Search Result
Results for "
ICR
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-19336
-
|
Epigenetic Reader Domain
|
Cancer
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BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe .
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-
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- HY-151563A
-
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Deubiquitinase
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Cancer
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OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
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- HY-160926
-
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Glutathione S-transferase
|
Cancer
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16-Oxocafestol enhances levels of glutathione S-transferase (GST) and tissue sulfhydryl in liver and in small bowel mucosa .
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-
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- HY-161539
-
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Opioid Receptor
|
Neurological Disease
|
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-115826
-
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Others
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Cancer
|
AB-163 is an alkylating agent with anti-tumor activity. AB-163 exerts LD50s of 198 (p.o.) and 159 (i.p.) mg/kg in ICR/Ha male mice and can be utilized in cancer research .
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- HY-163315
-
|
Keap1-Nrf2
AMPK
|
Metabolic Disease
|
YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active .
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-
- HY-162485
-
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Dengue virus
Virus Protease
|
Infection
|
DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
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- HY-158365
-
|
LRRK2
|
Neurological Disease
|
LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .
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- HY-162408
-
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Protease Activated Receptor (PAR)
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Others
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PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min .
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-
-
- HY-162409
-
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Protease Activated Receptor (PAR)
|
Others
|
PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min .
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-
-
- HY-161523
-
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Xanthine Oxidase
URAT1
|
Metabolic Disease
|
XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model .
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- HY-161723
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Dopamine Transporter
CDK
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Neurological Disease
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LH2-051 is a lysosome-enhancing lead compound, which promotes the lysosome biogenesis and the Aβ aggregate clearance through dopamine transporter-cyclin-dependent kinase 9-transcription factor EB (DAT-CDK9-TFEB) pathway. LH2-051 exhibits good pharmacokinetic characteristics in mouse models. LH2-051 is potential for ameliorating Aleheimer’s Disease .
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- HY-19126
-
|
Platelet-activating Factor Receptor (PAFR)
|
Infection
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CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
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- HY-120843
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Endothelin Receptor
|
Cardiovascular Disease
|
WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases .
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- HY-W008151
-
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Mitochondrial Metabolism
|
Metabolic Disease
|
Diphenyl Phosphate inhibits growth and energy metabolism in zebrafish and mice in a sex-specific manner. Diphenyl Phosphate can inhibit the activity of SDH (respiratory complex II), reduce the expression of CPT1 and disrupts the integrity of the mitochondrial membrane. Diphenyl Phosphate may be used in research on metabolic diseases .
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-
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- HY-162407
-
|
Btk
|
Cancer
|
I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively .
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-
-
- HY-163879
-
|
Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
|
Neurological Disease
|
hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
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- HY-162764
-
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Androgen Receptor
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Cancer
|
Androgen receptor degrader-5 (compound 14k) exhibits promising properties, including superior androgen receptor degradation activity and antiproliferative activity .
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-
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- HY-118803
-
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Factor Xa
|
Others
|
AS1468240 is an orally active inhibitor for anticoagulant factor Xa (fXa), that inhibits human fXa with IC50 of 8.7 nM. AS1468240 prolongs the coagulation time in mice .
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-
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- HY-129246
-
|
DNA/RNA Synthesis
|
Cancer
|
Cytembena is inhibitor for replicative DNA synthesis, purine synthesis and tetrahydrofolate formylase activity. Cytembena ameliorates ovarian or breast cancer, relieves the pain from skeletal metastases .
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- HY-146615
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TAM Receptor
|
Cancer
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Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
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-
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- HY-152031
-
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Amyloid-β
|
Neurological Disease
|
Glutaminyl Cyclase Inhibitor 5 (Compound 71) is a potent and selective human glutaminyl cyclase (hQC) inhibitor with an IC50 of 3.2 nM .
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-
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- HY-W012977
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-
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- HY-161643
-
|
Cholinesterase (ChE)
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
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-
- HY-163505
-
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Bacterial
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Others
|
Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
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-
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- HY-139414
-
|
Interleukin Related
p38 MAPK
ERK
Apoptosis
|
Inflammation/Immunology
|
Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis .
|
-
-
- HY-146619
-
|
Amyloid-β
Serotonin Transporter
|
Neurological Disease
|
RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression .
|
-
-
- HY-146883A
-
|
Filovirus
|
Infection
|
As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC50s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety .
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-
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- HY-147943
-
|
PROTACs
Btk
|
Cancer
|
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 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-126383
-
|
Bacterial
|
Infection
Others
Inflammation/Immunology
Cancer
|
Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research .
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-
-
- HY-121152
-
-
-
- HY-161627
-
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NF-κB
|
Inflammation/Immunology
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Anemoside A3-methyl 6-aminohexanoate (Compound A3-6) is a derivative of Pulchinenoside C (Anemoside B4) (HY-N0205). Anemoside A3-methyl 6-aminohexanoate inhibits pyruvate carboxylase (PC) with an IC50 of 0.058 μM, reprograms macrophage function, and alleviates DSS-induced colitis through inhibition of the NF-κB and NLRP3 inflammasome pathway. Anemoside A3-methyl 6-aminohexanoate exhibits a moderate in vivo pharmacokinetic characters compared with Anemoside B4 .
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-
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- HY-126876
-
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Apoptosis
AMPK
Reactive Oxygen Species
|
Cancer
|
GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
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-
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- HY-P10302A
-
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GLP Receptor
|
Metabolic Disease
|
GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-14849
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Razupenem; SM 216601; SMP 601
|
Antibiotic
Bacterial
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Others
|
PTZ601 (SMP 601) is an antibiotic, which inhibits the gram-positive bacteria, including the Vancomycin (HY-B0671)-resistant Enterococcus faecium (VREF) and Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). PTZ601 exhibits antimicrobial activity in infected mouse models .
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-
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- HY-159088
-
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Opioid Receptor
|
Neurological Disease
|
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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- HY-143586
-
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CDK
|
Cancer
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CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models .
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-
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- HY-146468
-
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Dipeptidyl Peptidase
GPR119
Potassium Channel
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Metabolic Disease
|
DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research . DPP-4/GPR119 modulator 1 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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-
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- HY-162633
-
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Deubiquitinase
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Cancer
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USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
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- HY-148013
-
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Beta-secretase
NF-κB
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Neurological Disease
|
K284-6111 is an orally active inhibitor for protein chitinase 3-like 1 (CHI3L1). K284-6111 reduces the expression of inflammatory proteins such as iNOS, COX-2, GFAP, and Iba-1, inhibits β-secretase and NF-κB, and suppresses Aβ production. K284-6111 ameliorates the Aβ1–42-induced mice memory impairment, and can be used in research about Alzheimer’s Diseases .
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-
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- HY-161893
-
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Bacterial
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Infection
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Anti-MRSA agent 15 (Compound 9o10) exhibits antibacterial activity, that inhibits methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 0.0625 μg/mL. Anti-MRSA agent 15 exhibits low hemolysis and low cytotoxicity. Anti-MRSA agent 15 exhibits anti-infective in mice .
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-
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- HY-164384
-
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PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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- HY-163345
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
Pharmacokinetic Analysis ICR Male Mice
药代动力学分析
Plasma |
Intravenous Administration |
Intraperitoneal Administration |
Tmax (h) |
0.08 |
0.25 |
T1/2 (h) |
0.77 |
1.06 |
Cmax (ng/mL) |
33.07 |
156.44 |
AUClast (ng·h/mL) |
28.31 |
143.27 |
CL (L/h/kg) |
41.61 |
- |
Vss (L/kg) |
32.43 |
- |
MRT (h) |
0.79 |
0.93 |
F (%) |
50.60 |
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-
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- HY-Y0946
-
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
Acetamide is used as an intermediate in the synthesis of methylamine, thioacetamide, and insecticides, and as a plasticizer in leather, cloth and coatings. Acetamide has carcinogenicity. Acetamide derivatives may has antioxidant activity and potential anti-inflammatory activity. Acetamide holds promise for research in the fields of anti-inflammatory and cancer studies .
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-
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- HY-115996
-
|
Others
|
Cancer
|
Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity .
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-
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- HY-145845
-
|
HDAC
Monoamine Oxidase
|
Neurological Disease
|
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease .
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-
-
- HY-158113
-
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Histone Acetyltransferase
PROTACs
|
Cancer
|
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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-
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- HY-163923
-
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Apoptosis
|
Cancer
|
Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg) .
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-
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- HY-Y0946R
-
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Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
Acetamide (Standard) is the analytical standard of Acetamide. This product is intended for research and analytical applications. Acetamide is used as an intermediate in the synthesis of methylamine, thioacetamide, and insecticides, and as a plasticizer in leather, cloth and coatings. Acetamide has carcinogenicity. Acetamide derivatives may has antioxidant activity and potential anti-inflammatory activity. Acetamide holds promise for research in the fields of anti-inflammatory and cancer studies .
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- HY-146715
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
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IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
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- HY-146672
-
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Itk
|
Cancer
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
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- HY-147395
-
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GPR52
|
Neurological Disease
|
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .
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- HY-143414
-
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Beta-lactamase
Bacterial
|
Infection
|
Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL .
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- HY-P10435
-
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Dopamine Receptor
|
Neurological Disease
|
KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
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- HY-164595
-
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Hippo (MST)
Apoptosis
AMPK
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Metabolic Disease
|
IHMT-MST1-39 is an orally active inhibitor for MST kinase, with IC50 of 42 nM and 109 nM, for MST1 and MST2. IHMT-MST1-39 activates the AMPK signaling pathway in liver cells, reduces apoptosis of pancreatic β-cells. IHMT-MST1-39 ameliorates diabetes in Streptozotocin (HY-13753)-induced type 1 diabetes (T1D) mouse models .
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- HY-144658
-
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Factor Xa
|
Cardiovascular Disease
|
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
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- HY-149844
-
|
Fungal
|
Infection
|
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections .
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- HY-160761
-
|
Opioid Receptor
|
Inflammation/Immunology
|
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
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- HY-162600
-
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CDK
|
Inflammation/Immunology
|
CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases .
|
-
- HY-143434
-
|
FLT3
|
Cancer
|
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) .
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- HY-163403
-
|
VEGFR
|
Cardiovascular Disease
Cancer
|
VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-139414
-
|
Cell Assay Reagents
|
Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10302A
-
|
GLP Receptor
|
Metabolic Disease
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GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
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- HY-163315
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Keap1-Nrf2
AMPK
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Metabolic Disease
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YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active .
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- HY-P10435
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Dopamine Receptor
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Neurological Disease
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KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
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