NMT activity, leading to central norepinephrine depletion. During chronic treatment, norepinephrine and dopamine concentrations increased in the brainstem and hypothalamus of SHR. Despite chronic inhibition of central NMT and norepinephrine depletion, cardiovascular parameters in SHR treated groups were not significantly different from those in saline-injected controls. Chronic treatment with LY134046 did not result in tolerance to its central biochemical effects or acute cardiovascular activity. The present study does not support the idea that norepinephrine-producing neurons are involved in the central regulation of cardiovascular function, because the hypotension and bradycardia induced by acute administration of LY134046 occurred before a significant decrease in hypothalamic norepinephrine concentrations, whereas chronic inhibition of central NMT and depletion of norepinephrine resulted in minimal changes in baseline cardiovascular parameters.
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-
- HY-100277R
-
|
|
PPAR
|
Metabolic Disease
|
|
Mifobate (Standard) is the analytical standard of Mifobate. This product is intended for research and analytical applications. Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-P10281
-
|
|
Bacterial
|
Infection
|
|
RW3 is a small cationic hexapeptide with amphiphilic properties. RW3 targets the plasma membrane of bacteria and works by inhibiting cell respiration and cell wall synthesis. RW3 shows high biological activity against gram-positive bacteria and does not show significant cytotoxic or hemolytic effects in previous studies. RW3 quickly kills 97% of the initial colony forming units (CFU) within 10 minutes at twice the minimum inhibitory concentration (MIC). RW3 can be used in antimicrobial and antifungal studies .
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-
- HY-12755
-
|
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-124691
-
D-I03
2 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin .
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-
- HY-16940
-
|
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
|
-
- HY-116423
-
|
|
NEKs
|
Cancer
|
|
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 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-116423A
-
|
|
NEKs
|
Cancer
|
|
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) 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-136252
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-04-132 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity .
|
-
- HY-123264
-
|
|
Potassium Channel
|
Neurological Disease
|
|
RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has the potential for neurologic disorders associated with neuronal hyperexcitability research .
|
-
- HY-131404
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
|
-
- HY-150622
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent nsp13 (non-structural protein 13) inhibitor. SARS-CoV-2 nsp13-IN-1 only inhibits nsp13 ssDNA + ATPase, with an IC50 of 6 μM. SARS-CoV-2 nsp13-IN-1 does not inhibit ssDNA - ATPase. SARS-CoV-2 nsp13-IN-1 can be used for COVID-19 research .
|
-
- 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-136250A
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity .
|
-
- HY-P5836
-
|
|
Interleukin Related
Bacterial
Enterovirus
|
Inflammation/Immunology
|
|
Citrullinated LL-37 1cit is a citrullinated LL-37 (HY-P1222) peptide. Citrullinated LL-37 1cit does not alter the antiviral effect of LL-37 toward human rhinovirus. Citrullinated LL-37 1cit shows antibacterial activity toward S. aureus. Citrullinated LL-37 1cit causes a reduction in the levels of IL-8, CCL5, and IL-6 mRNA induced by RV1B .
|
-
- HY-155300
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease .
|
-
- HY-145749
-
|
|
PARP
|
Cancer
|
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
|
-
- HY-W728005
-
|
|
SARS-CoV
|
Infection
|
|
Covidcil-19 (compound C5) avidly binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with a Kd of 11 nM. Covidcil-19 stabilizes the hairpin’s folded state and impairs frameshifting in cells. Covidcil-19 reduces frameshifting efficiency of the SARS-CoV-2 FSE and does not affect SARS-CoV-2 FSE RNA levels. Covidcil-19 inhibits a process essential for SARS-CoV-2 viral propagation .
|
-
- HY-160477
-
|
|
PIKfyve
NF-κB
IKK
|
Inflammation/Immunology
|
|
DC-SX029 is a potent SNX10 protein-protein interaction (PPI) inhibitor with oral activity with an estimated KD constant of ~0.935 μM by surface plasmon resonance (SPR). DC-SX029 blocks the SNX10-PIKfyve interaction, thereby decreased the TBK1/c-Rel signaling activation. DC-SX029 does not affect the protein level of SNX10. DC-SX029 has the potential for inflammatory bowel disease (IBD) research .
|
-
- HY-15648I
-
|
|
Others
|
Cancer
|
|
GSK-J2 sodium is the sodium form of GSK-J2 (HY-15648A). GSK-J2 is an isomer of GSK-J1, and does not have any specific activity. GSK-J1 (HY-15648) is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A .
|
-
- HY-106909A
-
|
KAE-393
|
5-HT Receptor
|
Cardiovascular Disease
|
|
YM114 (KAE-393) is a highly potent and selective (5-HT)3-receptor antagonist that does not affect Veratridine (HY-N6691)- or electrical stimulation-induced bradycardia in anesthetized rats. YM114 inhibits 2-methyl-5-HT (HY-19358)-induced Bezold-Jarisch reflex, which originates from (5-HT)3-receptor located on the endings of vagal afferent nerves in the heart .
|
-
- HY-W747104
-
|
|
Others
|
Endocrinology
|
|
(9E)-Tetradecen-1-ol is a pheromone that has no significant sexual attraction when used alone and can be secreted from the abdomen of the female Bertha armyworm moth (Mamestra configurata (Walker)). Isolate in tip extract to get in isolate. Another pheromone (Z)-11-hexadecen-1-ol was also isolated at the same time. Only when the two pheromones are mixed do they show male attraction (the ratio of C16:C14 in the mixture is about 19:1). optimal) .
|
-
- HY-A0170R
-
|
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin (Standard) is the analytical standard of Trovafloxacin. This product is intended for research and analytical applications. Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
|
-
- HY-10256
-
Adezmapimod
Maximum Cited Publications
453 Publications Verification
SB 203580; RWJ 64809
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-10256A
-
|
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-D0970
-
|
Direct Blue 14; Trypan Blue
|
Fluorescent Dye
|
Others
|
|
Diphenyl Blue (Trypan Blue) is a cell active dye, the most commonly used dye for the identification of dead cells, of en used to test cell membrane integrity and cell viability. Diphenyl Blue staining is one of the methods for tissue and cell culture. When cells are deactivated or have incomplete cell membranes, Diphenyl Blue can stain them Blue. Normal living cells with intact cell membranes reject Diphenyl blue and do not stain them blue. However, macrophages are capable of phagocytosis of Diphenyl Blue, so it can be used as a living stain for macrophages .
|
-
- HY-110105
-
|
|
Potassium Channel
|
Neurological Disease
|
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively) .
|
-
- HY-P99045
-
|
|
ADC Antibody
TROP2
|
Cancer
|
|
Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab is used for the synthesis of antibody-drug conjugates (ADC) drugs. Antibody-drug conjugates with sacituzumab (sacituzumab govitecan) (HY-132254) targeting TROP-2 have been approved for the field of triple-negative breast cancer .
|
-
- HY-149269
-
|
|
COX
Carbonic Anhydrase
LOX-1
|
Inflammation/Immunology
|
|
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
|
-
- HY-P5189A
-
|
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Others
|
|
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .
|
-
- HY-155983
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 nsp14-IN-4 (Compound 12q) is a selective SARS-CoV-2 nsp14 methyltransferase inhibitor with an IC50 value of 19 ± 2.5 nM. SARS-CoV-2 nsp14-IN-4 (Compound 12q) do not have a zwitterionic character and can penetrate into cells. SARS-CoV-2 nsp14-IN-4 (Compound 12q) can be used for COVID-19 and its causative agent SARS-CoV-2 research .
|
-
- HY-P990090
-
|
CBP-201
|
Interleukin Related
|
Inflammation/Immunology
|
|
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
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-
- HY-P10420
-
|
|
CD47
Interleukin Related
|
Cancer
|
|
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
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-
- HY-116863
-
|
|
Bacterial
|
Infection
|
|
KKL-40 is a small molecule inhibitor that targets the trans-transcription process and is effective against methicillin-sensitive and -resistant Staphylococcus aureus (S. aureus) as well as other Gram-positive pathogens including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. KKL-40 synergizes with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not synergize with other antibiotics such as daptomycin, kanamycin, or erythromycin. Trans-transcription is an extreme form of recoding, and KKL-40 inhibits trans-transcription but is nontoxic to HeLa cells .
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-
- HY-162712
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX-201 is a selective agonist for OX2R with an EC50 of 8 nM. Pathological proteins produced by neurons are released into the interstitial fluid (ISF) in a manner dependent on neuronal activity and are cleared from the brain via lymphatic pathways. The outflow of pathological proteins to the ISF is related to the arousal state of neurons. OX-201 can induce neuronal awakening and promote the release of tau into the hippocampal ISF. Although OX-201 does not alter hippocampal tau levels, it has potential applications for Alzheimer's disease (AD) associated with sleep/wake rhythm disturbances .
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-
- HY-162749
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
G9D-4 is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of ＞10 μM. G9D-4 plays an important role in pancreatic cancer research (Pink: Ligand for target protein G9a/GLP Inhibitor (HY-15273); Black: Linker; Blue: Ligand for E3 ligase (HY-10984)) .
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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 .
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-
- HY-124798
-
|
|
mTOR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity .
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
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-
- HY-N6785
-
|
|
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
|
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
|
-
- HY-106178
-
PMX-53
4 Publications Verification
3D53
|
Complement System
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects .
|
-
- HY-129917
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
|
-
- HY-117724
-
|
|
PAI-1
|
Cardiovascular Disease
|
|
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay .
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-
- HY-N6785A
-
|
|
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
|
Okadaic acid sodium, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid (sodium) has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid sodium increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid sodium induces tau phosphorylation .
|
-
- HY-162373
-
|
|
Amylases
Glucosidase
P-glycoprotein
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC50: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects .
|
-
- HY-116163
-
|
CYM50202
|
Others
|
Others
|
|
ML350 (CYM50202) is a highly potent OPRK1 antagonist with selectivity and broad biological applications. With IC50 values of 9-16 nM, ML350 shows high selectivity for OPRK1, with selectivity of 219-382-fold and 20-35-fold relative to OPRD1 and OPRM1, respectively. ML350 exhibited favorable characteristics in in vivo pharmacokinetic analysis, including high passive membrane permeability and moderate human plasma protein binding. Extensive screening of ML350 against multiple ion channels, receptors, and transporters showed that it does not have adverse off-target effects .
|
-
- HY-115760
-
|
|
Phosphatase
|
Neurological Disease
Cancer
|
|
Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation .
|
-
- HY-118119
-
|
|
PGE synthase
|
Cancer
|
|
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
|
-
- HY-156237
-
|
|
Autophagy
|
Others
|
|
Beclin1-ATG14L interaction inhibitor 1 (com 19) is a selective Beclin1-ATG14L interaction inhibitor. This protein interaction mechanism specifically targets complex I of the lipid kinase VPS34 without affecting complex II. Because the integrity of VPS34 complex II depends on the Beclin 1-UVRAG interaction. Beclin1-ATG14L interaction inhibitor 1 can disrupt the formation of VPS34 complex I and inhibit autophagy, but does not affect complex II-related vesicle transport .
|
-
- HY-130311
-
|
2-Monolinolein; 2-Monolinoleoylglycerol
|
Cannabinoid Receptor
|
Neurological Disease
|
|
2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
|
-
- HY-W111141
-
|
endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne
|
Biochemical Assay Reagents
|
Others
|
|
BCN-OH (endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne) is a mitochondrial probe based on the lyophilic bidentate bicyclic ligand BCN and is a control reagent for BCN-TPP. The TPP group is a reactive sulfenic acid probe that targets mitochondria. BCN-TPP is known to affect mitochondrial energy, causing a sharp decrease in basal respiration, causing it to exhibit faster reaction kinetics with sulfonated proteins. BCN-OH does not contain hydrophobic triphenylphosphonium (TPP) ions. Using BCN-OH as a control allows the TPP group to be safely introduced when designing sulfenic acid traps .
|
-
- HY-126830
-
|
|
Antifolate
Apoptosis
|
Cancer
|
|
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed .
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-
- HY-121998
-
|
|
Aurora Kinase
|
Others
|
|
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
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-
- HY-10015
-
|
5-(4-Phenoxybutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
|
-
- HY-144123
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
|
-
- HY-16094
-
|
BW 467C60
|
Adrenergic Receptor
|
Neurological Disease
|
|
Bethanidine sulfate and its ortho-chloro derivative (BW 392C60) are potent adrenergic neurone blockers with sympathomimetic effects similar to bretylium and guanethidine in various animal models, particularly in cats. They inhibit the release of noradrenaline during nerve stimulation and enhance smooth muscle responses to adrenaline and noradrenaline. Bethanidine sulfate increases pressor responses to tyramine, though this effect diminishes with higher doses. Unlike guanethidine, Bethanidine sulfate does not deplete pressor amine content in the iris of cats post-administration. It also briefly inhibits autonomic cholinergic mechanisms and causes temporary neuromuscular paralysis in large doses, contrasting with its prolonged adrenergic neurone blocking effects .
|
-
- HY-123035
-
|
|
HSP
Akt
EGFR
|
Endocrinology
|
|
Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research .
|
-
- HY-N6785R
-
|
|
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
|
Okadaic acid (Standard) is the analytical standard of Okadaic acid. This product is intended for research and analytical applications. Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
|
-
- HY-163982
-
|
|
Others
|
Inflammation/Immunology
|
|
FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
|
-
- HY-123189
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
- 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-P5357
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)
|
-
- HY-W241345
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
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.
|
-
- HY-N7402
-
|
|
Others
|
Others
|
|
Hexyl hexanoate is a fruit aroma component with potential food and beverage additive activity. Hexyl hexanoate is found in alcoholic beverages and is used to blend fruit flavors. Hexyl hexanoate is present in many fruits, Parmesan cheese, alcoholic beverages, and black tea. Hexyl hexanoate is a volatile component produced as a result of fruit ripening. Toxicity assessments of hexyl hexanoate showed that it is not mutagenic and that exposure is below safety thresholds for repeated dose, reproduction, and local respiratory toxicity. Hexyl hexanoate is also below thresholds in skin sensitization assessments, and for phototoxicity and photosensitization, the results showed that it does not present a relevant risk. Hexyl hexanoate is considered non-persistent, non-bioaccumulative, and non-toxic according to the environmental criteria of the International Fragrance Association .
|
-
- HY-139124
-
|
15(R)-Carboprost; 15(R)-15-methyl PGF2α
|
Others
|
Metabolic Disease
|
|
15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
|
-
- HY-130743
-
|
Bis-eugenol; Dehydrodieugenol
|
Parasite
|
Infection
|
|
Dieugenol is a neolignan that has been found in N. leucantha and has antioxidative and antiprotozoal activities. It inhibits the formation of thiobarbituric acid reactive substances (TBARS) and scavenges superoxide anions, but not hydroxyl radicals, in cell-free assays. It has anti-trypanosomal activity against T. cruzi amastigotes and trypomastigotes (IC50s=15.1 and 11.5 μM, respectively) but is cytotoxic to NCTC L-929 fibroblasts with a 50% cytotoxic concentration (CC50) value of 58.2 μM.2 Dieugenol (15 μM) disrupts the integrity of the T. cruzi trypomastigote plasma membrane but does not induce the production of reactive oxygen species (ROS) in trypomastigotes or LPS-stimulated and unstimulated isolated mouse peritoneal macrophages.
|
-
- HY-150087
-
|
|
Fluorescent Dye
|
Others
|
|
Ctrl-CF4-S2 is a chemically modified control probe of the copper probe Copper Fluor-4 (CF4, HY-150086), in which two of the four thioether ligands in CF4 (HY-150086) are replaced with methylene groups. CF4 (HY-150086) is a fluorescent probe used for detecting the presence and distribution of copper ions, whereas Ctrl-CF4-S2 does not respond to copper ions. This allows it to eliminate background signals from copper, thereby helping to determine whether the signals from CF4 (HY-150086) accurately reflect the dynamic changes of copper ions in biological systems
|
-
- HY-114796
-
|
|
Others
|
Inflammation/Immunology
|
|
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
|
-
- HY-101448
-
|
WAY-171318
|
MMP
Apoptosis
Interleukin Related
TNF Receptor
Caspase
|
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 .
|
-
- HY-116282
-
|
DSS (MW 5000); DXS (MW 5000)
|
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).
|
-
- HY-155297
-
|
FLA-136
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
|
-
- 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).
|
-
- HY-W008820R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaric acid (Standard) is the analytical standard of Glutaric acid. This product is intended for research and analytical applications. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I .
In Vitro: Glutaric acid (GA) at concentrations of 1 and 2 mM is able to reduce TRAP measurement by up to 28% in a dose-dependent manner (β=0.77; P<0.001). Furthermore, a significantly inverse correlation is also verified between chemiluminescence and TRAP (β=0.81; P<0.001). Glutaric acid does not alter the activities of Cat and SOD, but strongly inhibits (up to 46%) the activity of GPx even at the lower concentration used (0.5 mM). It is observed that the metabolite inhibits this activity in a dose-dependent manner at concentrations as low as 0.05 mM .
|
-
- HY-123597
-
|
DDUG; NCI C04808
|
Others
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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-
- HY-135534
-
|
|
Others
|
Others
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|
Lysine 4-nitroanilide is an amino acid derivative used in studies of enzymology. Two major arylamidase activities were isolated from particle-free supernatant of rat heart by DEAE-Sephadex chromatography. Although both enzymes hydrolyze L-leucine 4-nitroanilide, only the peak II enzyme does so. A third, minor peak (Ia) contains the enzyme active primarily toward L-lysine 4-nitroanilide. The molecular weights of the enzymes in peaks I and II are approximately 257,000 and 105,000, respectively. The optimum pH for the peak I enzyme is approximately pH 7.0, while that for the peak II enzyme is between 7.0 and 8.0. Both enzymes are inhibited by puromycin, p-hydroxymercurybenzoate, catechol, and divalent metal ions. Addition of dithiothreitol stimulates both activities. Dialysis against catechol resulted in inhibition of both peak I and II enzymes, but dialysis against EDTA inhibited only the peak II enzyme.
|
-
- HY-30004
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
- HY-138185
-
|
SF 2738A
|
Bacterial
|
Infection
|
|
Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae by 44% in a model of neuronal cell death induced by all-trans retinoic acid.
|
-
- 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 .
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-
-
-
HY-L115
-
|
|
2,929 compounds
|
|
Natural products are characterized by enormous scaffold diversity and structural complexity, because of which, natural products do show a wide range of biological activities. Medicinal plants have been the major source of medicines over many centuries. About a quarter of all Food and Drug Administration (FDA) and/or the European Medical Agency (EMA) approved drugs are plant based, with well-known drugs such as Paclitaxel and Aspirin having been isolated from plants.
MCE provides a unique collection of 2,929 plant-sourced natural products. MCE Plant-Sourced Natural Product Library is a useful tool for drug discovery that can be used for high throughput screening (HTS) and high content screening (HCS).
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-
-
HY-L003
-
|
|
2,380 compounds
|
|
Apoptosis is an ordered and orchestrated cellular process that occurs in physiological and pathological conditions, which is also called programmed cell death (PCD). Apoptosis plays a crucial role in developing and maintaining the health of the body by eliminating old cells, unhealthy cells and unnecessary cells. Too little or too much apoptosis contribute to many diseases. When apoptosis does not work correctly, cells that should be eliminated may persist and become immortal, for example, in cancer and leukemia. When apoptosis works overly well, it kills too many cells and inflicts grave tissue damage. This is the case in strokes and neurodegenerative disorders such as Alzheimer's, Huntington's, and Parkinson's disease.
MCE designs a unique collection of 2,380 apoptosis-related compounds mainly focusing on the key targets in the apoptosis signaling pathway and can be used in the research of apoptosis signal pathway and related diseases.
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-
-
HY-L142
-
|
|
103 compounds
|
|
Tuberculosis (TB), usually caused by bacteria (Mycobacterium tuberculosis), is an infectious disease that mainly affects the lungs. According to the statistics of the World Health Organization (WHO), 10 million people suffer from tuberculosis every year, and 1.5 million people die of tuberculosis every year, which makes tuberculosis the number one killer of infectious diseases.
Tuberculosis can be cured through the standard 6-month course of treatment of four kinds of antibiotics. Common drugs include rifampicin and isoniazid. In some cases, TB bacteria do not respond to standard drugs, that is, patients with drug-resistant tuberculosis. The treatment of drug-resistant tuberculosis takes longer and is more complex. In the face of the resurgence of tuberculosis in the world and the rapid emergence of multi drug resistant tuberculosis, it is very important to develop new anti-tuberculosis drugs or new clinical treatment schemes for existing anti mycobacterium drugs.
MCE supplies a unique collection of 103 compounds with clear anti-tuberculosis activity. MCE Anti-tuberculosis Compound Library is a useful tool for anti-tuberculosis related research and anti-tuberculosis drug development
|
-
-
HY-L083
-
|
|
2,189 compounds
|
|
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 2,189 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0333
-
|
Sirius Red
|
Dyes
|
|
Direct Red 80 (Sirius Red) is a polyazo dye used principally in staining methods for collagen and amyloid. Direct Red 80 does not release benzidine upon degradation and is safer than many traditional direct dyes .
|
-
- HY-D2365
-
|
|
Dyes
|
|
QSY 21 NHS, a dark quencher is an efficient energy transfer acceptor of the far red and NIR fluorescent probes. QSY 21 NHS works in
the wavelength range of 540-750 nm, and is frequently used in FRET applications. QSY 21 NHS does not emit fluorescence in normal conditions. NHS esters can be used to label the primary amines (R-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules .
|
-
- HY-D0970
-
|
Direct Blue 14; Trypan Blue
|
Dyes
|
|
Diphenyl Blue (Trypan Blue) is a cell active dye, the most commonly used dye for the identification of dead cells, of en used to test cell membrane integrity and cell viability. Diphenyl Blue staining is one of the methods for tissue and cell culture. When cells are deactivated or have incomplete cell membranes, Diphenyl Blue can stain them Blue. Normal living cells with intact cell membranes reject Diphenyl blue and do not stain them blue. However, macrophages are capable of phagocytosis of Diphenyl Blue, so it can be used as a living stain for macrophages .
|
-
- HY-D1629
-
|
|
Fluorescent Dyes/Probes
|
|
Calcium Orange AM is an intracellular calcium reporter. Specific fluorescence can be detected when free calcium binds to Calcium Orange AM (Ex/Em=549/576 nm). Calcium Orange AM does not enter the vacuoles and does not compartmentalize into acidic vesicles .
|
-
- HY-D2182
-
|
|
Fluorescent Dyes/Probes
|
|
Preactivated PE-Cy5 Maleimide is a sulfhydryl reactive dye that reacts with free sulfhydryl groups on proteins. Preactivated APC-Cy5.5 Maleimide binds easily to proteins or antibodies, and does not change the spectral characteristics of APC-Cy/YF after activation.
|
-
- HY-D2180
-
|
|
Fluorescent Dyes/Probes
|
|
Preactivated APC-Cy5.5 Maleimide is a sulfhydryl reactive dye that reacts with free sulfhydryl groups on proteins. Preactivated APC-Cy5.5 Maleimide binds easily to proteins or antibodies, and does not change the spectral characteristics of APC-Cy/YF after activation.
|
-
- HY-150087
-
|
|
Fluorescent Dyes/Probes
|
|
Ctrl-CF4-S2 is a chemically modified control probe of the copper probe Copper Fluor-4 (CF4, HY-150086), in which two of the four thioether ligands in CF4 (HY-150086) are replaced with methylene groups. CF4 (HY-150086) is a fluorescent probe used for detecting the presence and distribution of copper ions, whereas Ctrl-CF4-S2 does not respond to copper ions. This allows it to eliminate background signals from copper, thereby helping to determine whether the signals from CF4 (HY-150086) accurately reflect the dynamic changes of copper ions in biological systems
|
| Cat. No. |
Product Name |
Type |
-
- HY-156262
-
|
|
Gene Sequencing and Synthesis
|
|
DEPC-Treated Water is ultrapure water that has been sterilized by high temperature and high pressure and does not contain nuclease. It can avoid contamination by non-specific endonucleases and exonucleases and does not affect RNase activity .
|
-
- HY-W283556
-
|
|
Chelators
|
|
DO2A-tert-butyl ester is a bifunctional chelator (BFC) that can be used for the coupling of peptides and radionuclides. DO2A-tert-butyl ester can be used in the development of radionuclide imaging tracers .
|
-
- HY-W726767
-
|
|
Chelators
|
|
DO2Ais a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. DO2A can be used for conjugation of peptides and radionuclides.
|
-
- HY-W250844A
-
|
|
Chelators
|
|
DO3A (trisodium)is a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. DO3A (trisodium) can be used for conjugation of peptides and radionuclides.
|
-
- HY-W782081
-
|
|
Chelators
|
|
p-SCN-Bn-oxo-DO3Ais a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. p-SCN-Bn-oxo-DO3A can be used for conjugation of peptides and radionuclides.
|
-
- HY-W782080
-
|
|
Chelators
|
|
p-NH2-Bn-oxo-DO3Ais a bifunctional chelator (Bifunctional Chelator; BFC) and a macrocyclic DOTA derivative used for tumor pre-targeting. p-NH2-Bn-oxo-DO3A can be used for conjugation of peptides and radionuclides.
|
-
- HY-142981
-
|
DODA
|
Drug Delivery
|
|
Dioctadecylamine (DODA) is a secondary amine that has been shown to self-organize in plate-like structures in aqueous solution. Dioctadecylamine exhibits sufficiently hydrophobic properties of nanoparticles and good dispersibility in nonpolar solvent. Dioctadecylamine does not form a monolayer above pH 3.9 .
|
-
- HY-155909
-
|
mPEG-SC (MW 3400); mPEG-Succinimidyl ester (MW 3400)
|
Drug Delivery
|
|
m-PEG-NHS ester (MW 3400) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-155909A
-
|
mPEG-SC (MW 1000); mPEG-Succinimidyl ester (MW 1000)
|
Drug Delivery
|
|
m-PEG-NHS ester (MW 1000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-155909B
-
|
mPEG-SC (MW 550); mPEG-Succinimidyl ester (MW 550)
|
Drug Delivery
|
|
m-PEG-NHS ester (MW 550) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-155909C
-
|
mPEG-SC (MW 350); mPEG-Succinimidyl ester (MW 350)
|
Drug Delivery
|
|
m-PEG-NHS ester (MW 350) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-W591424
-
|
mPEG-SC (MW 2000); mPEG-Succinimidyl ester (MW 2000)
|
Drug Delivery
|
|
m-PEG-NHS ester (MW 2000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
|
-
- HY-W127739
-
|
Zinc ethylene-1, 2-bisdithiocarbamate
|
Biochemical Assay Reagents
|
|
Zineb is an agricultural fungicide of the dithiocarbamate class. Its toxicity is relatively low, and there is little evidence of human harm from exposure. Oxidative stress is one of the main factors contributing to diseases caused by Zineb. Zineb does not alter the activity of any superoxide dismutase enzymes. Catalase (CAT) activity was reduced only by Zineb.
|
-
- HY-161587
-
|
|
Biochemical Assay Reagents
|
|
Chloramphenicol/OVA is a conjugate of Chloramphenicol (HY-B0239) and Ovalbumin (OVA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes and can enhance cross-presentation and the production of antigen-specific T cells.
|
-
- HY-161581
-
|
|
Biochemical Assay Reagents
|
|
Metronidazole/OVA is a conjugate of Metronidazole (HY-B0318) and Ovalbumin (OVA). By conjugating the antigen with protein adjuvants, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt the primary epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-163556
-
|
|
Biochemical Assay Reagents
|
|
COT/BSA is the antigen-adjuvant conjugate of COT (cyclooctatetraene) and Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes and can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-161553
-
|
|
Biochemical Assay Reagents
|
|
Biotin/KLH is an antigen-adjuvant conjugate that consists of Biotin and Keyhole Limpet Hemocyanin (KLH). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-161554
-
|
|
Biochemical Assay Reagents
|
|
Clenbuterol/BSA is an antigen-adjuvant conjugate of Clenbuterol (HY-B1615) and Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, it can enhance the production of antigen-specific antibodies in vaccine models. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-163553
-
|
|
Biochemical Assay Reagents
|
|
Metronidazole/BSA is an antigen-adjuvant conjugate of Metronidazole (HY-B0318) and Bovine Serum Albumin (BSA). By conjugating the antigen with the protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the production of antigen-specific T cells.
|
-
- HY-161594
-
|
|
Biochemical Assay Reagents
|
|
Furazolidone/BSA is the antigen-adjuvant conjugate of Furazolidone (HY-B1336) and bovine serum albumin (BSA). By conjugating the antigen with the protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt the major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-161585
-
|
|
Biochemical Assay Reagents
|
|
Diethylstilbestrol/KLH is an antigen-adjuvant conjugate formed by the coupling of Diethylstilbestrol (HY-14598) with Keyhole Limpet Hemocyanin (KLH). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-161586
-
|
|
Biochemical Assay Reagents
|
|
Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-163551
-
|
|
Biochemical Assay Reagents
|
|
The BNP peptide/KLH is an antigen-adjuvant conjugate formed by linking BNP peptide (human brain natriuretic peptide) with keyhole limpet hemocyanin (KLH). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or damage the major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-161545
-
|
|
Biochemical Assay Reagents
|
|
Sudan I/BSA is the antigen-adjuvant conjugate formed by Sudan I (HY-D0024) and Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-143202
-
|
|
Drug Delivery
|
|
DPhPC is a derivative of phosphatidylcholine (PC) used to synthesize bilayer vesicle phospholipids. DPhPC bilayer membranes do not leak ions in the absence of pores or ion channels, so they are often used to study the activity of ion channels and the regulation of membrane potential. Nanoliposomes (NTG) prepared based on DPhPC can improve the bioavailability of nitric oxide (NO) and have effective anti-inflammatory effects .
|
-
- HY-W034392
-
|
|
Biochemical Assay Reagents
|
|
Stewart-Grubbs catalyst is an effective catalyst for the cross-metathesis of olefins with a large number of allylic substituents. In addition, ChemBeads are chemically coated glass beads that improve flowability and chemical homogeneity, making them ideal for automated solid dispensing and high-throughput experiments. Notably, the manufacture of ChemBeads does not require additional chemicals or surfactants, allowing for precise dispensing of sub-milligram amounts of catalyst.
|
-
- HY-161565
-
|
|
Biochemical Assay Reagents
|
|
Gastrin(1-17)/BSA is an antigen-adjuvant conjugate formed by the coupling of Gastrin(1-17) and Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or destroy major epitopes, and it can enhance cross-presentation and the production of antigen-specific T cells.
|
-
- HY-126833
-
|
|
Enzyme Substrates
|
|
Myristoyl coenzyme A is a myristoylated coenzyme A (CoA). Myristoylation is an essential process in viruses and is generally controlled by N-myristoyltransferase (NMT). And NMT is more active in colon epithelial tumors than in normal cells. Reduced Ccoenzyme A (CoA) is known to be a key regulator of NMT activity, whereas oxidized CoA does not allow NMT to promote myristoylation. Myristoyl coenzyme A blocks the demyristoylation process and has potential anticancer and antiviral mechanisms.
|
-
- HY-161551
-
|
|
Biochemical Assay Reagents
|
|
25-OH Vitamin D3/KLH is an antigen-adjuvant conjugate of 25-OH Vitamin D3 (HY-158285) and Keyhole Limpet Hemocyanin (KLH). By conjugating the antigen with the protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-161525
-
|
|
Biochemical Assay Reagents
|
|
1-(2-Aminoethyl)-1H-pyrazol-4-ylphosphonic acid linker/BSA is the conjugate of 1-(2-Aminoethyl)-1H-pyrazol-4-ylphosphonic acid linker (1-(2-氨基乙基)-1H-吡唑-4-基膦酸连接子) and bovine serum albumin (BSA). By conjugating the antigen with a protein adjuvant, it enhances the production of antigen-specific antibodies in vaccine models. The conjugate does not affect protein folding or disrupt key epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
|
-
- HY-W111141
-
|
endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne
|
Biochemical Assay Reagents
|
|
BCN-OH (endo-9-Hydroxymethylbicyclo[6.1.0]non-4-yne) is a mitochondrial probe based on the lyophilic bidentate bicyclic ligand BCN and is a control reagent for BCN-TPP. The TPP group is a reactive sulfenic acid probe that targets mitochondria. BCN-TPP is known to affect mitochondrial energy, causing a sharp decrease in basal respiration, causing it to exhibit faster reaction kinetics with sulfonated proteins. BCN-OH does not contain hydrophobic triphenylphosphonium (TPP) ions. Using BCN-OH as a control allows the TPP group to be safely introduced when designing sulfenic acid traps .
|
-
- 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).
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1334A
-
-
- HY-P1333
-
|
|
Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
|
Neurological Disease
|
|
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
|
-
- HY-105343
-
BW-180C
1 Publications Verification
[D-Ala2, D-Leu5]-Enkephalin; DADLE
|
Opioid Receptor
|
Neurological Disease
|
|
BW-180C ([D-Ala2, D-Leu5]-Enkephalin; DADLE) is an δ opioid receptor (DOR) agonist, which belongs to the enkephalin family. Neuroprotective agent. BW-180C reversibly inhibits cellular transcription in neurons without causing cell injury .
|
-
- HY-P1334
-
-
- HY-P2669
-
-
- HY-P10203
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
|
-
- HY-P1333A
-
|
|
Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
|
Neurological Disease
|
|
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
|
-
- HY-P2021
-
-
- HY-P10672
-
-
- HY-P1854
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
|
-
- HY-P0233
-
Melittin
Maximum Cited Publications
11 Publications Verification
|
Phospholipase
|
Inflammation/Immunology
Cancer
|
|
Melittin is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2 .
|
-
- HY-P0233A
-
Melittin TFA
Maximum Cited Publications
11 Publications Verification
|
Phospholipase
|
Infection
Cancer
|
|
Melittin TFA is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2 .
|
-
- HY-P10008
-
|
|
Cathepsin
|
Cancer
|
|
Cathepsin D/E Substrate, Fluorogenic, 11 amino acid peptide, is a selective substrate for cathepsins D and E. Cathepsin D/E Substrate, Fluorogenic does not act as a substrate for cathepsins B, H, or L .
|
-
- HY-P3278
-
|
|
Proton Pump
|
Metabolic Disease
|
|
Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
- HY-118534
-
|
BRN-2209058
|
Peptides
|
Endocrinology
|
|
Cyclobutyrol is a potent choleretic agent. Cyclobutyrol also inhibits biliary lipid secretion. Cyclobutyrol induces choleretic is unrelated to bile acids. Cyclobutyrol and bile acids do not compete for the hepatobiliar transport mechanisms[1]
|
-
- HY-P5074
-
|
|
GCGR
|
Metabolic Disease
|
|
GRPP (human) is a 30 amino acid Gcg-derived peptide. GRPP (human) causes slight increases in plasma insulin and decreases in plasma glucagon. GRPP (human) does not affect insulin secretion in rat islets .
|
-
- HY-P10210
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Paenilagicin is a Gram-positive active antibiotic with a unique diphosphorylated prenyl binding mechanism that does not induce drug resistance. Paenilagicin exhibits a MIC value of 2 μg/mL against multidrug-resistant Gram-positive bacteria .
|
-
- HY-P2222
-
-
- HY-P3278A
-
|
|
Proton Pump
|
Metabolic Disease
|
|
Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
- HY-P0190A
-
|
|
Potassium Channel
|
Others
|
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .
|
-
- HY-P10107
-
|
|
Peptides
|
Others
|
|
TAT-PAK18 R192A is an inactive Tat-Pak peptide. TAT-PAK18 R192A does not have any effect in the translocation of Rac1 triggered by any of the interrogated proteins .
|
-
- HY-P10333
-
-
- HY-P2222A
-
-
- HY-P4114
-
|
|
HIV
|
Others
|
|
TAT-NSF700scr consists the intact TAT domain and glycine linker, followed by the NSF amino acids in a random order. TAT-NSF700scr is used as a control peptide that does not inhibit SNAREmediated exocytosis .
|
-
- HY-P10101
-
|
APTscr
|
Peptides
|
Others
|
|
APT STAT3, scrambled (APTscr), a control peptide of STAT3-specific aptide (APTSTAT3), does not bind STAT3. APT STAT3, scrambled contains the same trpzip scaffold but with a scrambled sequence in the target-binding site .
|
-
- HY-P0190
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels .
|
-
- HY-P5786
-
-
- HY-12290
-
|
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
|
-
- HY-P1711
-
|
|
Peptides
|
Cardiovascular Disease
|
|
L 366763 is a potent peptide that acts as a fibrinogen receptor antagonist, preventing collagen-induced platelet aggregation and adhesion. L 366763 inhibits platelet deposition and maintains blood flow in a baboon thrombosis model, significantly prolonging bleeding time. L 366763 has antithrombotic efficacy, whereas recombinant LAPP does not have the same effect .
|
-
- HY-12290A
-
|
RGDS peptide TFA; Fibronectin tetrapeptide TFA
|
Integrin
|
Inflammation/Immunology
|
|
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1 .
|
-
- HY-P1136B
-
-
- HY-P5422
-
|
|
Calcium Channel
|
Others
|
|
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
|
-
- HY-P10536
-
|
|
Bacterial
|
Infection
|
|
Temporin SHF is a broad-spectrum antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria and yeasts, but does not have hemolytic activity. Temporin SHF disrupts the acyl chain stacking of anionic lipid bilayers, leading to cracks and disintegration of microbial membranes. Temporin SHF can be used in the development of antimicrobial drugs .
|
-
- HY-P1136C
-
-
- HY-P3463
-
|
GLP-1 (human)
|
GCGR
|
Metabolic Disease
Inflammation/Immunology
|
|
Beinaglutide is a human GLP-1 polypeptide that shares almost 100% homology with human GLP-1 (7–36). Beinaglutide displays does-dependent effects in glycemic control, inhibiting food intake and gastric empty and promoting weight loss. Beinaglutide has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH) .
|
-
- HY-P10640
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
[Sar1,Thr8]-Angiotensin II is a potent angiotensin II antagonist. [Sar1,Thr8]-Angiotensin II does not alter cardiac performance. [Sar1,Thr8]-Angiotensin II might be safe for patients with cardiac disease .
|
-
- HY-P10579
-
|
|
Ephrin Receptor
|
Cancer
|
|
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .
|
-
- HY-P2434
-
|
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
Cancer
|
|
AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research .
|
-
- HY-P2294
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
|
-
- HY-P2294A
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
|
-
- HY-P10281
-
|
|
Bacterial
|
Infection
|
|
RW3 is a small cationic hexapeptide with amphiphilic properties. RW3 targets the plasma membrane of bacteria and works by inhibiting cell respiration and cell wall synthesis. RW3 shows high biological activity against gram-positive bacteria and does not show significant cytotoxic or hemolytic effects in previous studies. RW3 quickly kills 97% of the initial colony forming units (CFU) within 10 minutes at twice the minimum inhibitory concentration (MIC). RW3 can be used in antimicrobial and antifungal studies .
|
-
- HY-P5836
-
|
|
Interleukin Related
Bacterial
Enterovirus
|
Inflammation/Immunology
|
|
Citrullinated LL-37 1cit is a citrullinated LL-37 (HY-P1222) peptide. Citrullinated LL-37 1cit does not alter the antiviral effect of LL-37 toward human rhinovirus. Citrullinated LL-37 1cit shows antibacterial activity toward S. aureus. Citrullinated LL-37 1cit causes a reduction in the levels of IL-8, CCL5, and IL-6 mRNA induced by RV1B .
|
-
- HY-P5189A
-
|
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Others
|
|
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .
|
-
- HY-P10420
-
|
|
CD47
Interleukin Related
|
Cancer
|
|
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
|
-
- HY-106178
-
PMX-53
4 Publications Verification
3D53
|
Complement System
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects .
|
-
- HY-P5357
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)
|
-
- 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.)
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99706
-
|
AK 117
|
CD47
Interleukin Related
|
Cancer
|
|
Ligufalimab (AK 117) is a humanized IgG4 anti-CD47 monoclonal antibody. Ligufalimab does not induce RBC hemagglutination, and induces phagocytosis. Ligufalimab shows anti-tumor activity .
|
-
- HY-P9924
-
|
LY2439821
|
Interleukin Related
|
Inflammation/Immunology
|
|
Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis .
|
-
- HY-P9948
-
|
Campath-IH
|
Apoptosis
|
Cancer
|
|
Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research .
|
-
- HY-P99045
-
|
|
ADC Antibody
TROP2
|
Cancer
|
|
Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab is used for the synthesis of antibody-drug conjugates (ADC) drugs. Antibody-drug conjugates with sacituzumab (sacituzumab govitecan) (HY-132254) targeting TROP-2 have been approved for the field of triple-negative breast cancer .
|
-
- HY-P990090
-
|
CBP-201
|
Interleukin Related
|
Inflammation/Immunology
|
|
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
|
-
- HY-P990005
-
|
|
Inhibitory Antibodies
|
Others
|
|
Mouse IgG2a Fc, Isotype Control, is a Fc fragment of mouse IgG2a only and does not contain the Fab fragments. The molecular mass is about 34 kDa.
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1745
-
-
-
- HY-122365
-
-
-
- HY-18963
-
-
-
- HY-N6861
-
-
-
- HY-N12992
-
-
-
- HY-N8659
-
-
-
- HY-122367
-
-
-
- HY-117818
-
-
-
- HY-N1272
-
-
-
- HY-119874
-
-
-
- HY-P0190
-
-
-
- HY-124257
-
-
-
- HY-N8278
-
-
-
- HY-N8537
-
-
-
- HY-114252
-
-
-
- HY-N12540
-
|
MGDG
|
Structural Classification
Natural Products
other families
Source classification
Oplismenus burmannii
Plants
|
Others
|
|
Monogalactosyldiacylglycerol (MGDG) is a polar lipid that does not form a bilayer and is found, for example, in the chloroplast thylakoid of aerobic photosynthetic organisms. Monogalactosyldiacylglycerol lacks charge and is highly unsaturated, which provides a fluid environment that facilitates the diffusion process of electron transfer in photosynthesis and may be used in the packaging of natural proteins. The galactolipid Monogalactosyldiacylglycerol has anti-inflammatory effects in vivo ..
|
-
-
- HY-Z0283
-
-
-
- HY-163742
-
-
-
- HY-N2574
-
-
-
- HY-N8264
-
-
-
- HY-N0990
-
|
|
Anthraquinones
Source classification
Morinda citrifolia Linn.
Rubiaceae
Plants
|
Others
|
|
1,5,15-Trimethylmorindol is an anthraquinone isolated from the leaves of Morinda citrifolia. 1,5,15- trimethylmorindol (25 μg/mL) does not show significant cytotoxic activity on the human T-cell leukemia cell line, Jurkat, by itself but it shows cytotoxicity (IC50 14.5-15.0 μg/mL) when combined with 0.5-1.5 μg/mL of TRAIL in the cell proliferation assay .
|
-
-
- HY-126833A
-
-
-
- HY-114252R
-
|
|
Structural Classification
Source classification
Plants
Brassicaceae
Steroids
Erysimum cheiranthoides Linn.
|
Na+/K+ ATPase
|
|
Strophanthidin (Standard) is the analytical standard of Strophanthidin. This product is intended for research and analytical applications. Strophanthidin is a naturally available cardiac glycoside . Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal . Strophanthidin increases both diastolic and systolic intracellular Ca2+ concentration .
|
-
-
- HY-Z0283R
-
-
-
- HY-N2574R
-
|
|
Tribulus terrester Linn.
Structural Classification
Zygophyllaceae
Source classification
Plants
Steroids
|
Glucosidase
|
|
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
-
- HY-117730
-
|
Antibiotic 1063Z
|
Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
|
Antibiotic
|
|
Pulvomycin (Antibiotic 1063Z) is an antibiotic with protein biosynthesis inhibitory activity. Pulvomycin is able to block protein biosynthesis in Bacillus brevis grown in cells. Pulvomycin is highly sensitive to poly(Phe) synthesis in cell-free systems. Pulvomycin does not affect the transfer of phenylalanine to tRNA. Studies have shown that the target of Pulvomycin is the elongation of the polypeptide chain. Pulvomycin can also prevent the formation of a ternary complex between the elongation factor Tu, GTP and aminoacyl-tRNA .
|
-
-
- 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-16940
-
-
-
- HY-W747104
-
|
|
Structural Classification
Natural Products
Animals
Source classification
|
Others
|
|
(9E)-Tetradecen-1-ol is a pheromone that has no significant sexual attraction when used alone and can be secreted from the abdomen of the female Bertha armyworm moth (Mamestra configurata (Walker)). Isolate in tip extract to get in isolate. Another pheromone (Z)-11-hexadecen-1-ol was also isolated at the same time. Only when the two pheromones are mixed do they show male attraction (the ratio of C16:C14 in the mixture is about 19:1). optimal) .
|
-
-
- HY-N6785
-
Okadaic acid
Maximum Cited Publications
11 Publications Verification
|
Structural Classification
Animals
Ketones, Aldehydes, Acids
Marine natural products
Source classification
Other marine organisms
|
Phosphatase
Apoptosis
|
|
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
|
-
-
- HY-N6785R
-
|
|
Structural Classification
Animals
Ketones, Aldehydes, Acids
Marine natural products
Source classification
Other marine organisms
|
Phosphatase
Apoptosis
|
|
Okadaic acid (Standard) is the analytical standard of Okadaic acid. This product is intended for research and analytical applications. Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
|
-
-
- HY-N7402
-
|
|
Structural Classification
Natural Products
Animals
Source classification
|
Others
|
|
Hexyl hexanoate is a fruit aroma component with potential food and beverage additive activity. Hexyl hexanoate is found in alcoholic beverages and is used to blend fruit flavors. Hexyl hexanoate is present in many fruits, Parmesan cheese, alcoholic beverages, and black tea. Hexyl hexanoate is a volatile component produced as a result of fruit ripening. Toxicity assessments of hexyl hexanoate showed that it is not mutagenic and that exposure is below safety thresholds for repeated dose, reproduction, and local respiratory toxicity. Hexyl hexanoate is also below thresholds in skin sensitization assessments, and for phototoxicity and photosensitization, the results showed that it does not present a relevant risk. Hexyl hexanoate is considered non-persistent, non-bioaccumulative, and non-toxic according to the environmental criteria of the International Fragrance Association .
|
-
-
- HY-W008820R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endocrine diseases
Nervous System Disorder
Endogenous metabolite
|
Endogenous Metabolite
|
|
Glutaric acid (Standard) is the analytical standard of Glutaric acid. This product is intended for research and analytical applications. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I .
In Vitro: Glutaric acid (GA) at concentrations of 1 and 2 mM is able to reduce TRAP measurement by up to 28% in a dose-dependent manner (β=0.77; P<0.001). Furthermore, a significantly inverse correlation is also verified between chemiluminescence and TRAP (β=0.81; P<0.001). Glutaric acid does not alter the activities of Cat and SOD, but strongly inhibits (up to 46%) the activity of GPx even at the lower concentration used (0.5 mM). It is observed that the metabolite inhibits this activity in a dose-dependent manner at concentrations as low as 0.05 mM .
|
-
-
- HY-30004
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
|
Endogenous Metabolite
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
-
- HY-B2167R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endogenous metabolite
Cardiovascular System Disorder
|
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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- HY-N7091S2
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Atrazine-d5 is deuterium labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
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- HY-50683S
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JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
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- HY-N7091S
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Atrazine- 15N is the 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
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- HY-B1978S
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Iprodione-d5 is the deuterium labeled Iprodione[1]. Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective[2].
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- HY-N7091S1
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Atrazine- 13C3, 15N3 is the 13C-labeled and 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
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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-116423
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Alkynes
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JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 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-151691
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Tetrazine
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Trisulfo-Cy3 Methyltetrazine is a click chemistry reagent containing an methyltetrazine group. Methyltetrazine-activated Cy3 probe reacts with TCO-containing compounds via an Inverse-Electron-Demand Diels-Alder reaction to form a stable covalent bond and does not require Cu-catalyst or elevated temperatures .
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- HY-116423A
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Alkynes
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JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) 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-145749
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Alkynes
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PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
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- HY-W591424
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mPEG-SC (MW 2000); mPEG-Succinimidyl ester (MW 2000)
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Polymers
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m-PEG-NHS ester (MW 2000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
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- HY-157745
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mPEG-SC (MW 40000); mPEG-Succinimidyl ester (MW 40000)
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Polymers
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m-PEG-NHS ester (MW 40000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects .
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- HY-160046
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Aptamers
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AS2 sodium is an ssDNA aptamer (Kd: 0.7 nM) for prostate-specific antigen (PSA). AS2 sodium does not bind non-specifically to the anti-target and has the potential to be used in diagnostic systems for prostate cancer detection .
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- HY-142981
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DODA
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Cationic Lipids
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Dioctadecylamine (DODA) is a secondary amine that has been shown to self-organize in plate-like structures in aqueous solution. Dioctadecylamine exhibits sufficiently hydrophobic properties of nanoparticles and good dispersibility in nonpolar solvent. Dioctadecylamine does not form a monolayer above pH 3.9 .
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- HY-155909
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mPEG-SC (MW 3400); mPEG-Succinimidyl ester (MW 3400)
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Polymers
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m-PEG-NHS ester (MW 3400) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
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- HY-155909A
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mPEG-SC (MW 1000); mPEG-Succinimidyl ester (MW 1000)
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Polymers
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m-PEG-NHS ester (MW 1000) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
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- HY-155909B
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mPEG-SC (MW 550); mPEG-Succinimidyl ester (MW 550)
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Polymers
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m-PEG-NHS ester (MW 550) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
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- HY-155909C
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mPEG-SC (MW 350); mPEG-Succinimidyl ester (MW 350)
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Polymers
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m-PEG-NHS ester (MW 350) can be used to modify active molecules and improve their antigenicity, immunogenicity, and help prepare injection preparations. The modification of serine protease lumbrokinase (LK) by m-PEG-NHS ester does not affect its strong fibrinolytic and thrombolytic activities, and has good application prospects.
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- HY-147071
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DAPE
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Phospholipids
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1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine (DAPE) is a phospholipid phosphatidylethanolamine. Unlike other phospholipid phosphatidylethanolamines, 1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine has no significant effect on protein phosphatase PP2A activity and does not inhibit insulin-stimulated GLUT4 translocation .
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- HY-160045
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Aptamers
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AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
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- HY-143202
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Phospholipids
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DPhPC is a derivative of phosphatidylcholine (PC) used to synthesize bilayer vesicle phospholipids. DPhPC bilayer membranes do not leak ions in the absence of pores or ion channels, so they are often used to study the activity of ion channels and the regulation of membrane potential. Nanoliposomes (NTG) prepared based on DPhPC can improve the bioavailability of nitric oxide (NO) and have effective anti-inflammatory effects .
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- HY-153808A
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Montanide ISA-51
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Adjuvant
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Incomplete Freund's adjuvant (IFA) (Montanide ISA-51) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund. Incomplete Freund's adjuvant (IFA) does not contain inactivated tuberculosis bacilli and consists of petroleum jelly containing lanolin. Incomplete Freund's adjuvant (IFA) induces high antibody titers and long-lasting effector T cell responses with no long-term effects on collagen disease, tumors, or death. Complete Freund's adjuvant (CFA) (HY-153808) is another type of Freund's Adjuvant that stimulates a stronger immune response .
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- HY-153845
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Aptamers
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RNA Aptamer Broccoli (sodium) is a 49-nt-long aptamer that is substantially shorter than Spinach and Spinach2 and exhibits bright green fluorescence upon binding DFHBI or DFHBI-1T (soluble analogs of the fluorophore of green fluorescent protein). RNA Aptamer Broccoli (sodium) can be used to visualize RNA expression or localization in live cells. In vitro Broccoli exhibits a similar high folding efficiency as Spinach2, but exhibits markedly lower dependence on magnesium for folding and increased thermostability. Additionally, unlike Spinach2, Broccoli does not require the use of a tRNA scaffold to promote its folding in vivo.
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- HY-153843
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Aptamers
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RNA Aptamer Corn (sodium) is a 28-nt-long aptamer that is substantially shorter than Spinach and Spinach2 and exhibits bright red fluorescence upon binding DFHO (a soluble analog of the intrinsic fluorophore of red fluorescent protein), RNA Aptamer Corn (sodium) can be used to visualize RNA expression or localization in live cells which have been soaked with chromophores. The Corn-DFHO does not become appreciably cytotoxic when illuminated. And most importantly, Corn-DFHO exhibits markedly increased photostability compared to other aptamer-chromophore complexes both in vitro and in vivo. (36 nt Corn construct: 5'-GGCGCGAGGAAGGAGGUCUGAGGAGGUCACUGCGCC-3'; A 36-nt RNA construct, comprised of the 28-nt minimal Corn sequence extended proximally with a 4 base-pair stem.)
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