Search Result
Results for "
dose-dependent
" in MedChemExpress (MCE) Product Catalog:
6
Biochemical Assay Reagents
26
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-P3462A
-
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CGRP Receptor
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Metabolic Disease
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Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies .
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-
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- HY-12289A
-
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VS-6063 hydrochloride; PF 04554878 hydrochloride
|
FAK
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Cancer
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Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
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-
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- HY-111408
-
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Deubiquitinase
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Cancer
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EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
|
-
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- HY-104073
-
-
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- HY-13809
-
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XL-139
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Smo
Apoptosis
|
Cancer
|
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BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM .
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-
-
- HY-100585
-
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Splitomycin
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HDAC
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Cancer
|
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Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD +-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM .
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-
-
- HY-10787
-
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H 376/95
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Thrombin
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Cardiovascular Disease
|
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Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics .
|
-
-
- HY-W042191
-
|
|
Fungal
Apoptosis
Caspase
Bcl-2 Family
MDM-2/p53
PARP
|
Infection
Cancer
|
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Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer .
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-
-
- HY-B0848
-
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Environmental Pollutants
Bacterial
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Infection
Metabolic Disease
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Tricyclazole is a pentaketone melanin biosynthesis inhibitor and a unique fungicide for controlling rice blast. Tricyclazole alters the structure and function of fungal cell walls, reduces fungal pathogenicity and penetration, and causes dose-dependent liver damage in animals .
|
-
-
- HY-B0163A
-
-
-
- HY-159989
-
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Epigenetic Reader Domain
|
Cancer
|
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UNC10142 (Compound 44) is a first-in-class small molecule antagonist of CHD1 that binds with an IC50 value of 1.7 μM. UNC10142 leads to a dose-dependent reduction in viability in PTEN-deficient prostate cancer cells .
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-
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- HY-142052
-
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5a(6)-Anhydrotetracycline
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Antibiotic
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Infection
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Anhydrotetracycline shows dose-dependent and potent inhibition of tetracycline destructases in vitro .
|
-
-
- HY-P3030
-
-
-
- HY-N0775
-
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7-Isocorynoxeine
|
5-HT Receptor
|
Neurological Disease
|
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Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
|
-
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- HY-P10032
-
-
-
- HY-137820
-
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DNA/RNA Synthesis
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Others
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Brr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC50 value of 1.3 μM .
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-
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- HY-118541
-
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Insecticide
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Others
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RH-5849 is an orally active agonist for non-steroidal ecdysteroid, which inhibits the larval growth of Plodia inferpuncteila in a dose-dependent manner. RH-5849 exhibits molting hormone activity .
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-
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- HY-103101
-
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5-HT Receptor
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Others
|
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LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .
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- HY-124597
-
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Ceramidase
|
Inflammation/Immunology
|
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ARN726 is a potent NAAA (N-acylethanolamine acid amidase) inhibitor with an IC50 of 0.073 µM. ARN726 decreases alcohol self-administration in a dose-dependent manner .
|
-
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- HY-135555
-
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5-CT
|
5-HT Receptor
|
Neurological Disease
|
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5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist . 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .
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- HY-B1914
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-
-
- HY-P3730
-
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CDK
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Cancer
|
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Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
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- HY-107164
-
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4-Hydroxythiomarinol C
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Antibiotic
Bacterial
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Infection
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Thiomarinol A (4-Hydroxythiomarinol C) is a potent antibiotic. Thiomarinol A is a hybrid of dithiolopyrrolone and marinolic acid. Thiomarinol A shows antimicrobial activity. Thiomarinol A inhibits MRSA IleRS in a dose-dependent with a Ki app value of 19 nM .
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-
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- HY-111317
-
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Sirtuin
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Metabolic Disease
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SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches .
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- HY-108436
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Phosphodiesterase (PDE)
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Cancer
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Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines .
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- HY-N5099
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Others
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Metabolic Disease
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N-Vanillyldecanamide, a capsaicinoid isolated from the fruits of Capsicum annuum, significantly reduced the radical length of Lactuca sativa seedling in a dose-dependent manner .
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- HY-123239
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GPR55
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Neurological Disease
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KLS-13019 is an orally active GPR55 receptor antagonist and a structural analogue of cannabidiol (CBD). It can prevent and reverse chemotherapy-induced peripheral neuropathy (CIPN) in a dose-dependent manner in rats .
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- HY-110241
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nAChR
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Neurological Disease
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Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .
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-
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- HY-121007
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Web2170
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Platelet-activating Factor Receptor (PAFR)
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Others
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Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guinea pigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
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- HY-N11922
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Others
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Neurological Disease
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Ipalbidine is an alkaloid extracted from ipomoea Hardwickki Hemsl. Ipalbidine has dose-dependent analgesic effects .
|
-
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- HY-103188
-
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Adenosine Receptor
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Neurological Disease
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PD81723 is an adenosine receptor binding enhancer. PD81723 enhances the inhibition of exogenous adenosine in a dose-dependent manner in hippocampal brain sections .
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-
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- HY-101595
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Drug Derivative
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Others
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RPH-2823, a basic triamterene derivative, induces a dose-dependent decrease in short-circuit current (SCC) and increase in transepithelial electrical resistance .
|
-
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- HY-B0163
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-
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- HY-158051
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PKC
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Neurological Disease
|
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CIDD-0072424 selectively inhibits Protein Kinase C-epsilon (PKCε) (Ki=54 nM). CIDD-0072424 reduces ethanol consumption and preference in a dose-dependent manner .
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-
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- HY-N6681
-
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Caspase
Bacterial
Apoptosis
Antibiotic
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Infection
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15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
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-
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- HY-107627
-
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Melanocortin Receptor
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Inflammation/Immunology
|
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MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
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-
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- HY-111143
-
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nAChR
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Metabolic Disease
|
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SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA) .
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-
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- HY-106347
-
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CR 2945
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Cholecystokinin Receptor
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Inflammation/Immunology
|
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Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity .
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- HY-P11126
-
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Bacterial
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Infection
|
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Mel4 is an antimicrobial peptide, exhibiting broad-spectrum antimicrobial activity. Mel4 can neutralize bacterial lipopolysaccharide in a dose-dependent manner. Mel4 can be used in the research and prevention of related bacterial infectious diseases (such as ocular infections) .
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-
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- HY-P2005
-
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Reactive Oxygen Species (ROS)
SOD
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Others
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Malformin C is an algicidal peptide can be isolated from Aspergillus and exhibits dose-dependent algicidal activity. Malformin C induces a significant increase in ROS levels in algal cells, resulting in impaired SOD activity and high production of MDA content .
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-
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- HY-146681
-
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PAK
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Cancer
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PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner .
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- HY-125615
-
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Glycoprotein VI
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Cardiovascular Disease
Others
|
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DMP 728 methanesulfonate is a platelet glycoprotein (GP) IIb/IIIa receptor antagonist. DMP 728 methanesulfonate shows dose-dependent antiplatelet and antithrombotic effects. DMP 728 methanesulfonate can be used in the study of effective antithrombotic agents in thromboembolic diseases of coronary and peripheral arteries .
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- HY-136676
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Renin
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Cancer
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Cgp 38560 methanesulfonate is a well-tolerated renin inhibitor. Cgp 38560 methanesulfonate caused a dose-dependent decrease in angiotensin II and plasma renin activity, and a dose-dependent increase in active renin.
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- HY-144818
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Apoptosis
Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia .
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- HY-146782
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EGFR
|
Cancer
|
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EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
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- HY-157533
-
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Bacterial
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Others
|
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AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .
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- HY-W127334
-
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Biochemical Assay Reagents
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Others
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N-Palmitoyl phosphatidylethanolamine (Tripelargonin) is endogenous lipid anorectic hormone, significantly reduces food intake in a dose-dependent manner
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-
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- HY-19539
-
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SOS1
Ras
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Cancer
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NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation .
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-
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- HY-117019
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COX
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Cancer
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LY150310 inhibits thromboxane synthase, cyclooxygenase, and thrombin activation. LY150310 inhibits spontaneous lung metastasis in a dose-dependent manner.
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-
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- HY-106091B
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CI 941 hydrochloride; DUP 94 hydrochloride
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DNA Alkylator/Crosslinker
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Cancer
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Losoxantrone hydrochloride (CI 941 hydrochloride) is a DNA-binding agent. Losoxantrone hydrochloride has broad-spectrum antitumour activity. Losoxantrone hydrochloride induces dose-dependent leukopenia .
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- HY-N8816
-
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NF-κB
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Inflammation/Immunology
|
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Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM .
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-
- HY-167872
-
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Cytochrome P450
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Others
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Bifeprofen, a cytochrome P450 2C9 (CYP2C9) inhibitor, exhibits dose-dependent inhibition (75 μM, 50%) .
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- HY-136644
-
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Calcium Channel
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Others
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PD-217014-methyl ester is an α?δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity, and its anti-hyperalgesic effect is dose-dependent.
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- HY-N1159
-
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NF-κB
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Inflammation/Immunology
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Teuclatriol is an NF-κB inhibitor can be isolated from salvia mirzayanii, has anti-inflammatory effects. Teuclatriol inhibits TNF-α secretion in a dose-dependent manner .
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- HY-136644A
-
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Calcium Channel
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Others
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PD-217014 is an α2δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity reactions. Its anti-allodynic effect is dose-dependent.
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- HY-W703398
-
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Drug Metabolite
|
Infection
|
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Monopropyl phthalate is a compound derived from the hydrolysis of Dipropyl phthalate (DPrP). Monopropyl phthalate is hydrolyzed to PA. DPrP shows significant dose-dependent toxic effects on K. brevis .
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- HY-P3731
-
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CDK
|
Cancer
|
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Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
|
-
- HY-122874
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-
- HY-121866
-
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Topoisomerase
|
Cancer
|
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Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25 μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
|
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- HY-P5921
-
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TsTx-Kα
|
Potassium Channel
|
Neurological Disease
|
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Tityustoxin-Kα (TsTx-Kα) is an inhibitor of potassium voltage-gated channels. Tityustoxin-Kα shows a dose-dependent block of the sustained outward current in cultured hippocampal neurons .
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-
- HY-118364
-
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RAR/RXR
|
Metabolic Disease
|
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AGN 190727 is a structural isomer of AGN 190121 and has no activating effect on RAR/RXR. AGN 190121 is a RAR-specific agonist that causes a dose-dependent increase in serum triglycerides, leading to hypertriglyceridemia.
|
-
- HY-N2383
-
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(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Glycosidase
|
Metabolic Disease
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
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-
- HY-169210
-
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Apoptosis
|
Cancer
|
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ECDD-S18 (compund ECDD-S18) induces apoptosis in a dose-dependent manner, effectively targets vacuolar ATPase (V-ATPase), and impairs lysosomal acidification .
|
-
- HY-116560
-
-
- HY-123767
-
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HBV
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Infection
|
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HEC72702 is a potent and orally active hepatitis B virus capsid inhibitor with an EC50 values of 0.039 µM. HEC72702 dose-dependently reduced HBV DNA in both the plasma and livers .
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-
- HY-12956B
-
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Prostaglandin F2β; PGF2β
|
Endogenous Metabolite
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Others
|
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(5R)-Dinoprost is a metabolite produced by cyclooxygenase metabolism of arachidonic acid. (5R)-Dinoprost (Prostaglandin F2β) induces dose-dependent release of hexose containing mucin .
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-
- HY-159885
-
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Apoptosis
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Cancer
|
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MG-B-28 is an inhibitor of BTLA-HVEM with an IC50 value of 906 nM. MG-B-28 promotes T-cell activation in a dose-dependent manner by blocking the BTLA-HVEM interaction .
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-
- HY-P1086
-
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Transmembrane Glycoprotein
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Others
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Cadherin Peptide, avian is a calcium-dependent glycoprotein. Cadherin Peptide, avian takes part in homophilic cell-cell adhesion and dose-dependently inhibits bovine brain microvessel endothelial cells (BBMECs) adhesion .
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- HY-119819
-
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Bacterial
Parasite
Antibiotic
|
Infection
|
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Psicofuramine a nucleoside antibiotic and has the inhibition of xanthosine 5'-phosphate aminase. Psicofuranine also specifically inhibits GMP synthase, and interrupts parasite growth. Psicofuranine exhibits a dose-dependent inhibition of P. falciparum growth .
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-
- HY-122049
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-
- HY-121377
-
-
- HY-179113
-
-
- HY-144731
-
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HIV
|
Inflammation/Immunology
|
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gp120-IN-2 (compound 4i) is a potent HIV-1 gp120 inhibitor with an IC50 of 7.5 µM and CC50 of 112.93 µM. gp120-IN-2 shows anti-HIV-1 activity. gp120-IN-2 shows cytotoxicity in a dose dependent manner in SUP-T1 cells .
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-
- HY-10845
-
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Bacterial
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Others
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CGI-17341 is a 5-nitroimidazole antibacterial agent that has the activity of inhibiting sensitive and multidrug-resistant strains of Mycobacterium tuberculosis in vitro and prolonging the survival time of mice infected with Mycobacterium tuberculosis in vivo in a dose-dependent manner.
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-
- HY-121931
-
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Lipoxygenase
|
Cancer
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AA863 is a 5-lipoxygenase inhibitor with activity in inhibiting the proliferation of human glioma cells. AA863 exhibits significant and dose-dependent inhibitory effects in monolayer cultured glioma cells with an IC50 of 9.0 micromolar .
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- HY-137831
-
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Apoptosis
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Cancer
|
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TLBC, a boronic-chalcone derivative, shows a dose-dependent inhibition with IC50 values of 5.5-25.5 μM in various glioma cell lines. TLBC induces apoptosis independent of changes to the tumor suppressor p53 .
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- HY-114850A
-
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Prostaglandin F2β tromethamine; PGF2β tromethamine
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Endogenous Metabolite
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Others
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(5R)-Dinoprost tromethamine (Prostaglandin F2β tromethamine) is a metabolite produced by the metabolism of arachidonic acid cyclooxygenase. (5R)-Dinoprost tromethamine induces dose-dependent release of hexosaccharide containing mucin .
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- HY-111181
-
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Sodium Channel
Potassium Channel
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Metabolic Disease
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A 56234 is an orally active benzisoxazole diuretic. A 56234 produces dose-dependent diuresis, sodium and chloride excretion, significantly increases potassium excretion, and also slightly increases calcium, magnesium, and total protein excretion. A 56234 has shown uricosuric effects in animal studies
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- HY-149856
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research .
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- HY-B0163AR
-
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Reference Standards
Adrenergic Receptor
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Neurological Disease
Endocrinology
|
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Detomidine (hydrochloride) (Standard) is the analytical standard of Detomidine (hydrochloride). This product is intended for research and analytical applications. Detomidine hydrochloride, an imidazole derivative, is a potent α2-adrenergic agonist. Detomidine hydrochloride produces dose-dependent analgesic effects .
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- HY-157124
-
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Tyrosinase
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Metabolic Disease
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Tyrosinase-IN-19 (compound 9) is a competitive tyrosinase inhibitor. Tyrosinase-IN-19 has strong antioxidant activities against ROS, ABTS+, and DPPH radicals. Tyrosinase-IN-19 suppresses tyrosinase expression in a dose-dependent manner .
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- HY-12289AR
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VS-6063 hydrochloride (Standard); PF 04554878 hydrochloride (Standard)
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FAK
Reference Standards
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Cancer
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Defactinib (hydrochloride) (Standard) is the analytical standard of Defactinib (hydrochloride). This product is intended for research and analytical applications. Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
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- HY-167858
-
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Thrombin
|
Cardiovascular Disease
|
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LK-732 is a thrombin inhibitor with anti-thrombotic activity.LK-732 has a dose-dependent inhibition of hypercoagulability in the model, with an IC50 of 1.3 mg/kg. LK-732 can be used in cardiovascular and cerebrovascular research .
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- HY-114748
-
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Bacterial
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Infection
|
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AHU1 is a compound that inhibits the expression of Shiga toxin type 2 in Escherichia coli O157:H7, demonstrating a dose-dependent reduction in toxin activity by interfering with the SOS response through its effects on RecA.
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- HY-143468
-
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Apoptosis
MEK
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Cancer
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MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
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- HY-14919A
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MN-029
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Microtubule/Tubulin
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Cancer
|
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Denibulin (MN-029) hydrochloride is an anti-angiogenic agent with anticancer activity. It can cause rapid closure of blood vessels in solid tumors and lead to dose-dependent killing of tumor cells, effectively enhancing the antitumor effects of radiation and cisplatin chemotherapy .
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- HY-N0775R
-
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7-Isocorynoxeine (Standard)
|
Reference Standards
5-HT Receptor
|
Neurological Disease
|
|
Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
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- HY-B1914R
-
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Reference Standards
Mitochondrial Metabolism
|
Neurological Disease
|
|
Tebufenpyrad (Standard) is the analytical standard of Tebufenpyrad. This product is intended for research and analytical applications. Tebufenpyrad can induce mitochondrial dysfunction and oxidative damage. Tebufenpyrad induces dose-dependent cell death on N27 cells, with an EC50 value of 3.98 μM .
|
-
- HY-168920
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
NSD-IN-4 (Compound A8) is a potent and an orally active NSD3 inhibitor. NSD-IN-4 induces Apoptosis in a dose-dependent manner. NSD-IN-4 exhibits significant antitumor effects against lung squamous carcinoma .
|
-
- HY-N4209
-
|
|
Others
|
Cardiovascular Disease
|
|
3α-Dihydrocadambine is a natural product isolated from the heartwoods of Anthocephalus cadamba.3α-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats .
|
-
- HY-118683
-
|
|
Potassium Channel
|
Others
|
|
KR-31378 is a neuroprotectant with dose-dependent pharmacokinetic properties and relevant activity in rats. After intravenous and oral administration of KR-31378 in rats, its pharmacokinetic parameters showed dose-dependent changes, such as decreased clearance with increasing doses, good oral absorption, and comparable AUCs for intravenous and oral administration at different doses.
|
-
- HY-134192
-
-
- HY-106091
-
|
CI 941; DuP-941; Biantrazole
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Losoxantrone (CI 941) is a DNA-binding agent. Losoxantrone has broad-spectrum antitumour activity. Losoxantrone induces dose-dependent leukopenia .
|
-
- HY-N11950
-
|
|
Others
|
Others
|
|
N-Vanillyloctanamide is a capsaicinoid that has the activity of inhibiting the root growth of plant seedlings. N-Vanillyloctanamide significantly reduces the root length of Lactuca sativa (seedling) in a dose-dependent manner .
|
-
- HY-P3730A
-
|
|
CDK
|
Cancer
|
|
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) acetate, a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
|
-
- HY-105334A
-
|
E-6006 citrate
|
Neurokinin Receptor
|
Neurological Disease
|
|
Dilopetine citrate is an inhibitor of substance P release. Dilopetine citrate dose-dependently reduces the vocalizing of isolated guinea pig pups. Dilopetine citrate shows good activity as an antidepressant .
|
-
- HY-182406
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
CU-2010 is a Serine protease inhibitor. In canine models, CU-2010 reduces blood loss after cardiac surgery in a dose-dependent manner and improves post-ischemic recovery .
|
-
- HY-N17528
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Triptohypol E is a triterpenoid compound and nitric oxide production inhibitor that can be isolated from the leaves of Rhododendron dauricum L. Triptohypol E inhibits nitric oxide production in LPS-stimulated macrophages in a dose-dependent manner .
|
-
- HY-19413
-
-
- HY-N17468
-
|
|
|
Neurological Disease
|
|
Neocrocin B is a carotenoid crocin. Neocrocin B inhibits L-Glutamic acid (HY-14608)-induced neuronal cell damage in a dose-dependent manner. Neocrocin B can be used in studies related to neuronal injury .
|
-
- HY-162153
-
|
|
FGFR
|
Cancer
|
|
CYY292 is an FGFR1 inhibitor that specifically targets the FGFR1/AKT/Snail pathway in GBM cells. CYY292 dose-dependently inhibits cancer cell proliferation, epithelial-mesenchymal transition, stemness, invasion, and migration in vitro .
|
-
- HY-171175
-
|
|
Ephrin Receptor
|
Cancer
|
|
UniPR500, a UniPR129 derivative, is a competitive EphA2 receptor antagonist with a Ki of 0.78 μM. UniPR500 dose-dependently reduces binding of biotinylated ephrin-A1 to EphA2 with an IC50 value of 1.1 μM .
|
-
- HY-P1235A
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-P5859
-
|
α-PMTX
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
α-Pompilidotoxin (α-PMTX) is a neurotoxin that can be obtained from the venom of Anoplius safnariensis. α-Pompilidotoxin reversibly and dose-dependently enhances excitatory postsynaptic currents (EPSCs). α-Pompilidotoxin is a useful tool in the field of neuroscience research .
|
-
- HY-116498
-
|
|
Others
|
Infection
|
|
Penigequinolone A is an alkaloid isolated from Penicillium. It is lethal to P. penetrans (LD50=100 mg/L) but has no effect on C. elegans at concentrations up to 1000 mg/L.1 Penigequinolone A also accelerates the root growth of rice seedlings in a dose-dependent manner.
|
-
- HY-13570B
-
|
|
Glucocorticoid Receptor
|
Others
|
|
Betamethasone acetate is a glucocorticoid with prenatal application for preventing respiratory distress syndrome (RDS) in premature infants. Betamethasone acetate exhibits dose-dependent effects on somatic and brain development in offspring when administered prenatally to pregnant rats. Betamethasone acetate can be used for the study of antenatal intervention .
|
-
- HY-P3100
-
|
|
Parasite
|
Infection
|
|
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC50 value of 34.5 μg/mL .
|
-
- HY-106363
-
|
L 654066
|
5 alpha Reductase
|
Others
|
|
MK-0963 is a steroidal 5α-reductase inhibitor. MK-0963 reduces serum dihydrotestosterone (DHT) concentrations in a dose-dependent manner. MK-0963 can be used for the study of dihydrotestosterone-related diseases such as benign prostate hyperplasia (BPH) .
|
-
- HY-P991222
-
|
|
Phosphatase
|
Cardiovascular Disease
|
|
AMG-529 is a humanized monoclonal antibody against ASGR1 that binds to ASGR1, blocks ligand binding, and causes a dose-dependent increase in ALP (a biomarker of ASGR1 inhibition). AMG-529 can be used for the research of cardiovascular diseases .
|
-
- HY-B1914S
-
-
- HY-W416440
-
|
ASL-8123 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Esmolol acid (ASL-8123) hydrochloride is a weak β-adrenergic receptor antagonist. Esmolol acid hydrochloride inhibits the heart rate and diastolic blood pressure response induced by Isoproterenol (HY-B0468) in a dose-dependent manner and can be used in studies of renal failure .
|
-
- HY-N11911
-
|
(-)-Verazine
|
Fungal
|
Infection
Neurological Disease
|
|
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases .
|
-
- HY-B1041A
-
|
Pimagedine; GER-11free base ; Aminoguanidinium
|
NO Synthase
Apoptosis
|
Endocrinology
|
|
Aminoguanidine (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine has antioxidant properties. Aminoguanidine can be used in diabetic nephropathy research .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-139692
-
|
|
EAAT
|
Neurological Disease
|
|
EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently .
|
-
- HY-P10032A
-
-
- HY-128431
-
|
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
|
|
Arochlor 1254 is a polychlorinated biphenyl (PCB) mixture with biphenyl and 54% chlorine. Aroclor 1254 reduced cell viability and induced overproduction of intracellular reactive oxygen species in a dose-dependent manner. Arochlor 1254 exposure reduces calcium homeostasis, osteoblast differentiation and bone formation .
|
-
- HY-P0262A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
|
|
Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
|
-
- HY-24366
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Quindoxin is an antibacterial and growth promoter, commonly used in the livestock industry. Quindoxin exhibits clear dose-dependent mutagenic activity against Salmonella typhimurium TA98 and TA100 strains. Quindoxin can cause DNA damage and has potential genotoxicity and carcinogenic risks .
|
-
- HY-175591
-
|
|
Photosensitizer
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Photosensitizer-7 is a endoplasmic reticulum (ER)-targeted photosensitizer (PS) (λab = 610 nm, λem = 622 nm). Photosensitizer-7shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells under light irradiation. Photosensitizer-7 exhibits dose-dependent cellular uptake and predominant colocalization with ER. Photosensitizer-7 induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis upon light irradiation in cells. Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice. Photosensitizer-7 can be used for the study of photodynamic anticancer applications .
|
-
- HY-181996
-
|
|
Btk
Caspase
Apoptosis
PARP
|
Cancer
|
|
BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies .
|
-
- HY-144448
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
|
-
- HY-118131
-
|
|
Ser/Thr Protease
|
Infection
|
|
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages .
|
-
- HY-15297
-
|
OPC-8212
|
Phosphodiesterase (PDE)
|
Infection
Cardiovascular Disease
|
|
Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research .
|
-
- HY-N5099R
-
|
|
Others
Reference Standards
|
Metabolic Disease
|
|
N-Vanillyldecanamide (Standard) is the analytical standard of N-Vanillyldecanamide (HY-N5099). This product is intended for research and analytical applications. N-Vanillyldecanamide, a capsaicinoid isolated from the fruits of Capsicum annuum, significantly reduced the radical length of Lactuca sativa seedling in a dose-dependent manner .
|
-
- HY-137111
-
|
|
5-HT Receptor
PERK
|
|
|
p-MPPF dihydrochloride is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF dihydrochloride can be used for neurological disease research .
|
-
- HY-N7583
-
|
|
Parasite
|
Infection
|
|
Norcaesalpinin E, a C-17-norcassane-type diterpene found in Caesalpinia crista, is a Plasmodium falciparum growth inhibitor with an IC50 of 90 nM. Norcaesalpinin E induces dose-dependent growth inhibition of Plasmodium falciparum. Norcaesalpinin E can be used for the research of malaria .
|
-
- HY-W288480
-
|
|
Apoptosis
|
Cancer
|
|
Trihexyl phosphate is an organophosphate flame retardant. Trihexyl phosphate causes mitochondrial impairment and induces cell apoptosis in CHO cells. Trihexyl phosphate promotes the proliferation of human breast cancer cells (MCF-7) in a dose-dependent manner and exerts estrogenicity via ERα-independent pathways .
|
-
- HY-137111A
-
|
|
5-HT Receptor
PERK
|
|
|
p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF can be used for neurological disease research .
|
-
- HY-121725
-
|
|
STAT
|
Cancer
|
|
MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines .
|
-
- HY-157508
-
|
|
p97
|
Others
|
|
VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
|
-
- HY-P2082
-
|
|
GnRH Receptor
|
Others
|
|
[D-pGlu1,D-Phe2,D-NaI3,6]-Gn-RH is a gonadotropin-releasing hormone (Gn-RH) agonist that has a dose-dependent inhibitory activity on progesterone secretion from cultured human granulosa cells.
|
-
![[D-pGlu1,D-Phe2,D-NaI3,6]-Gn-RH](//file.medchemexpress.com/product_pic/hy-p2082.gif)
- HY-A0224
-
|
SC-52458
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Forasartan is an nonpeptide angiotensin AT1 receptor antagonist with an IC50 of 2.9 nM. Forasartan is also an anti-hypertension agent. Forasartan significantly inhibits preganglionic stimulation in a dose-dependent manner in vivo. Forasartan can inhibit the heart rate increase induced by angiotensin II .
|
-
- HY-B1072
-
|
|
Environmental Pollutants
Parasite
Insecticide
|
Infection
|
|
Phenothrin is a Type I pyrethroid insecticide. Phenothrin induces dose-dependent DNA damage in human peripheral blood lymphocytes and hepatocytes, and exhibits definite genotoxic potential. Phenothrin acts as an insecticide for pest control in agriculture, households and public health, as well as for the elimination of human head lice infestations .
|
-
- HY-126910
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
|
-
- HY-145846
-
|
|
NO Synthase
Interleukin Related
|
Inflammation/Immunology
|
|
iNOs-IN-1 (YPW) is a potent inducible nitric oxide synthase (iNOS) inhibitor. iNOs-IN-1 can significantly inhibit the expression of IL-6 and iNOS, as well as reduce LPS-induced NO generation with dose-dependent manner in mouse macrophages. Anti-inflammatory effects .
|
-
- HY-15480
-
|
JAK2 Inhibitor V; Z3
|
JAK
|
Cancer
|
|
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
|
-
- HY-N5054
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
(R)-5,7-Dimethoxyflavanone shows potent antimutagenic activity against MeIQ mutagenesis in Ames test using the S. typhimurium TA100 and TA98 strains . And (R)-5,7-Dimethoxyflavanone significantly and dose-dependently inhibits the inflammatory mediato .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-133130
-
|
|
MAGL
|
Neurological Disease
|
|
JNJ-42226314, a chemical probe, is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
|
-
- HY-146433
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer .
|
-
- HY-113820
-
|
|
PPAR
|
Metabolic Disease
|
|
AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug .
|
-
- HY-104073R
-
|
|
Reference Standards
Sirtuin
|
Metabolic Disease
Inflammation/Immunology
|
|
CAY10602 (Standard) is the analytical standard of CAY10602 (HY-104073). This product is intended for research and analytical applications. CAY10602 is a SIRT1 activator. CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells .
|
-
- HY-106326
-
|
FAD 104
|
Others
|
Cancer
|
|
ME 2303 (FAD 104) is a fluoro-pyranosyl adriamycin analogue with anti-tumor potential. ME 2303 can inhibit the proliferation of acute undifferentiated myeloblastic leukemia (AML) blast cells in a dose-dependent manner. ME 2303 can be used for the study of acute undifferentiated myeloblastic leukemia (AML) .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-P992007
-
|
RN909
|
GCGR
|
Metabolic Disease
|
|
PF-06293620 (RN909) is a monoclonal antibody antagonist of the glucagon receptor. PF-06293620 produces dose-dependent, durable lowering of fasting plasma glucose and reduces HbA1c levels. PF-06293620 can be used for the research of type 2 diabetes mellitus .
|
-
- HY-114766
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
|
-
- HY-144730
-
|
|
HIV
|
Inflammation/Immunology
|
|
gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with an IC50 of 2.2 µM and CC50 of 100.90 µM. gp120-IN-1 shows anti-HIV-1 activity. gp120-IN-1 shows cytotoxicity in a dose dependent manner in SUP-T1 cells. gp120-IN-1 shows inhibition of gp120-mediated virus enter into cells .
|
-
- HY-156500
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-1 (compound 75) is an inhibitor of ICMT (IC50=0.0013 μM). ICMT-IN-1 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
|
-
- HY-179475
-
|
|
CaSR
|
Endocrinology
|
|
KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
|
-
- HY-B0162
-
|
|
HCN Channel
|
Cardiovascular Disease
Cancer
|
|
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-100585R
-
|
Splitomycin (Standard)
|
Reference Standards
HDAC
|
Cancer
|
|
Splitomicin (Standard) is the analytical standard of Splitomicin. This product is intended for research and analytical applications. Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM .
|
-
- HY-163172
-
|
|
Mitophagy
|
Neurological Disease
|
|
Miro1 Reducer is a small molecule that can repair this defect of Miro1 in Parkinson's disease (PD) fibroblasts. Miro1 Reducer reduces the delayed mitophagy phenotype in PD fibroblasts. Miro1 Reducer reduces Miro1 protein levels in dose-dependent manner (IC50 = 7.8 mM) .
|
-
- HY-185561
-
|
RC88
|
Mesothelin
|
Cancer
|
|
Misitatug blivedotin (RC88) is an antibody-drug conjugate (ADC) targeting mesothelin (MSLN). Misitatug blivedotin binds to mesothelin and exhibits dose‐dependent antitumor activity. Misitatug blivedotin can be used for the research of ovarian cancer, non-squamous non-small-cell lung carcinoma, cervical cancer .
|
-
- HY-146260
-
|
|
PI3K
|
Cancer
|
|
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
|
-
- HY-149705
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-7 (compound 74) is an inhibitor of ICMT (IC50=0.015 μM). ICMT-IN-7 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
|
-
- HY-B0094
-
Artemisinin
Maximum Cited Publications
32 Publications Verification
Qinghaosu; NSC 369397
|
HCV
Parasite
Akt
Ferroptosis
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-P1257
-
|
|
Insulin Receptor
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-149906
-
|
GEM91
|
HIV
|
Infection
|
|
Trecovirsen is an antiviral agent targeting HIV gag mRNA, which hybridizes with complementary HIV gag mRNA at the initiation site. Trecovirsen induces a reversible, dose-dependent prolongation of activated partial thromboplastin time via its polyanionic properties. Trecovirsen is applicable to research related to HIV infection .
|
-
- HY-144127
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-P10517
-
|
SFT
|
HIV
|
Infection
|
|
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs .
|
-
- HY-151926
-
|
|
Enterovirus
|
Infection
|
|
Antiviral agent 24 is a potent antiviral agent with EC50 values of 0.101, 19.9, 91.2 µM for EV71, CVA21, EV68, respectively. Antiviral agent 24 inhibits METTL3/METTL14 activity in a dose-dependent manner .
|
-
- HY-169941
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and ERβ. ERα/ERβ antagonist-1 reduces ERα and ERβ activity in a dose-dependent manner in HepG2 liver cells .
|
-
- HY-10119
-
|
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-B0162A
-
|
|
HCN Channel
|
Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-N5060R
-
|
4-Allylanisole (Standard)
|
Parasite
Reference Standards
|
Neurological Disease
|
|
Estragole (Standard) is the analytical standard of Estragole. This product is intended for research and analytical applications. Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole dose-dependently blocks nerve excitability . Estragole displays anti-toxoplasma activity .
|
-
- HY-121356S
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
|
Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
|
-
- HY-P10517A
-
|
SFT acetate
|
HIV
|
Infection
|
|
Sifuvirtide (SFT) acetate is a potent HIV fusion inhibitor. Sifuvirtide acetate inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide acetate can be used in the research of anti-HIV drugs .
|
-
- HY-P1440A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.
|
-
- HY-154995
-
|
|
Glycosidase
|
Infection
|
|
N-4′-(p-Trifluoromethylphenyl)butyl-DAB (compound 5g) is an agonit of lysosomal acid α-glucosidase (GAA). N-4′-(p-Trifluoromethylphenyl)butyl-DAB increases intracellular GAA activities dose-dependently, in Pompe patient's fibroblasts with the M519V mutation .
|
-
- HY-N7934
-
|
(-)-Trachelogenin
|
HCV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Trachelogenin ((-)-Trachelogenin) is an HCV entry inhibitor without genotype specificity, and with low cytotoxicity. Trachelogenin inhibits HCVcc infection and HCVpp cell entry in a dose-dependent manner with an IC50 of 0.325 and 0.259 μg/mL in HCVcc and HCVpp models, respectively. Trachelogenin exhibits effective antiviral, anti-inflammatory and analgesic effects .
|
-
- HY-130323
-
|
|
Bacterial
|
Infection
|
|
13-HPOT is a linolenic acid hydroperoxide and an antibacterial agent. 13-HPOT interacts with lipid representatives of bacterial inner membranes. 13-HPOT exerts dose-dependent in vitro antibacterial activity against Pectobacterium carotovorum, Pseudomonas syringae pv. syringae DC3000, and Xanthomonas translucens pv. translucens .
|
-
- HY-P2080
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-121356S1
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
|
Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
|
-
- HY-P2080B
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human acetate is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human acetate dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-N0262
-
-
- HY-N14645
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Ipolamiide is an antiosteoporotic agent that can be isolated from Barleria lupulina. Ipolamiide exhibits a potent antiosteoporotic effect. Ipolamiide dose-dependently enhances alkaline phosphatase (ALP) activity in MC3T3-E1 cells. Ipolamiide can be used for osteoporosis research .
|
-
- HY-W800105
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Geranyl isovalerate is a chemical component that can be extracted from Argyreia Nervosa. Geranyl isovalerate inhibits cancer cell proliferation in a dose-dependent and time-dependent manner. Geranyl isovalerate activates the apoptotic pathway by inducing mitochondrial membrane potential loss and ROS accumulation. Geranyl isovalerate can be used for cancer research .
|
-
- HY-152535
-
|
|
HSV
|
Infection
Inflammation/Immunology
|
|
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
|
-
- HY-173128
-
|
|
Apoptosis
|
Infection
|
|
TZOA is an antiviral agent that inhibits the replication of infectious hematopoietic necrosis virus (IHNV) in a dose-dependent manner and significantly reduces viral titers. TZOA can effectively counteract IHNV-induced apoptosis, maintain mitochondrial membrane potential and homeostasis, and restore MAVS-mediated interferon expression. TZOA has antiviral activity .
|
-
- HY-10119A
-
|
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-108716
-
|
CBS9106; SL-801
|
CRM1
Apoptosis
|
Cancer
|
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells .
|
-
- HY-138054
-
|
|
MDM-2/p53
|
Cancer
|
|
Cjoc42 is a compound capable of binding to gankyrin. Cjoc42 inhibits gankyrin activity in a dose-dependent manner. Cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin. Cjoc42 restores p53-dependent transcription and sensitivity to DNA damage .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-113798
-
|
|
Thymidylate Synthase
Antifolate
|
Cancer
|
|
ICI 198583 is a thymidylate synthase (TS) inhibitor with a Ki value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia .
|
-
- HY-P1257A
-
|
|
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-138939
-
|
|
Lipoxygenase
|
Cancer
|
|
5-LOX-IN-2, an inhibitor of 5-lipoxygenase (5-LOX) with an IC50 of 0.33 μM, inhibits 5-LOX in a dose-dependent manner . 5-LOX-IN-2, reduces the cell viability of renal cancer cells and induces apoptosis, can be used for cancer research .
|
-
- HY-B0607
-
|
NTBC; Nitisone; SC0735
|
HPPD
|
Metabolic Disease
|
|
Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-116431
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
I-BOP is an agonist for thromboxane A2 receptor (TP) with a KD of 0.61 nM. I-BOP promotes proliferation through activation of PI3K pathway in vascular smooth muscle . I-BOP dose-dependently biphasicly affects the excitatory postsynaptic potential (e.p.s.p.) in hippocampal neurons .
|
-
- HY-P1235
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-N15634
-
|
|
Insecticide
|
Neurological Disease
|
|
Anticopalic acid is a labdane-type diterpenoid insect antifeedant that exhibits dose-dependent antifeedant activity against the fall armyworm (Spodoptera frugiperda). Anticopalic acid can be isolated from Vitex hemsleyi. Anticopalic acid may be involved in neuroreceptor-mediated insect taste regulation and could be used to develop environmentally friendly antifeedants targeting lepidopteran pests .
|
-
- HY-N6745
-
|
|
Na+/K+ ATPase
Apoptosis
|
Infection
Cardiovascular Disease
|
|
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
|
-
- HY-162001
-
|
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-163106
-
|
|
Ceramidase
|
Cancer
|
|
W000113414_I13 is an acid ceramidase (AC) inhibitor. W000113414_I13 exhibits dose-dependent inhibition of AC with an IC50 value of 6.6?μM. W000113414_I13 can be used for the research of cancer .
|
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo .
|
-
- HY-B0162B
-
|
|
HCN Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ivabradine sulfate is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine sulfate reduces dose-dependently heart rate without modification of blood pressure. Ivabradine sulfate shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-177424
-
|
|
Proton Pump
|
Others
|
|
Eprazole trisulfide dimer is a trisulfide dimer of Ilaprazole (HY-101664), an orally active proton pump inhibitor that irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Eprazole trisulfide dimer can be utilized in research on gastric ulcers .
|
-
- HY-19233
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
BAM-1110 is a dopamine receptor agonist. BAM-1110 exhibits dose-dependent antiparkinsonian activity in MPTP (HY-W114750)-treated monkey models of Parkinson's disease. BAM-1110 has minimal side effects and can be used for the research of Parkinson's disease and other neurological disorders .
|
-
- HY-14371
-
|
|
Drug Derivative
LPL Receptor
|
Inflammation/Immunology
|
|
LX2932 is an orally active LX2931 (HY-14370) analogue and S1P/S1PR signaling axis modulator. LX2932 yields a dose-dependent decrease in circulating lymphocyte numbers. LX2932 improves collagen-induced arthritis .
|
-
- HY-19517
-
|
|
Endogenous Metabolite
|
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-167973
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABA-palmitamide is a GABA-responsive compound. GABA-palmitamide exhibits a dose-dependent bidirectional regulatory effect on the stereotyped behavior induced by Apomorphine (HY-12723): high doses inhibit motor behavior, while low doses enhance stereotyped behaviors in the oral cavity. GABA-palmitamide can be used in research on behavior regulation .
|
-
- HY-167886
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
GA 0113 is a potent and orally active angiotensin II (Ang II) AT1-receptor antagonist. GA 0113 inhibits the Ang II (HY-13948)-induced pressor response with ID50 of 0.032 mg/kg and dose-dependently increases plasma renin activity for 48 h .
|
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-N0092R
-
|
|
Reference Standards
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR .
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation .
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes .
In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
|
-
- HY-10787R
-
|
H 376/95 (Standard)
|
Reference Standards
Thrombin
|
Cardiovascular Disease
|
|
Ximelagatran (Standard) is the analytical standard of Ximelagatran (HY-10787). This product is intended for research and analytical applications. Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcoKinetics and pharmacodynamics .
|
-
- HY-122303
-
|
4-OH-DiPT hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
4-hydroxy DiPT hydrochloride is an 5-HT2A agonist that induces the head-twitch response (HTR) in mice, indicating psychoactivity . 4-hydroxy DiPT hydrochloride significantly reduced freezing responses to conditioned cues in a dose-dependent manner with a greater potency in female mice than male mice .
|
-
- HY-W042191R
-
|
|
Reference Standards
Fungal
Apoptosis
Caspase
Bcl-2 Family
MDM-2/p53
PARP
|
Infection
Cancer
|
|
Oxychlororaphine (Standard) is the analytical standard of Oxychlororaphine. This product is intended for research and analytical applications. Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer[1][2].
|
-
- HY-N3734
-
|
|
Beta-secretase
Phosphatase
|
Neurological Disease
|
|
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
|
-
- HY-B1309
-
|
AMAP
|
Drug Derivative
Mitochondrial Metabolism
|
Infection
Cancer
|
|
Metacetamol (AMAP) is an analog of Acetaminophen (HY-66005). Metacetamol induces dose-dependent necrosis in primary hepatocytes via glutathione depletion, mitochondrial damage, and formation of mitochondrial protein adducts. Metacetamol derivatives act as anticancer and antibacterial agents. Metacetamol can be used in studies related to breast cancer, bacterial infections, and fungal infections (candidiasis) .
|
-
- HY-130345
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension .
|
-
- HY-N12481
-
|
|
Others
|
Inflammation/Immunology
|
|
Cephalandole B is an indigo alkaloid that has the activity of inhibiting IL-17A gene expression. Cephalandole B significantly inhibited the activity of IL-17A luciferase reporter gene in Jukat cells, and this inhibitory effect was dose-dependent. Cephalandole B may have important application prospects in inflammation-related research .
|
-
- HY-152035
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Mycobacterial Zmp1-IN-1 is a mycobacterial zinc metalloprotease-1 (Zmp1) inhibitor. Mycobacterial Zmp1-IN-1 has anti-mycobacterial activity for Mtb H37Ra in dose-dependent inhibition. Mycobacterial Zmp1-IN-1 can be used for the research of tuberculosis (TB) .
|
-
- HY-B0006
-
-
- HY-14923
-
|
AVE 7688
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
|
|
Ilepatril, a dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase, has inhibitory effects in the type 2 diabetic nephropathy model in obese Zucker diabetic fatty (ZDF) rats. Ilepatril significantly reduced albuminuria in a dose-dependent manner and may be a strategy distinct from metabolic control to inhibit type 2 diabetic nephropathy .
|
-
- HY-125396
-
|
11-Deoxy-PGF2β
|
Endogenous Metabolite
|
Others
|
|
11-Deoxyprostaglandin F2β (11-deoxy PGF2β) is an analog of PGF2β (HY-12956B). PGF2β is a metabolite produced by cyclooxygenase metabolism of arachidonic acid. PGF2β induces dose-dependent release of hexose containing mucin .
|
-
- HY-103461
-
|
|
FAAH
|
Neurological Disease
|
|
FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain .
|
-
- HY-182765
-
|
|
Molecular Glues
|
Inflammation/Immunology
|
|
VAV1 degrader-4 is a VAV1 molecular glue degrader with a DC50 value of 3.93 nM for VAV1 in Jurkat cells. VAV1 degrader-4 can dose-dependently inhibit the production of IL-2. VAV1 degrader-4 can be used for research on autoimmune diseases .
|
-
- HY-142088
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Beauverolide Ka, a cyclotetradepsipeptide, is a metabolite of Beauveria bassiana fungus. Beauverolide Ka stimulates glucose uptake in cultured rat L6 myoblasts at 50 μM. Beauverolide Ka exhibits protecting effects on HEI-OC1 cells at 10 μM and shows dose-dependent activity in both L6 myoblasts and myotubes .
|
-
- HY-P2080C
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30)-Myr is the Myr-modified GIP (1-30), which is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-N13202
-
|
|
Others
|
Inflammation/Immunology
|
|
Black Currant Extract is a black currant extract, and its components include: Anthocyanidins. Black Currant Extract is an anti-inflammatory agent that can neutralize the cytotoxic effects of nicotine on epithelial cells and fibroblasts in a dose-dependent manner. Black Currant Extract can also inhibit LPS-induced IL-6 secretion by human macrophages. .
|
-
- HY-115579
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
|
-
- HY-178738
-
|
|
Antibiotic
Bacterial
Topoisomerase
DNA/RNA Synthesis
|
Infection
|
|
GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis .
|
-
- HY-135899
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. .
|
-
- HY-15297R
-
|
OPC-8212 (Standard)
|
Phosphodiesterase (PDE)
Reference Standards
|
Infection
Cardiovascular Disease
|
|
Vesnarinone (Standard) is the analytical standard of Vesnarinone. This product is intended for research and analytical applications. Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research .
|
-
- HY-122678
-
|
|
Survivin
Apoptosis
|
Cancer
|
|
LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC50s of 2.99 and 2.47 µM, respectively .
|
-
- HY-117236
-
|
|
γ-secretase
|
Neurological Disease
|
|
GSI-136 is an inhibitor of γ-secretase with an IC50 of 3 nM. GSI-136 can lead to a dose-dependent reduction of Aβ40 levels in diethylamine-extracted brain homogenates of C57BL/6 mice. GSI-136 can be studied in medicinal chemistry and Alzheimer's disease research .
|
-
- HY-108630
-
|
|
Phospholipase
|
Others
|
|
U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC .
|
-
- HY-182782
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Analgesic agent-4 is an adenosine A3AR ligand with analgesic/antinociceptive activity. Analgesic agent-4 inhibits writhing responses in mice and exhibits dose-dependent activity in the acetic acid (HY-Y0319)-induced mouse writhing model. Analgesic agent-4 can be used in the research of pain-related diseases .
|
-
- HY-B2145
-
|
IY-81149 sodium
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-103101R
-
|
|
Reference Standards
5-HT Receptor
|
Others
|
|
LP44 hydrochloride (Standard) is the analytical standard of LP44 hydrochloride (HY-103101). This product is intended for research and analytical applications. LP44 hydrochloride is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 hydrochloride induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 hydrochloride not causes considerable hypothermic response by intraperitoneal administration .
|
-
- HY-B2145A
-
|
IY-81149 sodium hydrate
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-162882
-
|
|
Xanthine Oxidase
Reactive Oxygen Species (ROS)
|
Metabolic Disease
|
CC15009 is a xanthine oxidoreductase (XOR) inhibitor, with an IC50 value of 0.237 nM. CC15009 can inhibit the oxidative subtype of XOR, thereby reducing the production of the byproduct ROS and exhibiting antioxidant activity. CC15009 has demonstrated a good dose-dependent uric acid-lowering effect in two different mouse models of hyperuricemia induced by XOR substrates .
|
-
- HY-106044
-
-
- HY-117952
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
|
-
- HY-168614
-
|
|
IKZF Family
|
Cancer
|
|
MGD-4 is an orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM) in a dose-dependent manner. MGD-4 effectively inhibits the growth of multiple myeloma .
|
-
- HY-181048
-
|
|
Casein Kinase
MDM-2/p53
|
Cancer
|
|
CK1α-IN-1 (Compound 7a) is a selective CK1α inhibitor with an IC50 of 10.96 nM. CK1α-IN-1 dose-dependently stabilizes p53 protein. CK1α-IN-1 has anticancer activity against acute monocytic leukemia .
|
-
- HY-105973
-
|
BRL 14342
|
Serotonin Transporter
|
Neurological Disease
|
|
Clemeprol (BRL 14342) is an orally active Noradrenaline (NA) and 5-HT uptake blocker. Clemeprol inhibits 6-
Hydroxydopamine (HY-B1081)-induced depletion of brain NA. Clemeprol exerts a dose-dependent inhibition of Reserpine (HY-N0480)-induced hypothermia. Clemeprol can be used in the research of depression .
|
-
- HY-124185
-
|
|
Others
|
Others
|
|
LC 6 is an anti-allergic compound that has the activity of inhibiting passive cutaneous allergic reactions in rats. Its half effective dose (ED50) is 35 mg/kg body weight. Oral administration is effective and long-lasting, and the effect is obviously dose-dependent. Its long-term binding to mast cells makes it a valuable tool for studying allergic reaction receptors.
|
-
- HY-100724
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
YM-17690 is a LTD4 and LTE4 agonist, with a pKi value of 9.28 for [3H]LTD4. It induces dose-dependent contractions in guinea pig ileum, lung parenchyma, and trachea, with EC50 values of 16, 3.9, and 22 nM, respectively. YM-17690 can be used in research related to asthma and inflammation .
|
-
- HY-122112
-
|
|
Sigma Receptor
|
Cancer
|
|
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
|
-
- HY-W133891
-
|
Peptones, soybean
|
Biochemical Assay Reagents
|
Others
|
|
Peptone from soy (peptones, soybean) is a peptone. Peptone from soy provides nitrogen and carbon sources, as well as other nutrients. Peptone from soy can stimulate/regulate the biosynthesis of cyclic eicosanoids. Peptone from soy induces dose-dependent contraction of guinea pig lung parenchyma. Peptone from soy can be used in microbial and cell culture .
|
-
- HY-B0094S
-
|
Qinghaosu-d3; NSC 369397-d3
|
Akt
Ferroptosis
HCV
Parasite
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-B1041R
-
|
Pimagedine hydrochloride (Standard); GER-11 (Standard); Aminoguanidinium chloride (Standard)
|
NO Synthase
Apoptosis
Reference Standards
|
Endocrinology
|
|
Aminoguanidine (hydrochloride) (Standard) is the analytical standard of Aminoguanidine (hydrochloride). This product is intended for research and analytical applications. Aminoguanidine hydrochloride (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine hydrochloride has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine hydrochloride has antioxidant properties. Aminoguanidine hydrochloride can be used in diabetic nephropathy research .
|
-
- HY-W008820R
-
|
|
Reference Standards
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-144797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction .
|
-
- HY-W025736
-
|
|
Drug Isomer
|
Neurological Disease
Inflammation/Immunology
|
|
5-Amino-2-methoxyphenol is a phenolic regioisomer. 5-Amino-2-methoxyphenol produces dose-dependent antinociception in the mouse formalin test, with its second-phase effect being mechanistically dependent on both FAAH and TRPV1. 5-Amino-2-methoxyphenol can be used for antinociception research .
|
-
- HY-10975
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 sodium is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 sodium crosses the blood-brain barrier. MK-0752 sodium reduces newly generated CNS Aβ in vivo .
|
-
- HY-13570BS1
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Betamethasone acetate-d5 is deuterium labeled Betamethasone acetate (HY-13570B). Betamethasone acetate is a glucocorticoid with prenatal application for preventing respiratory distress syndrome (RDS) in premature infants. Betamethasone acetate exhibits dose-dependent effects on somatic and brain development in offspring when administered prenatally to pregnant rats. Betamethasone acetate can be used for the study of antenatal intervention .
|
-
- HY-Y0284
-
-
- HY-N2252
-
-
- HY-159692
-
|
IONIS-1063734
|
TGF-beta/Smad
|
Inflammation/Immunology
Cancer
|
|
AZD8701 (IONIS-1063734) is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs), with a human IC50 of 65.2 nM. AZD8701 binds to intronic sites of all FOXP3 pre-mRNA isoforms and mediates dose-dependent FOXP3 knockdown via free uptake. AZD8701 can be used in cancer-related research .
|
-
- HY-101390B
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Niguldipine is a calcium channel blocker with activity in regulating cardiovascular function. Niguldipine can reduce systolic and diastolic blood pressure, thereby increasing heart rate and cardiac output. Niguldipine exhibits dose-dependent and sustained increases in coronary blood flow. Niguldipine also increases perfusion in the kidneys and femoral arteries, but the effect is temporary and to a lesser extent. The effect of Niguldipine on myocardial metabolism is not significant .
|
-
- HY-174311
-
|
|
Glycosidase
|
Neurological Disease
Metabolic Disease
|
|
GT-02216 can bind to GCase allosterically and enhance its activity. GT-02216 enhances the activity of GCase in primary human fibroblasts dose-dependently reduces the accumulation of its substrate, hexosylsphingosine (HexCer). GT-02216 reduces the Tau accumulation in mutant GBA1 fibroblasts. GT-02216 can be used for the study of Parkinson’s disease .
|
-
- HY-123714
-
|
|
MAP4K
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM) .
|
-
- HY-10974
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo .
|
-
- HY-B0162S
-
|
|
Isotope-Labeled Compounds
HCN Channel
|
Cardiovascular Disease
|
|
Ivabradine-d6 is the deuterium labeled Ivabradine . Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-167846
-
|
|
JAK
|
Cancer
|
|
YLIU-4-105-1 is a Type II JAK2 inhibitor. YLIU-4-105-1 binds to the ATP-binding pocket of JH1. YLIU-4-105-1 has in vivo pharmacodynamic activity as evidenced by inhibiting pSTAT5, reducing spleen to body weight, and lowering blood reticulocyte counts in a dose-dependent manner .
|
-
- HY-12953
-
-
- HY-101960A
-
|
AG-183
|
EGFR
|
Cancer
|
|
Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [ 3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation .
|
-
- HY-144657
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .
|
-
- HY-107037
-
|
RX71107
|
Vasopressin Receptor
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Tolmesoxide (RX71107) is a peripheral vascular dilator with blood pressure lowering activity. Tolmesoxide has shown direct vasodilation in the human forearm arterial bed and dorsal hand vein. Tolmesoxide can dose-dependently increase blood flow in the forearm and produce dilation during contraction of the dorsal hand veins. Tolmesoxide can be used to study high blood pressure and angina .
|
-
- HY-145153
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
|
-
- HY-105203
-
|
|
Others
|
Neurological Disease
|
|
MS-322 is an orally active centrally acting muscle relaxant. MS-322 can dose-dependently inhibit spinal reflex potentials, reduce neuronal excitability and muscle afferent discharges, and so on in rats. In addition, MS-322 has relatively weak inhibitory effects on other central nervous system pathways and no effect on the neuromuscular junction .
|
-
- HY-129737
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
|
-
- HY-139451
-
|
|
ELOVL
|
Neurological Disease
|
|
ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA .
|
-
- HY-180212
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SYK-1106 is a potent delta-opioid receptor (DOR) agonist with an EC50 of 89 pM and a Ki of 848 pM. SYK-1106 is selective for μ and κ opioid receptors, with Ki values of 9.54 nM and 2.45 nM, respectively. SYK-1106 induces dose-dependent antidepressant-like effects. SYK-1106 can be used for the research of depression .
|
-
- HY-11056
-
|
|
Dopamine Receptor
|
Neurological Disease
|
PF-04363467 is a highly preferring D3R antagonist. PF-04363467 produces dose-dependent changes in the EEG profile of freely moving rats. PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-04363467 can be used for the study of addiction, cognitive and mental illness .
|
-
- HY-146203
-
|
|
FAK
|
Cancer
|
|
Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
|
-
- HY-11062
-
Icilin
1 Publications Verification
AG-3-5
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response .
|
-
- HY-182420
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
DJT06001 is an orally active, highly selective Factor Xa inhibitor. DJT06001 shows inhibition with Ki of 0.99 nM, IC50 of 2.53 nM in prothrombinase complex and 3.33 nM in human plasma. DJT06001 dose-dependently prolongs PT and APTT, inhibits thrombus formation in vivo. DJT06001 can be used for the research of thromboembolic diseases .
|
-
- HY-118765
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Ro 23-3423 is a thromboxane synthase inhibitor with an IC50 value of 0.33 μM for human platelet microsomal thromboxane synthase. Ro 23-3423 increases plasma levels of PGF and PGE2 in a dose-dependent manner, accompanied by a decrease in mean systemic arterial pressure and systemic vascular resistance. Ro 23-3423 can be used in the study of general anesthesia .
|
-
- HY-18056
-
|
|
11β-HSD
|
Metabolic Disease
|
|
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
|
-
- HY-131334
-
|
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect .
|
-
- HY-105514
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
KP-10614 is a potent, orally active platelet aggregation inhibitor. KP-10614 inhibits platelet aggregation induced by ADP with IC50 of 1 nM. KP-10614 causes dose-dependent inhibition of ex vivo platelet aggregation in rats. KP-10614 shows antithrombotic effects in various thrombosis models. KP-10614 can be used for thrombotic diseases research .
|
-
- HY-113763
-
|
|
TNF Receptor
|
Others
|
|
L524-0366 is a specific, dose-dependent TWEAK-Fn14 inhibitor. L524-0366 specifically binds to the Fn14 surface with a KD of 7.12 μM, competitively inhibiting the binding of Fn14 to TWEAK (inhibition rate reaching 16%). L524-0366 inhibits TWEAK-induced glioma cell migration without potential cytotoxic effects .
|
-
- HY-N0262R
-
|
3'-Deoxyadenosine (Standard)
|
TNF Receptor
Reference Standards
MMP
Bacterial
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Cordycepin (Standard) is the analytical standard of Cordycepin. This product is intended for research and analytical applications. Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner . Cordycepin kills Mycobacterium tuberculosis through hijacking the bacterial adenosine kinase .
|
-
- HY-B0006S
-
-
- HY-B0006S1
-
|
BM 14190-d4
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
|
-
- HY-W581798
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
Cancer
|
|
Iron(II) sulfate hydrate is an iron(II) salt with oral activity, acting as an iron supplier, and is easily oxidized to iron(III) in water. Iron(II) sulfate hydrate induces apoptotic morphological changes in cancer cells, and promotes dose‑dependent iron accumulation in rats. Iron(II) sulfate hydrate can be used in studies of leukemia, breast cancer, iron deficiency, anemia, and restless legs syndrome .
|
-
- HY-10119R
-
|
SCH 530348 (Standard)
|
Reference Standards
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-B0094R
-
|
Qinghaosu (Standard); NSC 369397 (Standard)
|
Reference Standards
HCV
Parasite
Akt
Ferroptosis
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin (Standard) is the analytical standard of Artemisinin. This product is intended for research and analytical applications. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-12995A
-
|
|
FLAP
|
Inflammation/Immunology
|
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
|
-
- HY-101664
-
|
IY-81149
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-10119S
-
|
SCH 530348-d5
|
Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-155417
-
|
|
Orphan GPCR
ERK
|
Neurological Disease
|
|
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
|
-
- HY-B0006S2
-
-
- HY-179251
-
|
|
CHIKV
|
Infection
|
|
BDGR-651 is an efficient and selective inhibitor of the Chikungunya virus (CHIKV) with an EC50 in NHDF cells of 0.86 μM, and the therapeutic index (SI) of 22.1. BDGR-651 exhibits dose-dependent protective effects when infecting Vero E6 cells, with its EC50 being 6 μM. BDGR-651 can be used for research on CHIKV infection .
|
-
- HY-B1041
-
|
Pimagedine hydrochloride; GER-11; Aminoguanidinium chloride
|
NO Synthase
Apoptosis
ERK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Aminoguanidine (Pimagedine) hydrochloride is an inhibitor of diamine oxidase (DAO) and nitric oxide synthase (NOS). Aminoguanidine hydrochloride can reduce the formation of advanced glycation end products (AGEs). Aminoguanidine hydrochloride has a dose-dependent inhibitory effect on Doxorubicin (HY-15142)-induced cell apoptosis. Aminoguanidine hydrochloride has antioxidant properties. Aminoguanidine hydrochloride can be used in the research of diabetic nephropathy .
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- HY-B0162AR
-
|
|
Reference Standards
HCN Channel
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Ivabradine hydrochloride (Standard) is the analytical standard of Ivabradine hydrochloride. This product is intended for research and analytical applications. Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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- HY-W013053
-
|
DBA; 1,2,5,6-Dibenzanthracene; Benzo[k]tetraphene
|
Environmental Pollutants
DNA/RNA Synthesis
MDM-2/p53
Apoptosis
|
Cancer
|
|
Dibenz[a,h]anthracene (DBA) is an orally active polycyclic aromatic hydrocarbon, a by-product of incomplete combustion of organic matter, a potent carcinogen, and an agonist of AhR. Dibenz[a,h]anthracene induces dose-dependent increases in DNA adduct formation and lacZ mutation frequency. Dibenz[a,h]anthracene upregulates St3gal5. Dibenz[a,h]anthracene can be used in cancer-related research .
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-
![Dibenz[a,h]anthracene](//file.medchemexpress.com/product_pic/hy-w013053.gif)
- HY-B1246
-
|
|
Bacterial
Proton Pump
|
Infection
|
|
Thonzonium bromide is an antibacterial agent that is structurally similar to Farnesol (HY-Y0248A). Thonzonium bromide is also a monocationic surface-active agent, which inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo. Thonzonium bromide inhibits proton transport in a dose-dependent manner (EC50=69 μM) .
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-
- HY-120727
-
|
|
mGluR
|
Neurological Disease
|
|
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .
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- HY-129668
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Bremazocine is a potent opioid kappa receptor agonist with analgesic activity. Bremazocine induces peripheral analgesia by releasing endogenous norepinephrine. The analgesic effect of bremazocine is associated with interaction with adenosine receptors. Bremazocine produces a dose-dependent peripheral analgesia after topical application. The effect of bremazocine is affected by nonselective α(2) adrenaline receptor antagonists, suggesting that it acts through a norepinephrine pathway .
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- HY-13570BR
-
|
|
Glucocorticoid Receptor
Reference Standards
|
Others
|
|
Betamethasone acetate (Standard) is the analytical standard of Betamethasone acetate (HY-13570B). This product is intended for research and analytical applications. Betamethasone acetate is a glucocorticoid with prenatal application for preventing respiratory distress syndrome (RDS) in premature infants. Betamethasone acetate exhibits dose-dependent effects on somatic and brain development in offspring when administered prenatally to pregnant rats. Betamethasone acetate can be used for the study of antenatal intervention .
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- HY-P10228
-
|
|
Fungal
Bacterial
|
Infection
|
|
S-Thanatin is an insect antimicrobial peptide with potent broad-spectrum antibacterial activity. S-Thanatin can inhibit the activity of Gram-negative bacteria, Gram-positive bacteria, and fungi, without cytotoxicity. The antibacterial activity of S-Thanatin is not affected by PH value, but monovalent cations (Na +/K +) can reduce its antibacterial activity against Gram-negative bacteria in a dose-dependent manner .
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- HY-B1072R
-
|
|
Reference Standards
Parasite
Environmental Pollutants
Insecticide
|
Infection
|
|
Phenothrin (Standard) is the analytical standard of Phenothrin (HY-B1072). This product is intended for research and analytical applications. Phenothrin is a Type I pyrethroid insecticide. Phenothrin induces dose-dependent DNA damage in human peripheral blood lymphocytes and hepatocytes, and exhibits definite genotoxic potential. Phenothrin acts as an insecticide for pest control in agriculture, households and public health, as well as for the elimination of human head lice infestations.
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- HY-W013755
-
|
DNOP; Di-n-octyl phthalate; Phthalic acid dioctyl ester
|
Biochemical Assay Reagents
Aminotransferases (Transaminases)
Phosphatase
Bacterial
|
Inflammation/Immunology
|
|
Dioctyl phthalate (DNOP) is a plasticizer. Dioctyl phthalate increases the activities of alanine aminotransferase (ALT) and alkaline phosphatase (ALP) in the liver, as well as the levels of creatinine and urea in the kidney. Exposure to Dioctyl phthalate disrupts the homeostasis of the intestinal microbial community, increases the abundance of pathogenic bacteria, and reduces the abundance of beneficial bacteria such as Lactobacillus. Dioctyl phthalate induces significant and dose-dependent inflammatory responses in the liver, spleen and kidney of mice .
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-
- HY-B0607R
-
|
NTBC (Standard); Nitisone (Standard); SC0735 (Standard)
|
HPPD
Reference Standards
|
Metabolic Disease
|
|
Nitisinone (Standard) is the analytical standard of Nitisinone. This product is intended for research and analytical applications. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
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-
- HY-113439
-
12-HETE
2 Publications Verification
|
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway .12-HETE has both anti-thrombotic and pro-thrombotic effects . 12-HETE is a neuromodulator .
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- HY-124920
-
|
Mercaptodimethur
|
Insecticide
SOD
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
Cholinesterase (ChE)
|
Infection
Inflammation/Immunology
|
|
Methiocarb (Mercaptodimethur) is an orally active carbamate insecticide. Methiocarb exerts dose-dependent toxic effects on onions. In addition to inhibiting acetylcholinesterase to induce cholinergic excitation, Methiocarb can induce lipid peroxidation in liver, kidney, brain and testicular tissues and alter reduced glutathione levels by generating ROS. Methiocarb can be used for agricultural pest control and research on oxidative stress-related cellular damage in mammals .
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-
- HY-172133
-
-
- HY-182682
-
|
NSC-146171
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
IOB-82 is a bifunctional alkylating agent. IOB‑82 induces marked nuclear and cytoplasmic alterations, elicits severe chromatid and chromosome aberrations, and remodels chromosome ploidy. IOB-82 exerts dose-dependent radiomimetic effects and preferentially cytotoxic to large A-type rat ascites cells. IOB-82 can be applied in the research of melanoma‑derived tumors and leukemia .
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-
- HY-160853
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 42 (Compound 14b) dose-dependently inhibited the activity of β-microtubulin (IC50 = 3.5 µM).Tubulin inhibitor 42 interferes with microtubule dynamic homeostasis, resulting in the arrest of the cancer cell cycle in the G2/M phase and inducing apoptosis. Tubulin inhibitor 42 significantly inhibits the angiogenic process in vitro and in vivo, preventing vascularization and tumor growth .
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-
- HY-123970
-
|
|
Macrophage migration inhibitory factor (MIF)
|
Neurological Disease
Inflammation/Immunology
|
|
ISO-92 in an inhibitor of MIF. ISO-92 selectively inhibits MIF inflammatory activity with an IC50 of 550 nM. ISO-92 inhibits hypoxia-induced proliferation of CCL-210 cell line dose-dependently. ISO-92 significantly reduces the thickness of pulmonary vascular wall in mouse hypoxia models. ISO-92 can be studied in inflammatory and neurological research .
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-
- HY-117251
-
|
|
Amino acid Transporter
|
Neurological Disease
|
|
LP-403812 is a high affinity proline transporter (PROT) inhibitor that produces dose-dependent inhibition of hPROT (IC50=0.11 μM; Ki=0.12 μM) and also inhibits the activity of mouse brain synaptosomal mPROT with the same potency (IC50=0.23 μM). LP-403812 can be used to study the function of PROT in the brain .
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-
- HY-144657A
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .
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-
- HY-110100
-
CPYPP
3 Publications Verification
|
DOCK
|
Inflammation/Immunology
|
|
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9 .
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-
- HY-10119AR
-
|
SCH 530348 sulfate (Standard)
|
Reference Standards
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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-
- HY-143653
-
|
|
BCL6
|
Cancer
|
|
BCL6-IN-6 is a potent inhibitor of transcriptional repressor B-cell lymphoma 6 (BCL6). BCL6-IN-6 significantly blocks the interaction of BCL6 with its corepressors and reactivates BCL6 target genes in a dose-dependent manner. BCL6-IN-6 has the potential for the research of diffuse large B-cell lymphoma (DLBCL) .
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-
- HY-179443
-
|
|
SOS1
Ras
|
Cancer
|
|
SOS1-IN-25 is an SOS1 inhibitor. SOS1-IN-25 exhibits inhibitory activity against KRAS G12C/SOS1 complex formation (IC50 = 11.11 nM). SOS1-IN-25 leads to a dose-dependent decrease in pERK levels. SOS1-IN-25 can be used for the study of leukemia .
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-
- HY-152019
-
|
|
EGFR
|
Cancer
|
|
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner .
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-
- HY-117955
-
|
WAY 141839; Co 2-6749
|
GABA Receptor
|
Neurological Disease
|
|
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
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-
- HY-125916
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pseurotin A is a secondary metabolite of Aspergillus and other fungi. Pseurotin A is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50 = 3.6 μM). Pseurotin A inhibits the PCSK9-LDLr interaction. Pseurotin A shows dose-dependent reduction of PCSK9, along with increased LDLR levels in hormone-dependent breast cancer cell lines. Pseurotin A exhibits antitumor activity .
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-
- HY-122215
-
|
N-696
|
Adrenergic Receptor
|
Endocrinology
|
|
Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats .
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-
- HY-107036
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
BMS-394136 (compound 1) is a potent inhibitor of Kv 1.5, with an IC50 of 0.05 μM. BMS-394136 is a selective IKur inhibitor. BMS-394136 dose-dependently prolongs atrial effective refractory period (AERP) and action potential duration (APD) without effecting ventricular effective refractory period (VERP). BMS-394136 can be used for acute atrial ischemia research .
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-
- HY-178465
-
|
|
Prostaglandin Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
EP4 receptor antagonist 8 is an orally active EP4 antagonist (human EP4 IC50 = 6.40 nM). EP4 receptor antagonist 8 significantly reduced paw and joint swelling, inflammatory cell infiltration, cartilage damage, pannus formation, and joint bone erosion in arthritis (AIA) mice in a dose-dependent manner. EP4 receptor antagonist 8 can be used for the study of inflammatory pain .
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-
- HY-119495
-
|
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
JTP 2942 is a thyrotropin-releasing hormone analogue. JTP 2942 can promote the release of Acetylcholine in the hippocampus and frontal cortex of rats. JTP 2942 possesses neuroprotective and cognitive-improving activities. JTP 2942 dose-dependently improves motor and neurological deficits in rat models of chronic focal cerebral ischemia. JTP 2942 can be used for the research of cerebral ischemia, motor neuron diseases, and other related conditions .
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-
- HY-B0607S
-
|
NTBC-d3; Nitisone-d3; SC0735-d3
|
Isotope-Labeled Compounds
HPPD
|
Metabolic Disease
|
|
Nitisinone-d3 (NTBC-d3) is deuterium labeled Nitisinone. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
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-
- HY-19042
-
|
YM 638
|
Leukotriene Receptor
|
Inflammation/Immunology
|
YM-16638 is an orally active leukotriene (LT) antagonist. YM-16638 can inhibit the production of LTC4, LTD4, and LTE4 in guinea pig trachea, with IC50 values of 0.05 μM, 0.16 μM, and 0.096 μM, respectively. YM-16638 has a dose-dependent inhibitory effect on antigen-induced early and late respiratory responses in allergic sheep .
|
-
- HY-173009
-
|
|
PROTACs
Cyclophilin
HCV
HIV
|
Infection
|
|
PROTAC CG167 is a selective and potent CypA PROTAC degrader. PROTAC CG167 degrades CypA in a dose-dependent manner (Jurkat: DC50: 123 nM). PROTAC CG167 can inhibit HIV-1 and HCV and exhibits antiviral activity . (Pink: CypA Ligand (HY-170997); Black: Linker (HY-W123015); Blue: E3 Ligase Ligand (HY-112078))
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-
- HY-B0006R
-
|
BM 14190 (Standard)
|
Reference Standards
Adrenergic Receptor
Autophagy
Bacterial
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol (Standard) is the analytical standard of Carvedilol. This product is intended for research and analytical applications. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
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-
- HY-108554
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
|
-
- HY-134539
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
|
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
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-
- HY-100022A
-
|
eFT508 hydrochloride
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-101906
-
|
|
Free Fatty Acid Receptor
Apoptosis
|
Metabolic Disease
|
|
DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively) . DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis .
|
-
- HY-182427
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
ORF 17583 is a Ranitidine (HY-B0693) analogue and H2 receptor antagonist. ORF 17583 exhibits typical reversible competitive antagonism in the guinea pig right atria model, causing a dose-dependent rightward shift of the histamine concentration-response curve without reducing the maximum effect, and its action is fully reversible upon washing. ORF 17583 can be used for research on peptic ulcers and hyperacidity .
|
-
- HY-W1126504
-
|
MC339
|
Notch
|
Cancer
|
|
ETN029 (MC339) is a selective DLL3 ligand. ETN029 labeled with 225Ac has dose-dependent cytotoxicity in SCLC, NEPC and metastatic melanoma cells and increases the phosphorylation of H2AX expression. ETN029 labeled with 177Lu shows rapid uptake persistent tumor retention and favorable tumor-to-kidney ratio. ETN029 can be used for cancers like SCLC and NEPC imaging and research .
|
-
- HY-101960
-
|
(Z)-AG-183
|
EGFR
|
Others
|
|
(Z)-Tyrphostin A51 is the Z configuration of Lanoconazole A51. Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [ 3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation .
|
-
- HY-B0094S3
-
|
Qinghaosu-13C,d4; NSC 369397-13C,d4
|
Ferroptosis
Akt
Parasite
HCV
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-B2145R
-
|
IY-81149 sodium (Standard)
|
Proton Pump
TOPK
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (sodium) (Standard) is the analytical standard of Ilaprazole (sodium). This product is intended for research and analytical applications. Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-161894
-
|
|
CFTR
|
Inflammation/Immunology
|
|
CFTR corrector 13 (SVQ18) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector (EC50=3.14 μM). CFTR corrector 13 enhances the function of CFTR channels, especially when used in combination with Lumacaftor (HY-13262), it can produce a dose-dependent increase in CFTR function. CFTR corrector 13 can be used in the study of cystic fibrosis (CF) and other CFTR-related diseases .
|
-
- HY-W015912S
-
|
2-Furyl methyl ketone-d3
|
Isotope-Labeled Compounds
|
Others
|
|
2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
|
-
- HY-174420
-
|
|
LRRK2
|
Neurological Disease
|
|
RN277 is an inhibitor for LRRK2 type II kinase. RN277 can be used as a cellular tool targeting the LRRK2 inactive state. RN277 can inhibit LRRK1 kinase activity in vitro. RN277 inhibits LRRK2 kinase activity in vitro (IC50 = 70 nM). RN277 reduces phosphorylation of Rab8a dose-dependently. RN277 can be studied in research for Parkingson’s disease .
|
-
- HY-109125
-
|
SPA-S-753 free base
|
Fungal
|
Infection
|
|
SPK-843 is an antifungal agent. SPK-843 shows inhibitory activity against A. fumigatus MF-13, A. flavus TIMM 0057, and A. niger TIMM 2814 with MICs of 0.5 μg/mL, 0.25 μg/mL, and 0.0625 μg/mL, respectively. SPK-843 exhibits dose-dependent efficacy in murine models of pulmonary aspergillosis. SPK-843 can be used for the research of related fungal infections .
|
-
- HY-W777526
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Nitisinone- 13C6 is a 13C-labeled Nitisinone (HY-B0607). Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-150582
-
|
|
c-Met/HGFR
c-Kit
FLT3
Apoptosis
|
Cancer
|
|
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
|
-
- HY-N0407
-
|
6'-Cinnamoylcatalpol
|
STAT
|
Inflammation/Immunology
|
|
Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
- HY-179240
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
UNC9815 is a D1 dopamine receptor (D1R) orthosteric allosteric modulator (PAM). UNC9815 can dose-dependently enhance the functional efficacy of dopamine in β-inhibitory protein recruitment experiments and cAMP accumulation experiments. When used in combination with other PAMs, UNC9815 exhibits a significant synergistic enhancement effect. UNC9815 can be used to study neurological and psychiatric diseases such as Parkinson's disease and schizophrenia .
|
-
- HY-19541A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
|
-
- HY-161260
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-Y0590
-
|
|
Environmental Pollutants
Reactive Oxygen Species (ROS)
Glutathione Reductase (GR)
|
Inflammation/Immunology
|
|
Copper (I) oxide is an oxidative stress inducer and cytotoxic agent. Copper (I) oxide causes dose-dependent decrease in the viability of airway epithelial cells by impairing the activities of catalase and glutathione reductase, generating reactive oxygen species, and increasing the levels of 8-isoprostane and the ratio of oxidized glutathione. However, when combined with Resveratrol (HY-16561), the cytotoxic effect induced by Copper (I) oxide is significantly attenuated, and oxidative damage is effectively alleviated .
|
-
- HY-115497
-
BRD5529
4 Publications Verification
|
E1/E2/E3 Enzyme
|
Infection
Inflammation/Immunology
|
|
BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC) .
|
-
- HY-119805
-
|
|
Others
|
Inflammation/Immunology
|
|
YM 13650 is an orally active anti-nephritic agent. YM 13650 exhibits dose-dependent preventive and therapeutic effects in both the rat immune complex nephritis model and the mouse spontaneous lupus nephritis model. YM 13650 can inhibit the increase in urinary protein, improve serum cholesterol and urea nitrogen levels, alleviate renal pathological damage, and prolong the survival time of mice. YM 13650 can be used in the research of nephritic diseases .
|
-
- HY-183578
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TYY-31 is an orally active, selective S1PR1 agonist with an EC50 of 1.13 pM. TYY-31 promotes the phosphorylation of ERK1/2. TYY-31 exerts anti-inflammatory and immunosuppressive effects, ameliorates DSS-induced colitis in mice, and reduces peripheral blood lymphocyte counts in mice in a dose-dependent manner. TYY-31 can be used for the research of ulcerative colitis .
|
-
- HY-W203683
-
|
PFNA; Heptadecafluorononanoic acid
|
PPAR
PERK
|
Metabolic Disease
|
|
Perfluorononanoic acid (PFNA) is an orally active PPARα activator. Perfluorononanoic acid activates PPARα-mediated gene expression, including upregulating target genes associated with lipid metabolism and triglyceride storage. Perfluorononanoic acid exhibits certain developmental and reproductive toxicity. Perfluorononanoic acid causes hepatomegaly in pregnant mice, induces high postnatal mortality in neonatal mice, and leads to dose-dependent delays in eye-opening time and puberty onset in mouse offspring .
|
-
- HY-W725737
-
|
|
LPL Receptor
Phosphodiesterase (PDE)
|
Neurological Disease
Cancer
|
|
BrP-LPA is a LPA antagonist/ATX inhibitor. BrP-LPA shows pan-antagonist activity towards LPA1-4 GPCRs. BrP-LPA decreases blood vessel density. BrP-LPA dose-dependently inhibits Lysophosphatidic acid-induced head-dip counts. BrP-LPA exhibits anticancer activity against breast cancer, colon cancer, and lung cancer. BrP-LPA inhibits anxiety-like behavior .
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-
- HY-103484
-
|
|
IKZF Family
|
Cardiovascular Disease
|
|
GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression .
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-
- HY-181650
-
|
|
mTOR
Akt
Ribosomal S6 Kinase (RSK)
Apoptosis
Autophagy
PI3K
|
Cancer
|
|
T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer .
|
-
- HY-106317
-
|
Glutathione isopropyl ester; YM 737
|
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Glutathione monoisopropyl ester (Glutathione isopropyl ester) is an ester derivative of glutathione. Glutathione monoisopropyl ester can increase glutathione concentrations in tissues such as the liver, lungs, heart, and brain of mice, exerting a dose-dependent protective effect against liver injury. Glutathione monoisopropyl ester effectively inhibits ultraviolet-induced lipid peroxidation, inflammatory responses, and tumorigenesis in the skin of hairless mice by maintaining epidermal glutathione levels. Glutathione monoisopropyl ester also inhibits the progression of X-ray-induced cataracts in rats .
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-
- HY-143472
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
|
-
- HY-19202
-
|
rac-EMA401; rac-PD-126055; EMA400
|
Angiotensin Receptor
|
Neurological Disease
|
|
rac-Olodanrigan (rac-EMA401; EMA400) is a racemic mixture of the S-enantiomer (EMA401; HY-13106) and R-enantiomer (EMA402). rac-Olodanrigan is a potent and selective AT2 receptor antagonist with IC50s of 75.2 nM and 2918 nM for AT2R and AT1R, respectively. rac-Olodanrigan evokes dose-dependent relief of mechanical allodynia in the ipsilateral hind paws of rats with a chronic constriction injury (CCI) of the sciatic nerve .
|
-
- HY-P4641
-
|
Trp-Phe
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-N18279
-
|
|
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Bulbocapnine is an aporphine isoquinoline alkaloid that exerts antagonistic effects on dopamine Receptor) and α-adrenergic receptors, as well as anti-peroxidative effects. The Ki value of bulbocapnine for tyrosine hydroxylase (TH) is 0.20 mM. Bulbocapnine reduces intracellular dopamine content, inhibits TH activity, and decreases Ca 2+ concentration. Bulbocapnine antagonizes the dose-dependent inhibitory effect of dopamine on the heart rate acceleration induced by stimulating the postganglionic fibers of the right cardiac accelerator nerve .
|
-
- HY-B1041AS
-
|
Pimagedine-13C, 15N4; GER-11free base-13C, 15N4; Aminoguanidinium-13C, 15N4
|
Isotope-Labeled Compounds
NO Synthase
Apoptosis
|
Endocrinology
|
|
Aminoguanidine- 13C, 15N4 (Pimagedine- 13C, 15N4) is the 13C- and 15N-labeled Aminoguanidine (HY-B1041A). Aminoguanidine (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine has antioxidant properties. Aminoguanidine can be used in diabetic nephropathy research .
|
-
- HY-W816575
-
|
|
RAR/RXR
SARS-CoV
|
Infection
|
MDI-403 is a retinoic acid receptor (RAR) agonist with an EC50 value of less than 1 μM. MDI-403 exhibits significant antiviral activity against SARS-CoV-2, and can dose-dependently inhibit the expression of viral nucleoprotein (NP) and reduce the proportion of infected cells. MDI-403 mainly acts during the virus invasion stage. MDI-403 can be used in research on anti-SARS-CoV-2 .
|
-
- HY-182941
-
|
|
EAAT
|
Neurological Disease
|
|
Parawixin10 (Compound 2) is an N-acylpolyamine. Parawixin10 fails to enhance glutamate uptake in radioligand uptake assays of EAAT1, EAAT2 or EAAT3. Parawixin10 exhibits no positive allosteric modulatory activity in radioligand uptake assays of EAAT1−EAAT3, nor can it improve neuronal survival rates in mice in a dose-dependent and statistically significant manner. Parawixin10 has no neuroprotective activity .
|
-
- HY-119379
-
|
HOE-720 free acid
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Fonsartan (HOE-720) free acid is an orally active angiotensin II receptor (AT1R) antagonist with an IC50 value of 0.48 nM, exhibiting potent antihypertensive activity. Fonsartan free acid dose-dependently inhibits angiotensin II-induced pressor response in rats (ID50 = 0.11 mg/kg) and shows significant long-lasting blood pressure-lowering effects in high-renin animal models. Fonsartan free acid is primarily used in research on hypertension and cardiovascular diseases .
|
-
- HY-W004287
-
|
|
Amyloid-β
Cholinesterase (ChE)
Parasite
|
Infection
Neurological Disease
|
|
Methyl tridecanoate is a fatty acid methyl ester. Methyl tridecanoate exhibits an IC50 of 3.26 μM and a Ki of 2.30 μM against AsOBP21f in Anopheles sinensis. Methyl tridecanoate induces electroantennographic responses in female Anopheles sinensis. Methyl tridecanoate shows a dose-dependent attractive effect on Anopheles sinensis. Methyl tridecanoate weakly inhibits β-amyloid aggregation and AChE activity. Methyl tridecanoate can be used in the research of malaria and Alzheimer's disease .
|
-
- HY-182023
-
|
|
Reactive Oxygen Species (ROS)
GABA Receptor
|
Neurological Disease
|
|
Anticonvulsant agent 11 (Compound 8b) is an anticonvulsant agent. Anticonvulsant agent 11 exerts neuroprotective effects by enhancing cell viability and reducing ROS levels. Anticonvulsant agent 11 induces the expression of GABAA α1, resulting in neuronal hyperpolarization. Anticonvulsant agent 11 increases the number of neurite-bearing cells and the length of neurites. Anticonvulsant agent 11 exhibits dose-dependent anticonvulsant effects in mice. Anticonvulsant agent 11 can be used for the research of epilepsy .
|
-
- HY-401424
-
|
Polyoxyethylene(36) Castor Oil; PEG-36 Castor Oil
|
Environmental Pollutants
Biochemical Assay Reagents
|
Others
|
|
Cremophor EL-36 is a non-ionic surfactant, mainly used as a solubilizing carrier for poorly soluble Paclitaxel (HY-B0015). For example, Cremophor EL-36 can enhance the intracellular influx of Etoposide (HY-13629) without affecting drug efflux, and can dose-dependently increase the accumulation of VP-16 in lung adenocarcinoma cells (such as PC-14 and A549), significantly enhancing its cytotoxic effect .
|
-
- HY-P4984
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a T cell proliferation activator. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) promotes the in vitro proliferation of human peripheral blood mononuclear cells (PBMC) in a dose-dependent manner. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) can be used in research on inflammatory and immunity, as well as cancer .
|
-
- HY-N13739
-
|
|
Tyrosinase
|
Cancer
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
- HY-101664R
-
|
IY-81149 (Standard)
|
Reference Standards
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (Standard) is the analytical standard of Ilaprazole. This product is intended for research and analytical applications. Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-P10711
-
|
|
Autophagy
|
Cancer
|
|
ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation .
|
-
- HY-180323
-
|
|
RAR/RXR
|
Inflammation/Immunology
|
|
ER-38925 is a retinoid agonist with selevtivity to retinoic acid receptor subtype α (RAR-α). ER-38925 prolongs the lifespan of the recipient mice dose-dependently. ER-38925 potently inhibits alloantigenstimulated donor T lymphocyte prolifertion in vitro. ER-38925 can prevent the development of antiallogeneic cytotoxic T lymphocyte response in mice. ER-38925 inhibits serum anti-DNA autoantibody production in mouse model of human chronic GVHD .
|
-
- HY-107655
-
|
ABET
|
mAChR
|
Cardiovascular Disease
|
|
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research . Arecaidine but-2-ynyl ester (tosylate) 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-169060
-
|
|
Lactate Dehydrogenase
|
Cancer
|
|
LDHA-IN-8 (Compound 6) is a lactate dehydrogenase (LDHA) inhibitor. LDHA-IN-8 inhibits LDHA catalysis of pyruvate in a dose-dependent manner (EC50 value of 14.54 μM), reduces intracellular lactate levels, and increases intracellular reactive oxygen species (ROS) levels, thereby inhibiting the proliferation of pancreatic cancer cells and lung cancer cells. LDHA-IN-8 holds promise for research in the field of LDHA-related antitumor therapies .
|
-
- HY-100022
-
|
eFT508
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-180214
-
|
|
HDAC
|
Cardiovascular Disease
Neurological Disease
|
|
HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
|
-
- HY-W015892
-
|
γ-Caprolactone
|
Interleukin Related
TNF Receptor
Insecticide
|
Infection
|
|
γ-Hexalactone (γ-Caprolactone) is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage in human lymphocytes and HepG2 cells, modulates cytokine secretion in human lymphocytes, and reduces recombinant PON1 activity. γ-Hexalactone serves as a dose-dependent oviposition inhibitor against Bactrocera oleae. γ-Hexalactone can be used for the research of Bactrocera oleae pest management .
|
-
- HY-178740
-
|
|
Bacterial
EGFR
|
Infection
|
|
GI261520A is a egfr/erbb2 dual inhibitor. GI261520A inhibits PhoQ phosphorylation dose-dependently. GI261520A can downregulate the activity levels of PhoP/PhoQ. GI261520A inhibits pagC reporter expression levels with an IC50 of 3.2 μM. GI261520A inhibits PhoQc autokinase activtiy by 80%. GI261520A can permeate the eukaryotic plasmatic and vascular cell membranes and reach intravacuolar Salmonella to block intramacrophage proliferation .
|
-
- HY-145814
-
|
|
HSP
Fungal
|
Infection
|
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
|
-
- HY-180409
-
|
|
Androgen Receptor
|
Cancer
|
|
YM580 is a potent, orally active and selective Androgen Receptor (AR) antagonist (IC50 = 0.11 μM, hAR Ki = 4.6 nM, rAR Ki = 6.2 nM). YM580 exhibits good selectivity over PR, GR, and ERα (Kis > 3300 nM). YM580 decreases ventral prostate weight in mature intact rats dose-dependently without affecting serum testosterone levels. YM580 can be used for the research of prostate cancer .
|
-
- HY-118665
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
L-736380 is a high affinity CCK-B (cholecystokinin B receptor) receptor antagonist, with IC50 values of 0.054 nM and 400 nM for CCK-B and CCK-A, respectively. L-736380 dose-dependently inhibits gastric acid secretion in anesthetized rats (ID50, 0.064 mg/kg) and ex vivo binding of [125I]CCK-8S in BKTO mice brain membranes (ED50, 1.7 mg/kg) .
|
-
- HY-177559
-
|
|
NEKs
Interleukin Related
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NEK7 degrader-2 (Compound 25) is a NEK7 degrader. NEK7 degrader-2 shows dose-dependent NEK7 degradation ability in human PBMC-derived macrophages. NEK7 degrader-2 reduce the release level of pro-inflammatory cytokines IL-1β induced by NLRP3 inflammasome activation. NEK7 degrader-2 can be used for the study of inflammatory diseases .
|
-
- HY-176063
-
|
|
TRP Channel
Opioid Receptor
|
Neurological Disease
|
|
TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .
|
-
- HY-N18953
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Heparin disaccharide I-H trisodium (Compound SHS-5) is a heparin-derived disaccharide. Heparin disaccharide I-H trisodium blocks the spontaneous secretion of IL-8 and IL-1β in intestinal epithelial cells at the post-translational stage without reducing mRNA expression levels or intracellular contents. Heparin disaccharide I-H trisodium exhibits dose-dependent anti-inflammatory activity in intestinal epithelial cell models .
|
-
- HY-W008634
-
|
U-54461; U-54461S; PNU-54461
|
Toll-like Receptor (TLR)
|
Cancer
|
|
Bropirimine (U-54461; U-54461S; PNU-54461) is an orally active TLR7 agonist. Bropirimine inhibits RANKL-induced osteoclast differentiation of mouse bone marrow-derived macrophages (BMMs). Bropirimine exhibits dose-dependent direct inhibitory effects on colony formation of cultured KK-47 and 724 cells. Bropirimine can be used for the study of cancers and bone metabolic disorders such as osteoporosis .
|
-
- HY-10281
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-157164
-
|
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PROTAC EZH2 Degrader-2 is a PROTAC EZH2 inhibitor. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
|
-
- HY-176051
-
|
RgE
|
GLUT
|
Cancer
|
|
Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [ 3H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC50 values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells .
|
-
- HY-128661
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Metabolic Disease
|
|
IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor that exerts its activity through covalent modification of His315 with an IC50 value of 110 nM. IDH1 Inhibitor 2 can dose-dependently reduce the intracellular reduced glutamine metabolic flux, thereby affecting cellular metabolic homeostasis. IDH1 Inhibitor 2 can be used to study the role of IDH1 in cellular metabolic regulation and cancer development .
|
-
- HY-170579
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
NF-κB
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Antioxidant agent-20 (Compound 3d) has potent anti-inflammatory and antioxidant activity. Antioxidant agent-20 reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 exhibits photoprotective effect against UVB-irradiated human skin keratinocytes (HaCaT) (IC50=5.13 µM) via activation of Nrf2/HO-1 signaling and inhibition of NF-κB pathway .
|
-
- HY-118304
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .
|
-
- HY-18060A
-
|
TC-5619 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-100481
-
|
RPR101048
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
|
-
- HY-107915
-
|
(-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-18056R
-
|
|
11β-HSD
|
Metabolic Disease
|
|
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
|
-
- HY-18060
-
|
TC-5619
|
nAChR
|
Neurological Disease
|
|
Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-B0380B
-
|
GIC-1001
|
Biochemical Assay Reagents
|
Others
|
|
Trimebutine 3-TCBS (GIC-1001) is an innovative formulation designed to release hydrogen sulfide (H2S) in vivo. This compound combines trimebutine with an H2S-releasing antagonist (phenyl 3-thiocarbamate) and exhibits enhanced anti-nociceptive effects in a mouse colonic distension model, superior to conventional trimebutine. GIC-1001 can reduce visceral pain and discomfort associated with lumen distension in a dose-dependent manner, showing potential superiority .
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- HY-N3017
-
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Antibiotic
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Neurological Disease
Inflammation/Immunology
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Artemitin is a flavonoid neuroanesthetic agent with moderate cytotoxicity. Artemitint has selective inhibitory activity against Meth-A sarcoma cells with an ED50 of 5-10 μg/mL, and has no significant effect on LLC lung cancer cells. Artemitin exerts anticancer activity by affecting cell proliferation signaling pathways, and also has potential anti-inflammatory and neuroprotective effects. Artemitin exhibits a dose-dependent antinociceptive effect in the mouse hot plate test, with an ED50 of 1.6 μg/kg, and has analgesic activity .
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- HY-N9182
-
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Physalien
|
Adiponectin Receptor
P2X Receptor
Autophagy
|
Inflammation/Immunology
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Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .
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- HY-107387
-
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PI3K
|
Metabolic Disease
Inflammation/Immunology
|
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PF-376304 is an orally active non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor with an IC50 of 0.197 μM against PI3Kγ. PF-376304 induces dose-dependent glucose and lipid metabolic disorders in rats, causes rapid death at high doses, and leads to metabolic abnormalities that are self-reversible at low doses. PF-376304 is applicable to the research of metabolic and inflammatory diseases .
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- HY-B1246R
-
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Reference Standards
Bacterial
Proton Pump
|
Infection
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Thonzonium (bromide) (Standard) is the analytical standard of Thonzonium (bromide). This product is intended for research and analytical applications. Thonzonium bromide is an antibacterial agent that is structurally similar to Farnesol (HY-Y0248A). Thonzonium bromide is also a monocationic surface-active agent, which inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo. Thonzonium bromide inhibits proton transport in a dose-dependent manner (EC50=69 μM) .
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- HY-168615
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IKZF Family
Casein Kinase
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Cancer
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MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research .
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- HY-W727481
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Parasite
Insecticide
|
Infection
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|
Cyetpyrafen is a pyrazole insecticide/acaricide with broad-spectrum insecticidal activity. Cyetpyrafen binds to DhelOBP4 (Ki = 4.95 μM) and DhelOBP21 (Ki = 5.51 μM) to mediate olfactory recognition in *Cryptolaemus montrouzieri*. Cyetpyrafen induces dose-dependent electroantennogram responses in *Cryptolaemus montrouzieri* and exhibits repellent effects on the species. Cyetpyrafen has bioaccumulative properties, is rapidly and passively absorbed by the roots of lettuce and rice, reaches a steady state within 24 h, preferentially accumulates in roots, and shows limited xylem/phloem translocation .
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- HY-108630R
-
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Reference Standards
Phospholipase
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Others
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U-73343 (Standard) is the analytical standard of U-73343 (HY-108630). This product is intended for research and analytical applications. U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC .
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- HY-113439S
-
|
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Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
12-HETE-d8 is the deuterium labeled 12-HETE. 12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway .12-HETE has both anti-thrombotic and pro-thrombotic effects . 12-HETE is a neuromodulator .
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- HY-N11910
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Biochemical Assay Reagents
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Others
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Kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl (1→3) α-rhamnopyranoside]-7-O-α-rhamnopyranoside (Compound 3) is a wound healing agent with dose-dependent wound healing ability. Kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl (1→3) α-rhamnopyranoside]-7-O-α-rhamnopyranoside can be used for wound repair research .
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![Kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl (1→3) α-rhamnopyranoside]-7-O-α-rhamnopyranoside](//file.medchemexpress.com/product_pic/hy-n11910.gif)
- HY-173559
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Androgen Receptor
|
Cancer
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AR antagonist 12 (compound 20i) is an orally active androgen receptor antagonist wiith IC50 values of 119.3 μM and 98.2 μM for wt-AR and AR-F877L,respectively. AR antagonist 12 induces a dose-dependent and time-dependent reduction in AR, AR-V7, and PSA protein levels. AR antagonist 1 shows anticancer activuty and can be used for the study of Enzalutamide (HY-70002)-resistant Prostate cancer .
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- HY-158031
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Apoptosis
Polo-like Kinase (PLK)
Epigenetic Reader Domain
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Cancer
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PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .
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- HY-181562
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DNA/RNA Synthesis
|
Cancer
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WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer .
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- HY-157325
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RIP kinase
|
Inflammation/Immunology
|
|
RIPK2-IN-5 (compound 14) is a high affinity and excellent selectivity RIPK2 inhibitor with an IC50 value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases .
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- HY-177573
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GABA Receptor
|
Neurological Disease
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Cholesteryl γ-aminobutyrate is a γ-aminobutyric acid (GABA)-mimetic prodrug. Cholesteryl γ-aminobutyrate inhibits the orthodromically-evoked discharge of pyramidal cells in the CA1 region of the hippocampus. Cholesteryl γ-aminobutyrate suppresses the open-field activity of mice and rats in a dose-dependent manner and inhibits Bicuculline (HY-N0219)-induced seizures in mice. Cholesteryl γ-aminobutyrate can be used for the study of CNS diseases related to impaired GABAergic neuronal function .
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- HY-160943A
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|
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SARS-CoV
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Infection
|
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F594-1001 (compound 6) hydrochloride is a potent and highly selective SARS-CoV-2 Mac1-ADP-ribose inhibitor with IC50s of 8.5 μM, 68 μM and 45 μM for SARS-CoV-2 in AS, FP, and FRET assays, respectively. F594-1001 hydrochloride directly binds to SARS-CoV-2 Mac1 and exhibits a dose-dependent inhibition of Mac1 ADP-ribosylhydrolase activity .
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- HY-145649A
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AD-85481 sodium; ALN-AGT sodium
|
Small Interfering RNA (siRNA)
Asialoglycoprotein Receptor (ASGPR)
|
Cardiovascular Disease
|
|
Zilebesiran (AD-85481; ALN-AGT) sodium is a long-acting liver-targeted small interfering RNA (siRNA) antihypertensive agent. Zilebesiran sodium binds to the hepatic asialoglycoprotein receptor (ASGPR), activates the RNA-induced silencing complex to degrade hepatic angiotensinogen mRNA, thereby inhibiting the gene expression and synthesis of angiotensinogen. Zilebesiran sodium dose-dependently reduces serum angiotensinogen levels and 24-hour ambulatory blood pressure, with its effect persisting throughout the circadian cycle. Zilebesiran sodium is applicable to research related to hypertension .
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-
- HY-160943
-
|
|
SARS-CoV
|
Infection
|
|
F594-1001 (compound 6) is a potent and highly selective SARS-CoV-2 Mac1-ADP-ribose inhibitor with IC50s of 8.5 μM, 68 μM and 45 μM for SARS-CoV-2 in AS, FP, and FRET assays, respectively. F594-1001 directly binds to SARS-CoV-2 Mac1 and exhibits a dose-dependent inhibition of Mac1 ADP-ribosylhydrolase activity .
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- HY-18060B
-
|
TC-5619 tosylate
|
nAChR
|
Inflammation/Immunology
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline tosylate exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline tosylate possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline tosylate requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline tosylate is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
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- HY-108020
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Free Fatty Acid Receptor
|
Endocrinology
|
|
LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus . LY2881835 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-N0303
-
|
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Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
|
Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM) . Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells . Idebenone quickly crosses the blood-brain barrier.
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- HY-172621
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|
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EGFR
|
Cancer
|
|
EGFR-IN-159 (compound 12), a dihydropyrimidine, is a potent EGFR inhibitor with an IC50 value of 29.00 nM. EGFR-IN-159 exhibits dose-dependent inhibition against EGFR and HER2. EGFR-IN-159 shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 has no BBB permeation. EGFR-IN-159 shows appreciable anti-cancer activity .
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- HY-N15347
-
|
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NF-κB
p38 MAPK
Interleukin Related
TNF Receptor
NO Synthase
COX
|
Inflammation/Immunology
|
|
Talaromyketide B is a polyketide compound with anti-inflammatory activity, discovered in the soil bacterium Talaromyces sp. KYS-41. Talaromyketide B inhibits the activation of the NF-κB and MAPK signaling pathways and dose-dependently suppresses pro-inflammatory cytokines, such as IL-1β, IL-6, IL-10, and TNF-α, as well as the transcriptional activity of inflammatory mediators, including iNOS and COX-2. Talaromyketide B holds potential for research in the fields of immunity and inflammatory diseases .
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-
- HY-118304B
-
|
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FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
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- HY-105271
-
|
S-(+)-S-312-d
|
Calcium Channel
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Others
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|
S-312-d (S-(+)-S-312-d) is a calcium channel blocker with the activity of protecting the kidney from ischemic acute renal failure. S-312-d (0.01-0.1mg/kg b.wt. iv) administered before ischemia has a dose-dependent protective effect on ischemia-induced renal damage, improves the survival rate of ischemic rats, and reduces renal cortical edema and the increase in renal tissue calcium content.
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- HY-176860
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-
- HY-16913
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-
- HY-123440
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-
- HY-149897
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Transmembrane Glycoprotein
CD44
|
Cancer
|
|
HA-CD44 interaction inhibitor 2 is a CD44 inhibitor that can inhibit the interaction between Hyaluronic acid (HA) (HY-B0633A) and CD44. HA-CD44 interaction inhibitor 2 acts as an antiproliferative agent against CD44 + cancer cells. HA-CD44 interaction inhibitor 2 can disrupt the integrity of cancer spheres and reduce cancer cell viability in a dose-dependent manner. HA-CD44 interaction inhibitor 2 is applicable for tumor research .
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- HY-120321
-
|
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Mineralocorticoid Receptor
Carbonic Anhydrase
|
Cardiovascular Disease
|
|
DSR-71167 is an orally active mineralocorticoid receptor (MR) antagonist with an IC50 of 0.26 μM. DSR-71167 exhibits weak carbonic anhydrase (CA) inhibitory activity with an IC50 of 19 μM. DSR-71167 can dose-dependently increase urinary sodium excretion in rat models and has a very low risk of hyperkalemia in potassium-loading rat models. DSR-71167 lowers systolic blood pressure in hypertensive rat models. DSR-71167 can be used for research on hypertension and heart failure .
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- HY-182021
-
|
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Amine N-methyltransferase
|
Endocrinology
|
|
NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC50 values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC50 of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis .
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- HY-N15309
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|
Torvoside K
|
Fungal
|
Infection
|
|
Torvoside C (Torvoside K) is a compound found in Solanum torvum with antifungal activity. The ZOIs and MIC values of Torvoside C against the tested fungi (Alternaria brassicicola, Alternaria geophila, Aspergillus flavus, etc.) range from 33.4% to 87.4% and 31.25 to 250 μg/mL, respectively. Additionally, it exhibits a dose-dependent inhibitory effect on the production of mycotoxins aflatoxin B1 and fumonisin B1, which are produced by A. flavus and F. verticillioides, respectively. Torvoside C can be used for research in the field of antifungal infection .
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-
- HY-B2078
-
|
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Neurokinin Receptor
|
Inflammation/Immunology
|
|
Eprazinone can enhance lung function and arterial oxygen levels and can be used in the study of chronic bronchitis. Higher doses of eprazinone increased phospholipid levels and decreased neutral lipid content in bronchoalveolar lavage (BAL) fluid, but had no effect on protein and cell levels in BAL. Eprazinone dose-dependently reduced short-circuit current (Isc), primarily by reducing chloride secretion at lower concentrations and affecting sodium and chloride transport at higher doses. Eprazinone may exert its anti-inflammatory effects by regulating BAL lipid composition and airway ion transport .
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-
- HY-180537
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 57 is a apoptosis inducer and Thymidylate Synthase (TS) inhibitor. Apoptosis inducer 57 exhibits cytotoxic activity against SW480 and MCF-7 cancer cells with IC50 values of 15.7 and 16.5 µM, and induces dose-dependent apoptosis and S-phase cell cycle arrest. Apoptosis inducer 57 stalely binds the TS active site via interactions with Asp218 and Met311. TS-IN-9 can be used for breast cancer and colorectal cancer research .
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-
- HY-143792
-
|
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Huntingtin
P-glycoprotein
|
Neurological Disease
|
|
HTT-D3 is an orally active, blood-brain barrier penetrant splicing modulator of huntingtin (HTT). HTT-D3 promotes the inclusion of a pseudo-exon containing a premature termination codon into HTT pre-mRNA, triggers nonsense-mediated mRNA degradation and reduces HTT protein levels. HTT-D3 induces dose-dependent, comparable reductions in mutant HTT protein in both the brain and peripheral tissues of transgenic mouse models. HTT-D3 can be used for the research of Huntington's disease .
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-
- HY-123972
-
|
KL-2
|
DNA/RNA Synthesis
|
Cancer
|
|
SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
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-
- HY-172903
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Nav1.8-IN-16 (Compound (R)-40) is an orally active and selective hNaV 1.8 inhibitor (IC50: 5.9 nM). Nav1.8-IN-16 exerts analgesic effects by blocking NaV1.8 channels without significantly affecting other NaV subtypes or hERG channels. Nav1.8-IN-16 exhibits dose-dependent analgesic effects in postoperative pain and inflammatory pain models and can be used in pain-related research .
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-
- HY-180244
-
|
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Protease Activated Receptor (PAR)
p38 MAPK
|
Cancer
|
|
P2L-003 is a selective PAR2 antagonist with an IC50 of 0.62 μM in HT-29 cells. P2L-003 blocks PAR2-mediated Ca 2+ mobilization without affecting PAR1, PAR4, or ATP-mediated signaling and dose-dependently suppresses the downstream MAPK signaling cascades, including ERK1/2 and p38 phosphorylation. P2L-003 can be used for colon cancer research .
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-
- HY-178149
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-A/B-IN-5 is an orally active MAO-A (IC50 = 73.88 μM) and MAO-B (IC50 = 91.08 μM) inhibitor. MAO-A/B-IN-5 reverses Sodium nitroprusside (SNP) (HY-B0564)-induced cerebral lipid peroxidation (IC50 = 130.2 μM) and protein carbonylation (IC50 = 229.8 μM). MAO-A/B-IN-5 shows dose-dependent and time-dependent antidepressant-like efficacy in mice. MAO-A/B-IN-5 can be used for the study of depressive disorder .
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-
- HY-119298
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
AW-814141 is a selective and orally active p38 MAP kinase inhibitor. AW-814141 has an IC50 values of 100 nM and 158 nM for p38-α and β isoforms, respectively. AW-814141 can inhibit the production of TNF-α induced by LPS (HY-D1056). AW-814141 can inhibit paw edema in rats in a dose-dependent manner. AW-814141 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases such as rheumatoid arthritis .
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-
- HY-163987
-
|
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Sirtuin
|
Neurological Disease
|
|
SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 improved the thermal stability of SIRT3 in SH-SY5Y cells, indicating that it can directly bind to SIRT3, has SIRT3 dependency in SH-SY5Y to clear α-Syn. SIRT3 activator 2 improves motor function in Parkinson mice, preventing Parkinson (DA) neuron loss in the substantia nigra in a dose-dependent manner .
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-
- HY-124547
-
|
|
Endogenous Metabolite
|
Others
|
|
2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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-
- HY-E70541B
-
|
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
|
Canine Factor IX is a functional coagulation factor. Canine Factor IX shortens whole blood clotting time and activated partial thromboplastin time, and restores coagulation function. After intramuscular administration via rAAV vector in hemophilia B dogs, Canine Factor IX maintains a sustained circulating level for at least 1 year, partially corrects the hemophilia B phenotype in a dose-dependent manner, and its plasma expression persists for more than 17 months. Canine Factor IX is applicable to relevant research on hemophilia B .
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-
- HY-156815
-
|
|
Orphan GPCR
|
Neurological Disease
Inflammation/Immunology
|
|
YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain .
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-
- HY-182301
-
|
|
Renin
|
Cardiovascular Disease
|
|
CP 71362 is a renin inhibitor, a highly potent substrate-analog transition state mimic with antihypertensive properties. CP 71362 exhibits significant inhibitory activity against plasma renin from rats, dogs, and humans (IC50 values are 3 nM, 0.0033 nM, and 20 nM, respectively). CP 71362 reduces the mean arterial pressure of anesthetized and conscious sodium-depleted animals in a dose-dependent manner, and has pharmacokinetic characteristics of rapid elimination and short duration of action. CP 71362 can be used in research related to hypertension and congestive heart failure .
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-
- HY-N0407R
-
|
6'-Cinnamoylcatalpol (Standard)
|
Reference Standards
STAT
|
Inflammation/Immunology
|
|
Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
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-
- HY-123461
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Sul-121 hydrochloride is a novel compound with anti-oxidative capacity that effectively inhibits airway inflammation and hyperresponsiveness (AHR) in experimental models of chronic obstructive pulmonary disease (COPD). Sul-121 hydrochloride prevents lipopolysaccharide-induced airway neutrophilia and AHR in a dose-dependent manner. Sul-121 hydrochloride also demonstrates the ability to reduce oxidative stress markers in human airway smooth muscle cells. Sul-121 hydrochloride inhibits nuclear translocation of the NF-κB subunit, p65, thereby diminishing pro-inflammatory cytokine release.
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-
- HY-146169
-
|
|
Reactive Oxygen Species (ROS)
Microtubule/Tubulin
|
Cancer
|
|
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 μM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner . Antitumor agent-68 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-P0249
-
-
- HY-121020
-
|
|
SARS-CoV
|
Infection
Others
Inflammation/Immunology
|
|
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin induces dose-dependent relaxation of ileum and pulmonary artery smooth muscle, causes slight urinary bladder smooth muscle contraction at highest tested concentrations. Arcapillin binds to the active site of SARS-CoV-2 Mpro via interactions with Gln139, His163, and His164, exhibits antiviral activity against SARS-CoV-2 and MERS-CoV. Arcapillin can be used for the research of gastrointestinal disorders, COVID-19, and Middle East respiratory syndrome (MERS) .
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-
- HY-167848
-
|
XL-118
|
Others
|
Cardiovascular Disease
|
|
DMP-728 free base (XL-118) is a highly potent and selective GPIIb/IIIa antagonist with antiplatelet and antithrombotic activities. DMP-728 free base can inhibit ADP-induced human platelet aggregation in vitro, with an IC50 of 46 nmol/L, and can significantly reduce the interaction between fibrinogen and human platelets or Binding of purified human GPIIb/IIIa receptors. DMP-728 free base exhibits dose-dependent antiplatelet effects in anesthetized mongrel dogs, effectively inhibiting ADP-induced platelet aggregation and prolonging template bleeding time .
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-
- HY-164525
-
|
SC-81490; PF-02881307
|
MMP
|
Cancer
|
|
SD-7300 (SC-81490) is an orally active inhibitor of MMP-2, MMP-9, and MMP-13 with Ki values ??of 0.03, 0.01, and 0.03 nM, respectively. SD-7300 can reduce the degradation of extracellular matrix by tumor cells, thereby inhibiting the invasion and metastasis of tumor cells. In addition, SD-7300 is also a dose-dependent inhibitor of mouse corneal angiogenesis and an inhibitor of interleukin-1-induced bovine cartilage degradation. SD-7300 can be used in breast cancer research .
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-
- HY-N6609
-
|
|
nAChR
|
Others
|
|
Magnocurarine is a neuromuscular junction blocker that inhibits muscle contraction by functionally blocking signal transmission without directly damaging nerve or muscle tissues. In frog, mouse and rabbit models, Magnocurarine exerts a dose-dependent paralytic effect, which progresses gradually from limb weakness and loss of righting reflex to respiratory depression and even cardiac arrest. Although high doses cause complete cessation of movement, Magnocurarine does not affect the spinal multineuronal reflex in frogs. Magnocurarine exhibits biological activity similar to that of tubocurarine (HY-125901) in various animal models .
|
-
- HY-136634
-
|
|
mAChR
|
Others
|
|
BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guinea pig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.
|
-
- HY-175530
-
|
|
OLIG2
|
Cancer
|
|
OLIG2-IN-1 is a potent and selective oligodendrocyte transcription factor 2 (OLIG2) inhibitor. OLIG2-IN-1 directly and dose-dependently downregulates nuclear OLIG2 levels with an IC50 value of 0.88 μM. OLIG2-IN-1 exhibits strong anti-proliferative activity in U87 and U251 cells with IC50 values of 7.02 μM and 6.43 μM, respectively. OLIG2-IN-1 can be used for the research of cancer, such as glioblastoma multiforme .
|
-
- HY-N12461
-
|
|
Bacterial
Caspase
Apoptosis
|
Infection
|
|
Cucurbitacin F is a tetracyclic protostane-type triterpenoid with low toxicity, antibacterial and anti-inflammatory activities, and is also a related compound of Cucurbitacin B (HY-N0416). Cucurbitacin F widely exists in plants such as Cucurbitaceae plants, Quisqualis indica and Sorbaria sorbifolia. Cucurbitacin F acts as an actin aggregator and reduces cell viability in a dose-dependent manner. Cucurbitacin F induces apoptosis by triggering G2/M phase cell cycle arrest and activating the caspase-3-dependent apoptosis .
|
-
- HY-121554
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Kojic amine is an orally active γ-aminobutyric acid (GABA) analog. Kojic amine acts as a GABA mimic that inhibits sodium-independent [ 3H]GABA binding to rat brain cell membranes. Kojic amine reduces flexor spasms in chronic spinal rat and cat models. Kojic amine prevents tonic extensor convulsions in mice. Kojic amine produces a transient, dose-dependent analgesic effect in the mouse hot-plate test. Kojic amine can be used in research related to skeletal muscle spasm, epilepsy and analgesia [1][2]
|
-
- HY-N1393
-
|
NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether
|
Carbonic Anhydrase
Phospholipase
|
Cardiovascular Disease
|
|
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
|
-
- HY-118304A
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML) .
|
-
- HY-N6609B
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Magnocurarine chloride is a neuromuscular junction blocker that inhibits muscle contraction by functionally blocking signal transmission without directly damaging nerve or muscle tissues. In frog, mouse and rabbit models, Magnocurarine chloride exerts a dose-dependent paralytic effect, which progresses gradually from limb weakness and loss of righting reflex to respiratory depression and even cardiac arrest. Although high doses cause complete cessation of movement, Magnocurarine chloride does not affect the spinal multineuronal reflex in frogs. Magnocurarine chloride exhibits biological activity similar to that of tubocurarine (HY-125901) in various animal models .
|
-
- HY-179228
-
|
|
CTLA-4
TGF-beta/Smad
|
Cancer
|
|
AN02 is a derivative of Curcumin (HY-N0005). AN02 inhibits the proliferation and clonogenicity, migration and invasion of ovarian cancer cells. AN02 dose-dependently upregulates the expression of APC and mediates the degradation of CTLA-4 through SMAD4. In the small xenograft model, AN02 significantly inhibits tumor growth and reverses the tumor immune-suppressive microenvironment. AN02, when combined with Ipilimumab (HY-P9901), can enhance efficacy and inhibit epithelial-mesenchymal transition. AN02 can be used for the study of ovarian cancer .
|
-
- HY-178921
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
HJ-4 is a Piperine (HY-N0144) derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC) .
|
-
- HY-N6954
-
|
|
ATM/ATR
STAT
CDK
Hedgehog
|
Inflammation/Immunology
Cancer
|
|
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active .
|
-
- HY-12624
-
|
ON123300
|
CDK
AMPK
PDGFR
|
Cancer
|
|
Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
|
-
- HY-121586
-
|
Bay g 6575
|
Lipoxygenase
|
Cardiovascular Disease
|
|
Nafazatrom (Bay g 6575) is an orally active cardioprotective agent that protects against ischemic damage. Nafazatrom dose-dependently inhibits neutrophil aggregation, superoxide anion generation, arachidonic acid metabolism, and to a lesser extent the release of β-glucosidase, platelet aggregation or arachidonic acid in vitro. Acid metabolism has no significant effect. In a dog ischemia-reperfusion model, Nafazatrom (10 mg/kg; po) reduced infarct size and the occurrence of arrhythmias and rescued ischemic myocardial function without affecting any hemodynamic changes. The basis of Nafazatrom's cardioprotection may be inhibition of neutrophil function and cellular infiltration in vitro .
|
-
- HY-101906R
-
|
|
Reference Standards
Free Fatty Acid Receptor
Apoptosis
|
Metabolic Disease
|
|
DC260126 (Standard) is the analytical standard of DC260126 (HY-101906). This product is intended for research and analytical applications. DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively) . DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis .
|
-
- HY-181559S
-
|
AG06827
|
mAChR
|
Neurological Disease
|
|
VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M4 mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC50 of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease .
|
-
- HY-P991561
-
|
|
CD47
|
Cancer
|
|
AO-176 is a humanized anti-CD47 IgG2 monoclonal antibody. AO-176 induces tumor phagocytosis through blocking the CD47-SIRPα interaction. AO-176 preferentially binds to tumor versus normal cells and directly kills tumor by a cell autonomous mechanism not ADCC (antibody-dependent cell-mediated cytotoxicity). AO-176 demonstrates dose-dependent antitumor activity in tumor xenograft models. AO-176 can be used for the researches of cancer, such as lymphoma .
|
-
- HY-19210
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
|
-
- HY-155027
-
|
|
Dipeptidyl Peptidase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
DPP-4-IN-8 (compound 27) is a potent and selective DPP4 (dipeptidyl peptidase 4) inhibitor, with a Ki of 0.96 μM. DPP-4-IN-8 blocks the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells. DPP-4-IN-8 also dose-dependently suppresses the expression levels of the chemokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) .
|
-
- HY-N0340
-
|
Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
- HY-165456
-
|
|
Adrenergic Receptor
Vasopressin Receptor
|
Endocrinology
|
|
AGN-190851 is a potent and selective agonist of α2-adrenergic receptor (α2 adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α2-adrenergic receptor subtypes, and parturition .
|
-
- HY-P0249B
-
-
- HY-150739A
-
-
- HY-WAA0304
-
|
|
5-HT Receptor
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
|
|
1-(4-Aminobutyl) guanidine (Agmatine) is an orally active analgesic that can cross the blood-brain barrier. 1-(4-Aminobutyl) guanidine targets the 5-HT2A receptor, 5-HT3 receptor, α2-adrenergic receptor, and I1 imidazoline receptor. 1-(4-Aminobutyl) guanidine produces dose-dependent analgesic effects in various pain models. 1-(4-Aminobutyl) guanidine can be used in research related to visceral pain, neuropathic pain, and inflammatory pain .
|
-
- HY-101235
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ICI 185282 is a potent, selective, orally active thromboxane A2 (TXA₂) receptor antagonist. ICI 185282 causes dose-dependent inhibition of U-46619 (HY-108566)-induced platelet aggregation ex-vivo in guinea-pig. ICI 185,282 inhibits bronchospasm induced by U-46619, PGD2 (HY-101988), PGF2α (HY-12956), arachidonic acid (HY-109590), LTD4 and PAF (HY-108635) in vivo. ICI 185282 can be used for bronchial asthma research .
|
-
- HY-115860
-
|
|
iGluR
|
Neurological Disease
|
|
TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects .
|
-
- HY-178355
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
Anti-osteoporosis agent-12 (Compound 18) is an orally active pyrazole-fused betulinic acid derivative with potent anti-osteoporosis activity. Anti-osteoporosis agent-12 exhibits a strong inhibitory effect on RANKL-induced osteoclastogenesis in RAW264.7 cells, with an IC50 of 7.96 nM. Anti-osteoporosis agent-12 can dose-dependently improve key micro-CT parameters of bone, reduce the level of serum bone resorption marker (CTx), and effectively prevent ovariectomy-induced bone loss. Anti-osteoporosis agent can be used for the study of osteoporosis .
|
-
- HY-137131
-
|
DC-Cholesterol hydrochloride
|
Amyloid-β
Liposome
IFNAR
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
|
-
- HY-175846
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
TQFL13 is derivative of Thymoquinone (TQ) (HY-D0803) with potent anti-breast cancer activity. TQFL13 exhibits higher cytotoxicity against breast cancer cells (BT549, MDA-MB-231, 4T1). TQFL13 increases apoptosis and blocks the cell cycle at S and G2/G1 phases in breast cancer cells. TQFL13 shows dose-dependent anti-tumor efficacy in mouse breast cancer allograft model. TQFL13 can be used for the study of breast cancer .
|
-
- HY-P992052
-
|
|
|
Inflammation/Immunology
|
|
Anti-CD11a Antibody (AL-57) is a monoclonal antibody targeting human CD11a. Anti-CD11a Antibody (AL-57) binds to HA cells in a dose-dependent manner but did not bind to LA cells. Anti-CD11a Antibody (AL-57) preferentially binds to the active conformation of LFA-1 and blocks LFA-1-mediated adhesion and lymphocyte proliferation. Anti-CD11a Antibody (AL-57) can be used for the research of inflammatory and autoimmune diseases .
|
-
- HY-181506
-
|
|
Fluorescent Dye
Molecular Glues
CaMK
c-Myc
Bcl-2 Family
Cadherin
|
Cancer
|
|
TYMJ-01 is a fluorescent probe and eEF2K degrader. TYMJ-01 induces dose-dependent and specific degradation of eEF2K via the ubiquitin-proteasome pathway, with a DC50 of 82 nM. TYMJ-01 inhibits the proliferation, migration and invasion of triple-negative breast cancer cells. TYMJ-01 enables dynamic fluorescent imaging of eEF2K degradation in triple-negative breast cancer cells; it enhances the anti-tumor activity of Paclitaxel (HY-B0015). TYMJ-01 can be used for the research of triple-negative breast cancer .
|
-
- HY-158821A
-
|
|
TGF-beta/Smad
|
Neurological Disease
|
|
ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases .
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-151799
-
|
|
p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
|
-
- 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)
|
-
- HY-121634
-
|
|
Polo-like Kinase (PLK)
|
Others
|
|
DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.
|
-
- HY-107551
-
|
|
Hedgehog
Gli
|
Cancer
|
|
Hh Pathway-IN-1, a Hedgehog (Hh) pathway inhibitor, is a potent Gli antagonist. Hh Pathway-IN-1 inhibits Hh pathway functional with an IC50 value of 1.1 µM in C3H10T1/2 cells. Hh Pathway-IN-1 does not inhibit Wnt signaling. Hh Pathway-IN-1 shows anti-proliferative activity. Hh Pathway-IN-1 decreases the GLI1 mRNA expression. Hh Pathway-IN-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-183143
-
|
|
Topoisomerase
Apoptosis
TNF Receptor
PARP
STAT
P-glycoprotein
|
Cancer
|
|
Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer .
|
-
- HY-170574
-
|
|
Molecular Glues
Apoptosis
RIO Kinase
|
Cancer
|
|
CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .
|
-
- HY-178327
-
|
|
DGK
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
DGKα/ζ-IN-2 is a potent, orally active and selective dual DGKα/ζ inhibitor with IC50 values of 23 nM (DGKα) and 1.2 nM (DGKζ). DGKα/ζ-IN-2 exhibits selectivity over other DGK isoforms, such as DGKβ and DGKγ. DGKα/ζ-IN-2 shows robust and dose-dependent immune activation in the presence of antigen presentation in an OT-1 murine model. DGKα/ζ-IN-2 can be used for antitumor immunity .
|
-
- HY-N0303R
-
|
|
Reference Standards
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
|
Idebenone (Standard) is the analytical standard of Idebenone. This product is intended for research and analytical applications. Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM) . Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells . Idebenone quickly crosses the blood-brain barrier.
|
-
- HY-107915R
-
|
(-)-Cobefrin (Standard); (-)-α-Methylnoradrenaline (Standard); (-)-Nordefrin (Standard)
|
Reference Standards
Adrenergic Receptor
|
Others
|
|
Levonordefrin (Standard) is the analytical standard of Levonordefrin. This product is intended for research and analytical applications. Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism .
|
-
- HY-163527
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-101317A
-
|
SB-205607
|
Opioid Receptor
|
Metabolic Disease
|
|
TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
|
-
- HY-18940
-
|
Cilo
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Cilobradine (Cilo) is a HCN channel blocker with heart rate reducing activity. Cilobradine blocks the slow inward current of human HCN1, HCN2, HCN3, and HCN4 channels. Cilobradine has a slightly higher efficiency in blocking endogenous If in mouse sinoatrial node cells (IC50 value is 0.62μM). Cilobradine can dose-dependently reduce the heart rate from 600 to 200 bpm with an ED50 value of 1.2 mg/kg. Cilobradine induces arrhythmias at doses greater than 5 mg/kg, which are characterized by periodic fluctuations between T waves and P waves .
|
-
- HY-170418
-
|
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
ALK/ROS1-IN-5 (compound X4) is a selective ALK and ROS1 kinases inhibitor with IC50s of 0.512 μM (ALK), 0.766 μM (ROS1), respectively. ALK/ROS1-IN-5 inhibits H2228 cells with an IC50 of 0.034 μM. ALK/ROS1-IN-5 induces cancer cells apoptosis in dose-dependent manner. ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells[1].
|
-
- HY-148252
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
|
-
- HY-172883
-
|
|
FABP
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65 μM and 1.08 μM for FABP1 and FABP4, EC50 s of 9.19 μM, 2.20 μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
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-
- HY-145453
-
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|
Interleukin Related
|
Inflammation/Immunology
|
|
Propacetamol is an orally active prodrug of Acetaminophen (HY-66005), which exerts antipyretic and analgesic effects after metabolism. Propacetamol reduces Aspirin (ASA) (HY-14654)-induced elevation of malondialdehyde (MDA) in gastric mucosa and plasma, regulates the levels of gastric mucosal glutathione (GSH and GSSG) to maintain cellular antioxidant defense, and increases gastric mucosal uric acid (UA) levels. Propacetamol exerts a dose-dependent protective effect against ASA-induced gastric mucosal damage in rats. Propacetamol can be used for the study of gastric mucosal injury by interfering with oxidative stress .
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-
- HY-158821
-
|
|
TGF-beta/Smad
|
Neurological Disease
|
|
ISTH0036 is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases .
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-
- HY-148817
-
|
|
WDR5
|
Cancer
|
|
WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer .
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-
- HY-170947
-
|
|
STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
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-
- HY-112650
-
-
- HY-147391
-
|
|
Sodium Channel
|
Neurological Disease
|
|
ASIC-IN-1 is a potent acid sensing ion channel inhibitor with an IC50 value of < 10 µM. ASIC-IN-1 causes a dose- dependent reduction of the pain intensity .
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-
- HY-12191
-
|
|
Histamine Receptor
|
Metabolic Disease
|
|
A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation .
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-
- HY-183649
-
|
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
|
BCN-PEG6-OH is a neutralizing agent and anticoagulant inhibitor containing strained alkyne. BCN-PEG6-OH undergoes strain-promoted alkyne-azide cycloaddition (SPAAC) click reaction with azido-Warfarin to generate an inactive product that can be rapidly cleared via the kidneys. In mice, BCN-PEG6-OH effectively reduces the anticoagulant activity of azido-Warfarin in a dose-dependent manner, normalizes prothrombin time, and exhibits no inherent anticoagulant or procoagulant effects when administered alone. BCN-PEG6-OH can be used for the research of drug-induced coagulopathy .
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-
- HY-P10373
-
|
|
JAK
IFNAR
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
pJAK2(1001-1013) is a cell-penetrating peptide that corresponds to the activation loop of JAK2 tyrosine kinase and functions as a SOCS1/3antagonist. pJAK2 (1001-1013) blocks SOCS1-mediated negative regulation of immune function, and enhances the biological activity of cytokines such as IFNγ and IL6. pJAK2(1001-1013) inhibits the replication of a broad range of viruses and exerts dose-dependent protective efficacy against lethal viral infections. pJAK2(1001-1013) can be used for the study of immune regulation and infection .
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-
- HY-12443
-
|
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Casein Kinase
|
Neurological Disease
|
|
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
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-
- HY-182336
-
|
|
PROTACs
Dipeptidyl Peptidase
GLP Receptor
|
Inflammation/Immunology
Cancer
|
|
DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer .
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-
- HY-182314
-
|
|
JAK
STAT
Apoptosis
|
Cancer
|
|
JAK3-IN-20 is a selective and orally active JAK3 inhibitor with an IC50 of 0.7473 nM. JAK3-IN-20 forms a covalent bond with JAK3 Cys909, outcompetes ATP for catalytic site binding, and blocks JAK-STAT pathway activation. JAK3-IN-20 inhibits migration, proliferation, and tumor growth of Bortezomib (HY-10227)-resistant cancer cells. JAK3-IN-20 induces dose-dependent apoptosis. JAK3-IN-20 can be used for the research of Bortezomib-resistant multiple myeloma .
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-
- HY-W007223
-
|
D-5-HTP; 5-Hydroxy-D-tryptophan
|
5-HT Receptor
|
Neurological Disease
|
|
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range .
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-
- HY-157295
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .
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-
- HY-162103
-
|
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TAM Receptor
Apoptosis
|
Cancer
|
|
Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
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-
- HY-178353
-
|
|
EGFR
TNF Receptor
Interleukin Related
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR/Cytokine-IN-1 is an EGFR (IC50 = 0.03 μM) and Cytokine inhibitor (TNF-α, IC50 = 3.1 μM; IL-6, IC50 = 1.6 μM). EGFR/Cytokine-IN-1 shows potent anticancer activity on A549 and MCF7, respectively. EGFR/Cytokine-IN-1 significantly reduces IL-6 and TNF-α levels in A549 cells, and also shows promising ADMET profiles. EGFR/Cytokine-IN-1 can induce apoptosis in a dose-dependent manner. compound 5h can be used for the study of breast cancer and lung cancer .
|
-
- HY-175205
-
|
|
TGF-beta/Smad
|
Cancer
|
|
TGF-β2-IN-1 is a selective TGF-β2 inhibitor. TGF-β2-IN-1 exhibits potent antiproliferative effects on HCT-116, Caco-2 and HT-29 with IC50 values of 6.84, 10.21, and 9.47 μM, respectively. TGF-β2-IN-1 inhibits TGF-β2 signaling in a dose-dependent manner by suppressing both receptor and cytokine expression.TGF-β2-IN-1 can be used for the study of colorectal cancer .
|
-
- HY-P991855
-
|
|
TGF-β Receptor
|
Metabolic Disease
|
|
RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation .
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-
- HY-135783
-
AT 1001
1 Publications Verification
|
nAChR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
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-
- HY-113817
-
|
|
Phosphatase
|
Inflammation/Immunology
|
|
SHIP1 activator 1 is an SH3 domain-containing inositol 5-phosphatase regulator with SHIP1 activating activity. SHIP1 activator 1 retains its SHIA-1 activating ability by removing unnecessary functional groups. SHIP1 activator 1 is able to activate SHIP1 in vitro, inhibit Akt phosphorylation in MOLT-4 cells, and show dose-dependent activity in a mouse model of inflammation. SHIP1 activator 1 is an important chemical tool for evaluating the potential of SHIP1 activators as inhibitors of hematopoietic diseases involving abnormal PI3K cell signaling .
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-
- HY-142118A
-
|
AP 12009 sodium
|
TGF-beta/Smad
|
Cancer
|
|
Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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-
- HY-W015892R
-
|
γ-Caprolactone (Standard)
|
Reference Standards
Interleukin Related
TNF Receptor
Insecticide
|
Infection
|
|
γ-Hexalactone (Standard) is the analytical standard of γ-Hexalactone (γ-Caprolactone) (HY-W015892). This product is intended for research and analytical applications. γ-Hexalactone is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage in human lymphocytes and HepG2 cells, modulates cytokine secretion in human lymphocytes, and reduces recombinant PON1 activity. γ-Hexalactone serves as a dose-dependent oviposition inhibitor against Bactrocera oleae. γ-Hexalactone can be used for the research of Bactrocera oleae pest management .
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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-142118
-
|
AP 12009
|
TGF-beta/Smad
|
Cancer
|
|
Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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-
- HY-118775
-
|
|
5-HT Receptor
|
Others
|
|
LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.
|
-
- HY-N3389
-
|
|
SARS-CoV
Sirtuin
CDK
Apoptosis
|
Infection
Metabolic Disease
Cancer
|
|
Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-Cyclin E1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC50 of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection .
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-
- HY-181129
-
|
|
DNA/RNA Synthesis
IFNAR
Apoptosis
Necroptosis
|
Cancer
|
|
ADAR1i-124 is an A-to-I RNA editing inhibitor by inhibiting the catalytic activities of both ADAR1p150 and ADAR1p110. ADAR1i-124 activates type I interferon (IFN) and ZBP1 pathways and dose-dependently inhibits viability across different types of cancer cell lines. ADAR1i-124 can induce cells apoptosis and necroptosis. ADAR1i-124 can be used for the research of cancer, such as cutaneous melanoma and ovarian cancer .
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-
- HY-125172
-
|
Polyglutamine Aggregation inhibitor III
|
Huntingtin
|
Others
|
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s=25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2 transgenic mouse model of Huntington's disease.
|
-
- HY-111168
-
|
|
GSK-3
|
Cancer
|
|
MLS-2064 is a 3'-substituted 7-haloindirubin with antitumor activity. MLS-2064 induces caspase-independent cell death. MLS-2064 induces dose-dependent cell death in various human cancer cell lines. MLS-2064 shows no significant inhibitory activity against CDK1 and CDK5 kinases, and only weak inhibitory activity against GSK-3 kinase (IC50: 5 μM). MLS-2064 can be used in research related to colon cancer, breast cancer, lung cancer, prostate cancer, liver cancer, and neuroblastoma .
|
-
- HY-150739
-
-
- HY-123786
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage .
|
-
- HY-W753635
-
-
- HY-156696
-
|
|
Na+/H+ Exchanger (NHE)
|
Metabolic Disease
|
|
S3226 is a highly selective NHE-3 inhibitor (IC50<1 μM) that specifically blocks NHE-3-mediated sodium transport. S3226 significantly inhibits blastocyst formation and expansion in mouse embryos, and reduces fluid and electrolyte reabsorption in rat proximal tubules in a dose-dependent manner. S3226 effectively alleviates ischemia-induced acute renal failure by improving renal function parameters, reducing renal tubular injury and restoring intracellular pH homeostasis, without interfering with the normal tubuloglomerular feedback response. S3226 is widely used in studies of acute renal failure and related pathological mechanisms .
|
-
- HY-N1393R
-
|
NSC 3778 (Standard); O-Methylsalicylic acid (Standard); Salicylic acid methyl ether (Standard)
|
Reference Standards
Carbonic Anhydrase
Phospholipase
|
Cardiovascular Disease
|
|
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) (Standard) is the analytical standard of 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
|
-
- HY-B1777A
-
|
|
Endogenous Metabolite
Bacterial
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro. Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells .
|
-
- HY-B1777
-
|
NSC 268508; Neuridine
|
Endogenous Metabolite
Bacterial
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro .
|
-
- HY-137610A
-
|
|
P2X Receptor
P2Y Receptor
|
Neurological Disease
|
|
TNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors (IC50 = 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors). TNP-ATP reduces acetate-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively). TNP-ATP dose-dependently attenuates acetate-induced abdominal contractions in a mouse visceral pain model (ED50 = 6.35 µmol/kg) [1][2].
|
-
- HY-169059
-
|
|
Ferroptosis
|
Inflammation/Immunology
|
|
Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
|
-
- HY-150105
-
|
BMF-219; Menin-MLL inhibitor 21
|
Epigenetic Reader Domain
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes .
|
-
- HY-N6954R
-
|
|
Reference Standards
ATM/ATR
STAT
CDK
Hedgehog
|
Inflammation/Immunology
Cancer
|
|
Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active .
|
-
- HY-A0191
-
|
(+)-Brompheniramine; (S)-Brompheniramine
|
Endogenous Metabolite
Histamine Receptor
TRP Channel
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) is a dual inhibitor of histamine H1 receptor and TRPV1 receptor that can cross the blood-brain barrier. Dexbrompheniramine exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine can be used in the research of chronic cough and related pathological mechanisms .
|
-
- HY-P5900
-
|
m3-HwTx-IV
|
Sodium Channel
|
Neurological Disease
|
|
m3-Huwentoxin IV (m3-HwTx-IV) is a potent NaV inhibitor with IC50s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNaV1.7, hNaV1.6, hNaV1.3, hNaV1.1, hNaV1.2 and hNaV1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the NaV1.7 activator OD1 in a rodent pain model .
|
-
- HY-W005255
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
3-(3-Hydroxyphenyl)propionic acid (3HPPA) is an endothelium-dependent nitric oxide (NO) release promoter and endothelial nitric oxide synthase (eNOS) activator. 3-(3-Hydroxyphenyl)propionic acid activates eNOS to mediate vascular smooth muscle relaxation and enhances endothelial cell NO synthesis, inducing vasodilation and reducing peripheral vascular resistance. 3-(3-Hydroxyphenyl)propionic acid can dose-dependently reduce systolic and diastolic blood pressure in spontaneously hypertensive rats (SHR) without affecting cardiac contractility or heart rate. 3-(3-Hydroxyphenyl)propionic acid has antihypertensive and vascular protective effects and can be used in the prevention and treatment of cardiovascular diseases .
|
-
- HY-100658
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
|
-
- HY-181152
-
|
|
FGFR
|
Cancer
|
|
FGFR3-IN-11(compound B11) is a Fibroblast growth factor receptor 3 (FGFR3) inhibitor with a Ka value of 4.8 μM. FGFR3-IN-11 induces apoptosis, suppresses colony formation, and causes dose-dependent G0/G1 cell cycle arrest in cancer cells. FGFR3-IN-11 exerts anticancer activity against cancer cells with minimal toxicity toward normal hepatocytes and demonstrates tumor growth suppression in xenograft mouse models. FGFR3-IN-11 can be used for the research of hepatocellular carcinoma .
|
-
- HY-A0191A
-
|
(+)-Brompheniramine maleate; (S)-Brompheniramine maleate
|
TRP Channel
Histamine Receptor
|
Inflammation/Immunology
|
|
Dexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) maleate is a dual inhibitor of histamine H1 receptor and TRPV1 receptor that can cross the blood-brain barrier. Dexbrompheniramine maleate exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine maleate with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine maleate alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine maleate can be used in the research of chronic cough and related pathological mechanisms .
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- HY-176755
-
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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CCL-34 is a Toll-like receptor 4 (TLR4) activator. CCL-34 significantly induced dendritic cell (DC) CD83 expression and IL-12p70 production in a dose-dependent manner, thereby inducing DC maturation. CCL-34 enhanced the allostimulatory activity of DC on naive CD4+CD45+RA+ T cell proliferation and IFN-γ secretion. CCL-34 further induced antigen presentation ability in mice inoculated with doxorubicin-treated colorectal cancer cells. CCL-34 can be used in studies of immune stimulation.
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- HY-135439
-
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5-HT Receptor
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Neurological Disease
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SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .
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- HY-W777283
-
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Isotope-Labeled Compounds
Apoptosis
Mitochondrial Metabolism
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Neurological Disease
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Idebenone- 13C,d3 is the deuterium labeled and 13C-labeled Idebenone (HY-N0303). Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM) . Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells . Idebenone quickly crosses the blood-brain barrier.
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- HY-145720
-
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ALN-CC5
|
Complement System
Small Interfering RNA (siRNA)
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Metabolic Disease
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Cemdisiran (ALN-CC5) is an N-acetylgalactosamine-conjugated RNAi agent and also a complement component C5 inhibitor. Cemdisiran targets C5 mRNA, cleaves C5 mRNA via the endogenous RNA interference pathway, and inhibits the production of C5 protein in the liver. Cemdisiran exerts a dose-dependent inhibitory effect on total C5 concentrations in cynomolgus monkeys. When used in combination with Pozelimab (HY-P99786) in cynomolgus monkeys, Cemdisiran achieves a more sustained and complete inhibitory effect on complement activity. Cemdisiran can be used in the research of paroxysmal nocturnal hemoglobinuria and other complement-mediated diseases .
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- HY-124547R
-
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Endogenous Metabolite
Reference Standards
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Others
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2,4-D methyl ester (Standard) is the analytical standard of 2,4-D methyl ester. This product is intended for research and analytical applications. 2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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- HY-178389
-
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Molecular Glues
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
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Cancer
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GPX4-IN-20, a Arctigenin (HY-N0035) derived, is a GPX4& molecular gluedegrader. GPX4-IN-20 induces ferroptosis by increasing lipid ROS levels and suppressing GSH levels. GPX4-IN-20 reduces the protein expression and enzyme activity of GPX4 in a dose-dependent manner without affecting other ferroptosis-related proteins. GPX4-IN-20 induces ubiquitination-dependent proteasomal degradation of GPX4. GPX4-IN-20 also increases the level of malondialdehyde (MDA) in HCT-116 cells. GPX4-IN-20 can be used for the research of colorectal cancer .
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- HY-N1393S1
-
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NSC 3778-d3; O-Methylsalicylic acid-d3; Salicylic acid methyl ether-d3
|
Isotope-Labeled Compounds
Carbonic Anhydrase
Phospholipase
|
Cardiovascular Disease
|
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2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)-d3 is deuterium-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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- HY-N0340R
-
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Hyoscine butylbromide (Standard); (-)-Scopolamine butylbromide (Standard); Butylscopolamine bromide (Standard)
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Reference Standards
mAChR
|
Neurological Disease
Inflammation/Immunology
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Scopolamine butylbromide (Standard) is the analytical standard of Scopolamine butylbromide (HY-N0340). This product is intended for research and analytical applications. Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
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- HY-158821B
-
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TGF-beta/Smad
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Neurological Disease
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ISTH0036 sodium scrambled negative control is the sequence scrambled negative control of ISTH0036 sodium (HY-158821A). ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
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- HY-145453R
-
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Reference Standards
Interleukin Related
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Inflammation/Immunology
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Propacetamol (Standard) is the analytical standard of Propacetamol (HY-145453). This product is intended for research and analytical applications. Propacetamol is an orally active prodrug of Acetaminophen (HY-66005), which exerts antipyretic and analgesic effects after metabolism. Propacetamol reduces Aspirin (ASA) (HY-14654)-induced elevation of malondialdehyde (MDA) in gastric mucosa and plasma, regulates the levels of gastric mucosal glutathione (GSH and GSSG) to maintain cellular antioxidant defense, and increases gastric mucosal uric acid (UA) levels. Propacetamol exerts a dose-dependent protective effect against ASA-induced gastric mucosal damage in rats. Propacetamol can be used for the study of gastric mucosal injury by interfering with oxidative stress .
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- HY-116739R
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Brassidic acid (Standard); trans-13-Docosenoic acid (Standard)
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Drug Derivative
Reference Standards
Others
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Metabolic Disease
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2,4-D methyl ester (Standard) is the analytical standard of 2,4-D methyl ester. This product is intended for research and analytical applications. 2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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- HY-182504
-
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Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia . .
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- HY-117733
-
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Tie
VEGFR
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Cancer
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Zerumin A is an anti-angiogenic agent that acts on multiple molecular targets related to angiogenesis (including kdr/VEGFR2, angpt1, angpt2, tie1, and tie2). Zerumin A specifically inhibits the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by regulating the VEGF-VEGFR and ANGPT-TIE signaling pathways, and dose-dependently inhibits angiogenesis (10-20 μM significantly inhibits zebrafish embryo angiogenesis). Zerumin A can be used in the research of cancer and angiogenesis-related inflammatory diseases. Zerumin A can be naturally extracted from the 95% ethanol extract of the fruits, seeds, and pericarp of Alpinia caerulea (R.Br.) Bentham (a plant of the Alpinia genus in the Zingiberaceae family) .
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- HY-124547S
-
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Isotope-Labeled Compounds
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Others
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2,4-D methyl ester-d3 is the deuterium labeled 2,4-D methyl ester (HY-124547). 2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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- HY-103484R
-
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IKZF Family
Reference Standards
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Cardiovascular Disease
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GATA4-NKX2-5-IN-1 (Standard) is the analytical standard of GATA4-NKX2-5-IN-1 (HY-103484). This product is intended for research and analytical applications. GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression .
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- HY-175770
-
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Isocitrate Dehydrogenase (IDH)
PDK-1
Apoptosis
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Cancer
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mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma .
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- HY-N1393S
-
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NSC 3778-13C6; O-Methylsalicylic acid-13C6; Salicylic acid methyl ether-13C6
|
Isotope-Labeled Compounds
Carbonic Anhydrase
Phospholipase
|
Cardiovascular Disease
|
|
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)- 13C6 is the 13C-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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- HY-158821D
-
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Fluorescent Dye
TGF-beta/Smad
|
Neurological Disease
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Cy3 labled ISTH0036 sodium is a Cy3 labled ISTH0036 sodium (HY-158821A). ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
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- HY-158821C
-
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Fluorescent Dye
TGF-beta/Smad
|
Neurological Disease
|
|
FAM labled ISTH0036 sodiumis a FAM labled ISTH0036 sodium (HY-158821A). ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
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- HY-169103
-
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NO Synthase
COX
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
Neuroprotective agent 5 (compound 28) is a brain permeabilizing agent with anti-neuritis, anti-oxidative damage and neuroprotective effects. Neuroprotective agent 5 exhibits a potent NO inhibitory effect (EC50=0.49 μM), inhibits the release of proinflammatory factors PGE2 and TNF-α, downregulates the expression of iNOS and COX-2 proteins, and promotes the polarization of BV-2 cells from the proinflammatory M1 phenotype to the anti-inflammatory M2 phenotype. In addition, Neuroprotective agent 5 can also inhibit acetylcholinesterase (AChE) activity and Aβ42 aggregation in a dose-dependent manner. Neuroprotective agent 5 can be used for the study of Alzheimer's disease .
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- HY-107830
-
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Endogenous Metabolite
Collagen
|
Infection
Metabolic Disease
|
|
Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
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- HY-149010
-
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Keap1-Nrf2
|
Neurological Disease
|
|
NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research .
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-
- HY-175664
-
|
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RPE65
|
Metabolic Disease
|
|
EYE-003 is an orally active RPE65 inhibitor with an IC50 of 102 nM. EYE-003 regulates the visual cycle in mice by reducing 11-cis-retinal (11cRAL) (HY-116711) synthesis and increasing all-trans-retinyl esters (atREs). EYE-003 suppresses scotopic ERG b-wave amplitude and exerts protective effects against retinal degeneration in Abca4 ⁻/⁻ Rdh8 ⁻/⁻ mice (a STGD1 model) by reducing retinal autofluorescent puncta and preserving outer nuclear layer (ONL) thickness in a dose-dependent manner. EYE-003 can be used for the study of visual cycle-associated retinopathies, such as Stargardt disease type 1 (STGD1) .
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- HY-159945
-
|
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α-synuclein
|
Neurological Disease
|
|
Tau Protein/α-synuclein-IN-2 (Compound 14T) is a blood-brain barrier penetrating tau and α-syn inhibitor. Through its thiourea linker structure, Tau Protein/α-synuclein-IN-2 dose-dependently reduces α-syn oligomerization. In biosensor cells, Tau Protein/α-synuclein-IN-2 prevents the seeding effect of tau aggregation. In the M17D neuroblastoma model, Tau Protein/α-synuclein-IN-2 exhibits anti-inclusion effects. Additionally, Tau Protein/α-synuclein-IN-2 reduces Aβ plaque formation. Tau Protein/α-synuclein-IN-2 holds promise for Alzheimer's disease and Parkinson's disease research.
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-
- HY-117921
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
DA-E 5090 is an orally effective inhibitor of IL-1 production that can be converted into a pharmacologically active deacetylated form (DA-E5090) in vivo. In this study, the effects of DA-E5090 on IL-1 production in vitro were examined by LPS-stimulated human monocytes. The results showed that DA-E5090 could dose-dependently inhibit the production of IL-1α and IL-1β (1-10 μM) by LPS-stimulated human monocytes, as determined by LAF assay and ELISA. Northern blotting analysis showed that DA-E5090 inhibited the transcription of IL-1α and IL-1β mRNA.
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-
- HY-173280
-
|
CHNQD-01228
|
Arf Family GTPase
BMX Kinase
|
Cancer
|
|
Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins. The IC50 value for the proliferation of T24 cells is 0.22 μM. It can also dose-dependently inhibit the migration and colony formation of T24 cells, induce G1 phase arrest and trigger Apoptosis. Brefeldin A 4-O-nicotinate exerts its anti-cancer activity by targeting the BMX protein to inhibit the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, as well as by inhibiting the Arf1 protein to eliminate bladder cancer stem cells and activate anti-tumor immunity. Brefeldin A 4-O-nicotinate can be used in the research related to bladder cancer .
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-
- HY-100658S
-
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Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
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-
- HY-170921
-
|
|
Deubiquitinase
|
Cancer
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|
USP1-IN-11 (compound 38-P2) is a selective, reversible, and noncompetitive USP1 (Ubiquitin-specific protease 1) inhibitor. USP1-IN-11 activates the DDR (DNA damage repair) pathway, induces cell cycle arrest and cell Apoptosis, and inhibits cell survival. USP1-IN-11 enhances the sensitivity of Olaparib (HY-10162)-resistant cells to Olaparib (HY-10162) and shows a synergetic effect with Andrographolide (HY-N0191) in BRCA-proficient cancer cells. USP1-IN-11 displays significant, dose-dependent antitumor efficacy in the MDA-MB-436 xenograft model .
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-
- HY-175496
-
|
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Ceramidase
|
Inflammation/Immunology
|
|
Acid Ceramidase-IN-3 is a acid ceramidase (aCDase) inhibitor. Acid Ceramidase-IN-3 inhibits the enzymatic activity of aCDase with a pIC 50 of 8.5 in enzymatic assays and 6.8 in A375 melanoma cellular assays. Acid Ceramidase-IN-3 promotes HSC inactivation, as measured by a dose-dependent
reduction in COL1A1 and ACTA2. Acid Ceramidase-IN-3 inhibits aCDase activity in HSCs, promotes HSC inactivation and suppresses YAP/TAZ nuclear localization. Acid Ceramidase-IN-3 increases Dynein/Kinesin (NDE1, NDEL1.
KIF3B, KIF15) while decreases several proteins involved with signaling pathway (SARM1, RGAP1,
PDGF-D,PDGFR-B). Acid Ceramidase-IN-3 can be used for the study of fibrotic diseases .
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- HY-147862
-
|
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EGFR
Apoptosis
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Cancer
|
|
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
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- HY-183074
-
|
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CDK
Interleukin Related
|
Inflammation/Immunology
|
|
RO8323 is an orally active, selective CDK8/CDK19 inhibitor, with an IC50 of 2 nM against CDK8 and 3 nM against CDK19. RO8323 promotes regulatory T cell differentiation, inhibits effector T cell generation, reverses the Teff/Treg ratio, upregulates IL-10 production in myeloid cells, and suppresses the production of TNF-α, IL-6 and IL-12. RO8323 enhances immune reconstitution and prolongs cardiac allograft survival in a dose-dependent manner. RO8323 can be used in the research of chronic graft-versus-host disease, cardiac allograft rejection, acute graft-versus-host disease and experimental autoimmune encephalomyelitis .
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-
- HY-169006
-
|
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Apoptosis
PKC
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Cancer
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|
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
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-
- HY-143494
-
|
|
RSV
Influenza Virus
|
Infection
|
|
RSV/IAV-IN-3 (compound 14'i) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza A virus (IAV) with EC50 values of 2.92 µM and 1.90 µM,respectively. RSV/IAV-IN-3 has antiviral effect against H1N1 and H3N2 with EC50 values of 3.25 µM and 1.50 µM in MDCK cells, respectively. RSV/IAV-IN-3 significantly inhibits the activity of luciferase in a dose-dependent manner, with an EC50 of 3.89 µM. RSV/IAV-IN-3 inhibits IAV infectivity and RdRp activity. RSV/IAV-IN-3 inhibits IAV and RSV replication at the post-entry stage .
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- HY-113953
-
|
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Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development .
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-
- HY-155066
-
|
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PI3K
mTOR
Apoptosis
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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-
- HY-182372
-
|
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Epoxide Hydrolase
|
Neurological Disease
|
|
SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
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-
- HY-B1777AS
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Reactive Oxygen Species (ROS)
Bacterial
DNA/RNA Synthesis
|
Metabolic Disease
|
|
Spermine-d8 (tetrahydrochloride) is the deuterium labeled Spermine tetrahydrochloride. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro. Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells .
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-
- HY-101122
-
|
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SGLT
GLP Receptor
|
Metabolic Disease
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LX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC50 values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research .
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- HY-B1777AR
-
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Reference Standards
Endogenous Metabolite
Bacterial
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Spermine (tetrahydrochloride) (Standard) is the analytical standard of Spermine (tetrahydrochloride). This product is intended for research and analytical applications. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro. Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells .
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- HY-167924
-
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Kallikrein
Thrombin
Ser/Thr Protease
|
Inflammation/Immunology
|
|
Ono 3307 Free base is a novel synthetic protease inhibitor that exhibits protective effects against acute pancreatitis by preventing hyperamylasemia and pancreatic edema. Ono 3307 Free base also inhibits the redistribution of lysosomal enzymes in acinar cells and mitigates lactic dehydrogenase discharge. Ono 3307 Free base effectively reduces cathepsin B leakage from lysosomes in a dose-dependent manner. Ono 3307 Free base is able to target trypsin (Ki=48 nM), thrombin (Ki=0.18 μM), plasma kallikrein (Ki=0.29 μM), plasmin (Ki=0.31 μM), pancreatic kallikrein (Ki=3.6 μM), and chymotrypsin (Ki=47 μM).
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-
- HY-167939
-
|
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Adrenergic Receptor
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Inflammation/Immunology
|
|
(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
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- HY-181663
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PD-1/PD-L1
JAK
|
Cancer
|
|
PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3 +CD8 + and CD3 +CD4 + cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer .
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- HY-170965
-
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CDK
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
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- HY-101741
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|
A-289099
|
Microtubule/Tubulin
Apoptosis
|
Cancer
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|
A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
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- HY-172883A
-
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FABP
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
(E/Z)-ABP/PPAR modulator 1 is a mixture of the E and Z isomers of ABP/PPAR modulator 1 (HY-172883). ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65 μM and 1.08 μM for FABP1 and FABP4, EC50 s of 9.19 μM, 2.20 μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
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- HY-B1067
-
|
Phenazoline hydrochloride
|
Histamine Receptor
HBV
|
Neurological Disease
Endocrinology
|
|
Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV .
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- HY-N17778
-
|
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Others
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Cancer
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(2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol is a flavonoid and a selective inhibitor of human liver cancer cell growth, with an IC50 of 38.6 μg/mL (121.5 μM). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol inhibits cancer cell growth with dose-dependent cytotoxic activity, and its anticancer activity is comparable to that of Cisplatin (HY-17394). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol can be used in research on liver cancer and other types of cancer.
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- HY-168857
-
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GSK-3
Tau Protein
β-catenin
|
Neurological Disease
|
|
GSK-3β inhibitor 24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. GSK-3β inhibitor 24 increases GSK-3β phosphorylation at Ser9 site dose-dependently. GSK-3β inhibitor 24 inhibits the hyperphosphorylation of tau protein by decreasing the p-tau-Ser396 abundance. GSK-3β inhibitor 24 up-regulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2). GSK-3β inhibitor 24 demonstrates remarkable anti-Alzheimer's disease (AD) effects .
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- HY-130229
-
|
(±)5,6-DiHETrE lactone
|
Drug Derivative
|
Cardiovascular Disease
|
|
5,6-DiHET lactone ((±)5,6-DiHETrE lactone) is a lactonized form of 5,6-EET and 5,6-DiHET. In solution, 5(6)-EET degrades into 5(6)-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS.1 5,6-DiHET potently induces vasodilation of isolated canine coronary arterioles, with 41 and 100% inhibition occurring at 0.01 and 100 pM, respectively. It also induces vasodilation in isolated human microvessels and increases intracellular calcium levels in a dose-dependent manner, an effect that can be blocked by the nitric oxide scavenger L-NAME.
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-
- HY-P991944
-
|
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CCR
|
Cancer
|
|
ZL-1218 is a selective humanized IgG1 antibody, targeting CCR8. ZL-1218 induces antibody-dependent cellular cytotoxicity (ADCC), leading to NK cell-mediated depletion of CCR8-expressing regulatory T cells (Tregs). ZL-1218 blocks the binding of the CCR8 ligand CCL1 to CCR8 and reduces Treg recruitment by inhibiting the chemotaxis of CCR8 + cells. ZL-1218 reduces intratumoral Treg levels in a dose-dependent manner. ZL-1218 exerts enhanced antitumor activity when combined with the anti-PD-1 antibody. ZL-1218 can be used for solid tumour research .
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- HY-12193
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Histamine Receptor
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Others
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A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
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- HY-179338
-
|
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MAP4K
HOXA
Interleukin Related
|
Cancer
|
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HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research .
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- HY-P2970
-
|
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Apoptosis
PARP
Caspase
Bcl-2 Family
Bacterial
Interleukin Related
|
Infection
Inflammation/Immunology
Cancer
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Stem bromelain (EC 3.4.22.32) is a cysteine protease and antibacterial agent. Stem bromelain can be isolated from the stem of the pineapple (Ananas comosus). Stem bromelain induces dose-dependent secretion of IL-12p70, and IL-6, induces Apoptosis, causes cleavage of full-length PARP protein, Caspase 3, and Caspase 9, increases Bax, and decreases Bcl-2. Stem bromelain possesses various fibrinolytic, antiedema, antithrombotic, and anti-inflammatory activities. Stem bromelain also exhibits in vivo antitumor and antileukemic activities, as well as antimetastatic effects. Stem bromelain has antimycobacterial activity. Stem bromelain provides protection against lead poisoning .
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- HY-117578
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
KB 5666 is a benzoxazine derivative with lipid peroxidation inhibitory activity. KB 5666 showed protective effects against post-ischemic neuronal death. KB 5666 effectively protected CA1 neurons when injected 5 minutes before or immediately after ischemia. KB 5666 also showed a dose-dependent protective effect when injected within 1 hour after ischemia. KB 5666 effectively prevented the significant decrease in microtubule-associated protein 2 immunoreactivity within the dendritic field of CA1 pyramidal cells. KB 5666 prevented the decrease in [3H]PDBu binding activity in different layers of the CA1 region after ischemia. The application of KB 5666 showed the ability to improve the cellular and functional consequences of ischemia .
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-
- HY-179502
-
|
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NF-κB
Glutathione Peroxidase
TNF Receptor
Interleukin Related
mTOR
SOD
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 107 is an orally active anti-inflammatory agent. Anti-inflammatory agent 107 inhibits and NF-κB with a superior binding affinity of -9.4578 kcal/mol. Anti-inflammatory agent 107 reduces levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, C-reactive protein and Erythrocyte Sedimentation Rate) and enhances the endogenous antioxidant defense system by elevating SOD (Superoxide Dismutase), CAT (Catalase) and GSH (Glutathione) activities. Anti-inflammatory agent 107 not induces liver toxicity and demonstrates hepatoprotective effects. Anti-inflammatory agent 107 dose-dependently ameliorates leukocyte infiltration and tissue edema. Anti-inflammatory agent 107 can be used for anti-inflammatory research .
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-
- HY-174974
-
|
|
FGFR
|
Cancer
|
|
ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in
FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations .
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-
- HY-126638
-
|
NSC 324645
|
Parasite
|
Infection
|
|
Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
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-
- HY-124726
-
|
|
Autophagy
|
Neurological Disease
Cancer
|
|
Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively .
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-
- HY-16074
-
ATN-224
4 Publications Verification
Bischolinetetrathiomolybdate
|
SOD
|
Cancer
|
|
ATN-224 is an orally active Cu 2+/Zn 2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5 nM.
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-
- HY-N5045
-
|
|
Others
|
Inflammation/Immunology
|
|
Jionoside A1 isolated from Radix Rehmanniae Praeparata displays dose dependent immune-enhancement activity and possesses moderate protective activities on H2O2-treated SH-SY5Y cells .
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-
- HY-175204
-
|
|
AUTACs
SHP2
Apoptosis
Autophagy
Atg8/LC3
|
Cancer
|
|
SHP2 protein degrader-3 is a SHP2 AUTAC degrader. SHP2 protein degrader-3 shows dose-dependent SHP2 degradation ability (DC50 = 3.22 μM) and anti-tumor activity (IC50 = 5.59 μM) in HeLa cells. SHP2 protein degrader-3 induces degradation through the LC3-mediated autophagy pathway, which can be inhibited by lysosome inhibitors. SHP2 protein degrader-3 induces apoptosis in various cancer cells (HeLa cells, HepG2 cells, LoVo cells, Huh-7 cells) (SHP2 Ligand : (HY-100388); LC3 Ligand: (HY-10542); Linker : (HY-128834)) .
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-
- HY-170522
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases .
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-
- HY-182503
-
|
|
Adenosine Kinase
|
Others
Inflammation/Immunology
|
|
GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock .
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-
- HY-107830R
-
|
|
Reference Standards
Endogenous Metabolite
Collagen
|
Metabolic Disease
|
|
Methyl cholate (Standard) is the analytical standard of Methyl cholate. This product is intended for research and analytical applications. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
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-
- HY-181722
-
|
|
Sigma Receptor
Histamine Receptor
|
Neurological Disease
|
|
σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain .
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-
- HY-111140
-
|
|
PGE synthase
Lipoxygenase
PPAR
|
Inflammation/Immunology
|
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) . YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research .
|
-
- 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 .
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-
- HY-116062A
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
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-
- HY-100658R
-
|
|
5-HT Receptor
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
|
-
- HY-144668
-
|
|
DNA/RNA Synthesis
Influenza Virus
|
Infection
|
|
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
|
-
- HY-B1777S
-
|
NSC 268508-15N2; Neuridine-15N2
|
Isotope-Labeled Compounds
Endogenous Metabolite
Bacterial
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Spermine- 15N2 (NSC 268508- 15N2) is the 15N-labeled Spermine (HY-B1777). Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro .
|
-
- HY-138232
-
|
LTNAM
|
Aminopeptidase
|
Neurological Disease
|
|
Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
|
-
- HY-B1067A
-
|
Phenazoline
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Antazoline (Phenazoline) is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV .
|
-
- HY-W746556
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Collagen
|
Metabolic Disease
|
|
Methyl cholate-d5 is the deuterium labeled Methyl cholate. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
|
-
- HY-175207
-
|
|
Glycosidase
|
Cancer
|
|
CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
|
-
- HY-19471
-
|
|
Drug Isomer
CDK
VEGFR
Survivin
Apoptosis
|
Cancer
|
|
(rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET .
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-
- HY-181889
-
|
|
Ras
|
Cancer
|
|
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS G12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS G12C alkylation in KRAS G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .
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-
- HY-152524
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
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-
- HY-106200
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM . PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
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-
- HY-129421
-
|
|
PACAP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain .
|
-
- HY-107922
-
|
Isothazine
|
Cholinesterase (ChE)
iGluR
mAChR
|
Neurological Disease
|
|
Ethopropazine (Isothazine) hydrochloride is a potent and selective BChE inhibitor, a poor AChE inhibitor and a non-selective mAChR and NMDA antagonist. Ethopropazine hydrochloride has anticholinergic, antihistamine, antiadrenergic actions and properties. Ethopropazine hydrochloride alleviates thermal hyperalgesia in a dose dependent manner. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease .
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-
- HY-P2026
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
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-
- HY-B1067AR
-
|
Phenazoline (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Antazoline (Phenazoline) (Standard) is the analytical standard of Antazoline. This product is intended for research and analytical applications. Antazoline is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV .
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-
- HY-B1067R
-
|
Phenazoline hydrochloride (Standard)
|
Reference Standards
Histamine Receptor
HBV
|
Neurological Disease
Endocrinology
|
|
Antazoline (hydrochloride) (Standard) is the analytical standard of Antazoline (hydrochloride). This product is intended for research and analytical applications. Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV .
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-
- HY-N4183
-
|
|
Apoptosis
Caspase
Estrogen Receptor/ERR
|
Cardiovascular Disease
Infection
|
|
Licoflavone C is a broad-spectrum antiviral inhibitor with estrogen-like properties. Licoflavone C binds to viral endonuclease (CEN) and inhibits the replication of various bunyaviruses including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus in a non-substrate competitive manner. The IC50 values of Licoflavone C against SFTSV CEN and SFTSV CEN are 35.5 μM and 135.8 μM, respectively, and its Kd value against SFTSV CEN is 9.53 μM. After viral entry into cells, Licoflavone C reduces viral loads in mouse tissues in a dose-dependent manner, and exhibits extremely low cytotoxicity and genotoxicity. Licoflavone C induces apoptosis by increasing caspase 3/7 activity, blocks the cell cycle, and alleviates chemotherapy-induced chromosomal damage. Licoflavone C is applicable to the research on severe fever with thrombocytopenia syndrome and related viral infection mechanisms .
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-
- HY-182760
-
|
|
DNA Alkylator/Crosslinker
Bcl-2 Family
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
|
MN33-63 is a Bcl-2 inhibitor, caspase-3 activator and DNA crosslinker with broad-spectrum anticancer activity. MN33-63 improves the water solubility of SN-38 (HY-13704), inhibits tumor growth and proliferation in a dose-dependent manner, and causes no obvious toxicity. MN33-63 relieves the inhibition of the mitochondrial apoptotic pathway, initiates the apoptosis program, inhibits Topo I activity, and promotes its degradation via the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-63 induces DNA crosslinking, G2/M cell cycle arrest, inhibition of cancer cell migration, and cancer cell apoptosis through the mitochondrial pathway. MN33-63 can be used in the research of colorectal cancer, cervical cancer, hepatocellular carcinoma, lung adenocarcinoma and gastric cancer .
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-
- HY-Y0070
-
|
|
Phytohormone
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
Cyanamide is a cell division and plant growth inhibitor, as well as an allelochemical derived from Vicia villosa. Cyanamide inhibits root growth and biomass accumulation in a dose-dependent manner by disrupting the formation of mitotic spindles and phragmoplast complexes, reducing the number of mitotic cells and blocking the cell cycle. The effects of Cyanamide are partially reversible after removal from low-concentration environments. Cyanamide is also a specific inhibitor of aldehyde dehydrogenase (ALDH). Although Cyanamide has no direct effect on tumor growth, it can significantly enhance the anti-tumor efficacy of Cyclophosphamide (HY-17420) at non-toxic doses by inhibiting the inactivation of Cyclophosphamide. Cyanamide enables Cyclophosphamide to exert equivalent therapeutic effects at lower doses, effectively inhibiting the growth of primary and metastatic tumors and prolonging the lifespan of tumor-bearing mice. Cyanamide is commonly used in studies related to ha-1 hepatoma and rls lymphosarcoma .
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-
- HY-160267
-
|
|
HIV
DNA/RNA Synthesis
|
Infection
Neurological Disease
Cancer
|
|
iPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4 +T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders) .
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-
- HY-168996
-
|
|
CDK
Apoptosis
|
Cancer
|
|
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
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-
- HY-B1067BR
-
|
Phenazoline phosphate (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline phosphate can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline phosphate can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline phosphate can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline phosphate also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline phosphate has anti-arrhythmic effect in acute myocardial infarctions. Antazoline phosphate can be studied in research for cardiovascular diseases, and HBV .
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-
- HY-108557
-
-
- HY-N16632
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
1-O-Caffeoylglycerol is a compound with anti-inflammatory activity found in Sorghum bicolor. 1-O-Caffeoylglycerol significantly inhibits LPS (HY-D1056) induced NO production (IC50 = 18.5 μM) and dose dependently inhibits iNOS protein expression. 1-O-Caffeoylglycerol can be used for research on inflammatory conditions .
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-
- HY-111527
-
|
|
Calcium Channel
|
Neurological Disease
|
|
PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
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-
- HY-159941
-
|
|
α-synuclein
|
Neurological Disease
|
|
tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
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-
- HY-W680886
-
|
|
Monoamine Transporter
Serotonin Transporter
Dopamine Transporter
5-HT Receptor
|
Neurological Disease
|
|
6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse .
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-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
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-
- HY-111137
-
|
XC-302 free base
|
Akt
|
Cancer
|
|
Puquitinib (XC-302 free base) is a multi-target inhibitor with the activity of inducing autophagy in nasopharyngeal carcinoma cells by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib was able to inhibit the proliferation of CNE-2 cells, showing a dose-dependent antiproliferative effect. Puquitinib induced the formation of autophagosomes and autolysosomes in CNE-2 cells, which were observed by fluorescence microscopy and electron microscopy. Puquitinib promoted the formation of LC3-II and increased the expression of beclin 1, while reducing the level of p62. Puquitinib inhibited the PI3K/AKT/mTOR pathway by reducing the expression of p-AKT and p-mTOR. Puquitinib also induced apoptosis in CNE-2 cells, and when autophagy was inhibited, the apoptosis rate was reduced, which means that autophagy may interact with apoptosis to induce cell death .
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-
- HY-B1067B
-
|
Phenazoline phosphate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
Antazoline phosphate is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline phosphate can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline phosphate can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline phosphate can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline phosphate also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline phosphate has anti-arrhythmic effect in acute myocardial infarctions. Antazoline phosphate can be studied in research for cardiovascular diseases, and HBV .
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-
- HY-175870A
-
|
|
Ras
ERK
|
Cancer
|
|
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
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-
- HY-144132
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner .
|
-
- HY-139342
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependent kinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner .
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-
- HY-106863
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BRL 35135 is a potent and selective β3-adrenergic receptor agonist. BRL 35135 can dose dependently increase energy expenditure, reduce weight, and only reduce fat without reducing muscle protein. BRL 35135 can significantly improve glucose tolerance and insulin sensitivity. BRL 35135 can be used to study metabolic conditions such as obesity and diabetes .
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-
- HY-122720
-
|
KL-1
|
Apoptosis
|
Cancer
|
|
SEC inhibitor KL-1 (KL-1) is a peptide-like lead compound that is an effective selective SEC inhibitor. SEC inhibitor KL-1 promotes apoptosis and has anti-tumor activity. SEC inhibitor KL-1 doses dependently inhibits the AFF4-CCNT1 interaction, with a Ki value of 3.48 μM .
|
-
- HY-145865
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
|
-
- HY-122681
-
|
SR-16435 free base
|
Opioid Receptor
|
Neurological Disease
|
|
SR-16434 is a nociceptin/orphanin FQ (NOP)/μ-opioid receptor partial agonist, with high binding affinity (NOP receptor Ki=7.49; μ-Opioid receptor Ki=2.70). SR-16434 can relieve pain .
|
-
- HY-181193
-
|
|
PROTACs
SARS-CoV
Virus Protease
|
Infection
|
|
PROTAC SARS-CoV-2 Mpro degrader-7 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader with a DC50 of 0.985 μM. PROTAC SARS-CoV-2 Mpro degrader-7 promotes K48-linked polyubiquitination of SARS-CoV-2 Mpro, leading to proteasome-dependent degradation via the ubiquitin-proteasome system.PROTAC SARS-CoV-2 Mpro degrader-7 forms a ternary complex with SARS-CoV-2 Mpro and CRBN E3 ubiquitin ligase to enable viral protease ubiquitination.PROTAC SARS-CoV-2 Mpro degrader-7 exhibits a high selectivity index, and induces dose-dependent degradation of SARS-CoV-2 Mpro in stable cells expressing the viral protease.PROTAC SARS-CoV-2 Mpro degrader-7 can be used for the research of COVID-19 .
|
-
- HY-182671
-
|
|
PI3K
Btk
Apoptosis
|
Cancer
|
|
SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL .
|
-
- HY-W720629
-
|
|
Isotope-Labeled Compounds
Phytohormone
Aldehyde Dehydrogenase (ALDH)
|
Others
|
|
Cyanamide- 15N2 is the 15N-labeled Cyanamide (HY-Y0070). Cyanamide is a cell division and plant growth inhibitor, as well as an allelochemical derived from Vicia villosa. Cyanamide inhibits root growth and biomass accumulation in a dose-dependent manner by disrupting the formation of mitotic spindles and phragmoplast complexes, reducing the number of mitotic cells and blocking the cell cycle. The effects of Cyanamide are partially reversible after removal from low-concentration environments. Cyanamide is also a specific inhibitor of aldehyde dehydrogenase (ALDH). Although Cyanamide has no direct effect on tumor growth, it can significantly enhance the anti-tumor efficacy of Cyclophosphamide (HY-17420) at non-toxic doses by inhibiting the inactivation of Cyclophosphamide. Cyanamide enables Cyclophosphamide to exert equivalent therapeutic effects at lower doses, effectively inhibiting the growth of primary and metastatic tumors and prolonging the lifespan of tumor-bearing mice. Cyanamide is commonly used in studies related to ha-1 hepatoma and rls lymphosarcoma .
|
-
- HY-153685
-
|
|
Topoisomerase
Akt
Apoptosis
|
Cancer
|
|
NISC-6 is a novel dual Topo-IIα/Akt inhibitor. NISC-6 has inhibitory activity against various cells, such as UACC903 (IC50 = 2.5 µM) and CHL-1 (IC50 = 0.8 µM) cells. NISC-6 dose dependently induces early and late apoptosis. NISC-6 can be used for research on melanoma .
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-
- HY-107922R
-
|
Isothazine (Standard)
|
Reference Standards
Cholinesterase (ChE)
iGluR
mAChR
|
Neurological Disease
|
|
Ethopropazine (hydrochloride) (Standard) is the analytical standard of Ethopropazine (hydrochloride) (HY-107922). This product is intended for research and analytical applications. Ethopropazine (Isothazine) hydrochloride is a potent and selective BChE inhibitor, a poor AChE inhibitor and a non-selective mAChR and NMDA antagonist. Ethopropazine hydrochloride has anticholinergic, antihistamine, antiadrenergic actions and properties. Ethopropazine hydrochloride alleviates thermal hyperalgesia in a dose dependent manner. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease .
|
-
- HY-182517
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus .
|
-
- HY-N9541
-
|
|
Others
|
Inflammation/Immunology
|
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-179484
-
|
|
Reactive Oxygen Species (ROS)
ERK
|
Cancer
|
|
KRASG12C IN-19 is a selective and orally active KRAS G12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRAS G12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRAS G12V and KRAS G12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRAS G12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRAS G12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer .
|
-
- HY-14840A
-
-
- HY-106200R
-
|
|
Reference Standards
Lipoxygenase
|
Inflammation/Immunology
|
|
CJ-13,610 (Standard) is the analytical standard of CJ-13,610 (HY-106200). This product is intended for research and analytical applications. CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM . PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
|
-
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
-
- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
|
-
- HY-182759
-
|
|
DNA Alkylator/Crosslinker
Topoisomerase
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-183684
-
|
|
RET
VEGFR
PDGFR
Akt
ERK
|
Endocrinology
Cancer
|
|
RET-IN-33 (Compound CN-3) is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer .
|
-
- HY-115903A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .
|
-
- HY-115903
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .
|
-
- HY-110381
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
JNJ-DGAT2-A is a selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. JNJ-DGAT2-A can be used for the research of triglyceride (TG) synthesis .
|
-
- HY-170576
-
|
|
FLT3
STAT
Apoptosis
|
Cancer
|
|
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .
|
-
- HY-178951
-
|
|
STING
IKK
Reactive Oxygen Species (ROS)
IFNAR
PARP
Caspase
|
Inflammation/Immunology
|
|
STING-IN-17 (compound 10a) is an orally active STING (human STING IC50 = 29 nM, mouse STING IC50 = 15 nM) inhibitor. STING-IN-17 can inhibit the phosphorylation of STING, TBK1 and IRF3. STING-IN-17 dose dependently inhibits the mRNA expression of IP10, IFNB1 and ISG56. STING-IN-17 can reduce ROS and inhibit the expression of cleaved-PARP/caspase-3. STING-IN-17 can improve kidney function. STING-IN-17 can be used for research on inflammatory conditions such as acute kidney injury .
|
-
- HY-126359
-
|
SLPC; 18:0-18:2 PC
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine (SLPC; 18:0-18:2 PC) is an endogenous phospholipid marker molecule in the glycerophospholipid metabolic pathway. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine is a core component of the phospholipid bilayer of biological membranes and a key responsive lipid for radiation injury and cardiometabolic diseases. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine constitutes the phospholipid bilayers of cell membranes and high-density lipoprotein (HDL), and regulates the core activity of lipoprotein functional homeostasis. The content of 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine in mouse serum shows a significant dose-dependent decrease with increasing ionizing radiation dose, and its level in human HDL also decreases significantly in metabolic syndrome. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can serve as a biological dosimeter marker for ionizing radiation injury, and is used for rapid and accurate assessment of radiation absorbed dose in exposed individuals. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can also act as a lipidomics research target for cardiometabolic diseases such as lipid metabolic syndrome and early-onset coronary heart disease .
|
-
- HY-179003
-
|
|
mTOR
Glutaminase
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Glutathione Peroxidase
|
Cancer
|
|
mTOR/GLS1-IN-1 (Compoud 9d) is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe 2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer .
|
-
- HY-N16853
-
-
| Cat. No. |
Product Name |
Type |
-
- HY-401424
-
|
Polyoxyethylene(36) Castor Oil; PEG-36 Castor Oil
|
Biochemical Assay Reagents
|
|
Cremophor EL-36 is a non-ionic surfactant, mainly used as a solubilizing carrier for poorly soluble Paclitaxel (HY-B0015). For example, Cremophor EL-36 can enhance the intracellular influx of Etoposide (HY-13629) without affecting drug efflux, and can dose-dependently increase the accumulation of VP-16 in lung adenocarcinoma cells (such as PC-14 and A549), significantly enhancing its cytotoxic effect .
|
-
- HY-137131
-
|
DC-Cholesterol hydrochloride
|
Biochemical Assay Reagents
|
|
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
|
-
- HY-W133891
-
|
Peptones, soybean
|
Biochemical Assay Reagents
|
|
Peptone from soy (peptones, soybean) is a peptone. Peptone from soy provides nitrogen and carbon sources, as well as other nutrients. Peptone from soy can stimulate/regulate the biosynthesis of cyclic eicosanoids. Peptone from soy induces dose-dependent contraction of guinea pig lung parenchyma. Peptone from soy can be used in microbial and cell culture .
|
-
- HY-W025736
-
|
|
Biochemical Assay Reagents
|
|
5-Amino-2-methoxyphenol is a phenolic regioisomer. 5-Amino-2-methoxyphenol produces dose-dependent antinociception in the mouse formalin test, with its second-phase effect being mechanistically dependent on both FAAH and TRPV1. 5-Amino-2-methoxyphenol can be used for antinociception research .
|
-
- HY-W127334
-
|
|
Biochemical Assay Reagents
|
|
N-Palmitoyl phosphatidylethanolamine (Tripelargonin) is endogenous lipid anorectic hormone, significantly reduces food intake in a dose-dependent manner
|
-
- HY-Y0070
-
|
|
Biochemical Assay Reagents
|
|
Cyanamide is a cell division and plant growth inhibitor, as well as an allelochemical derived from Vicia villosa. Cyanamide inhibits root growth and biomass accumulation in a dose-dependent manner by disrupting the formation of mitotic spindles and phragmoplast complexes, reducing the number of mitotic cells and blocking the cell cycle. The effects of Cyanamide are partially reversible after removal from low-concentration environments. Cyanamide is also a specific inhibitor of aldehyde dehydrogenase (ALDH). Although Cyanamide has no direct effect on tumor growth, it can significantly enhance the anti-tumor efficacy of Cyclophosphamide (HY-17420) at non-toxic doses by inhibiting the inactivation of Cyclophosphamide. Cyanamide enables Cyclophosphamide to exert equivalent therapeutic effects at lower doses, effectively inhibiting the growth of primary and metastatic tumors and prolonging the lifespan of tumor-bearing mice. Cyanamide is commonly used in studies related to ha-1 hepatoma and rls lymphosarcoma .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3462A
-
|
|
CGRP Receptor
|
Metabolic Disease
|
|
Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies .
|
-
- HY-P1235A
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-P10373
-
|
|
JAK
IFNAR
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
pJAK2(1001-1013) is a cell-penetrating peptide that corresponds to the activation loop of JAK2 tyrosine kinase and functions as a SOCS1/3antagonist. pJAK2 (1001-1013) blocks SOCS1-mediated negative regulation of immune function, and enhances the biological activity of cytokines such as IFNγ and IL6. pJAK2(1001-1013) inhibits the replication of a broad range of viruses and exerts dose-dependent protective efficacy against lethal viral infections. pJAK2(1001-1013) can be used for the study of immune regulation and infection .
|
-
- HY-P2080B
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human acetate is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human acetate dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P3030
-
-
- HY-P10032
-
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-P2026
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-P4641
-
|
Trp-Phe
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-P3730
-
|
|
CDK
|
Cancer
|
|
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
|
-
- HY-P4663
-
|
NSC 350591
|
Peptides
|
Cancer
|
|
Val-Gly-Ser-Glu (NSC 350591) is an ECF-A tetrapeptide. Val-Gly-Ser-Glu dose-dependently increases the number of human eosinophils, but not neutrophils, rosetting with complement-coated sheep erythrocytes (EAC3b) .
|
-
- HY-P1235
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-P4984
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a T cell proliferation activator. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) promotes the in vitro proliferation of human peripheral blood mononuclear cells (PBMC) in a dose-dependent manner. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) can be used in research on inflammatory and immunity, as well as cancer .
|
-
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-P3100
-
|
|
Parasite
|
Infection
|
|
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC50 value of 34.5 μg/mL .
|
-
- HY-179475
-
|
|
CaSR
|
Endocrinology
|
|
KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
|
-
- HY-W007223
-
|
D-5-HTP; 5-Hydroxy-D-tryptophan
|
5-HT Receptor
|
Neurological Disease
|
|
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range .
|
-
- HY-107627
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
|
-
- HY-P11126
-
|
|
Bacterial
|
Infection
|
|
Mel4 is an antimicrobial peptide, exhibiting broad-spectrum antimicrobial activity. Mel4 can neutralize bacterial lipopolysaccharide in a dose-dependent manner. Mel4 can be used in the research and prevention of related bacterial infectious diseases (such as ocular infections) .
|
-
- HY-P2005
-
|
|
Reactive Oxygen Species (ROS)
SOD
|
Others
|
|
Malformin C is an algicidal peptide can be isolated from Aspergillus and exhibits dose-dependent algicidal activity. Malformin C induces a significant increase in ROS levels in algal cells, resulting in impaired SOD activity and high production of MDA content .
|
-
- HY-P2082
-
|
|
GnRH Receptor
|
Others
|
|
[D-pGlu1,D-Phe2,D-NaI3,6]-Gn-RH is a gonadotropin-releasing hormone (Gn-RH) agonist that has a dose-dependent inhibitory activity on progesterone secretion from cultured human granulosa cells.
|
-
- HY-P1257
-
|
|
Insulin Receptor
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-P10517
-
|
SFT
|
HIV
|
Infection
|
|
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs .
|
-
- HY-P2080
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P5900
-
|
m3-HwTx-IV
|
Sodium Channel
|
Neurological Disease
|
|
m3-Huwentoxin IV (m3-HwTx-IV) is a potent NaV inhibitor with IC50s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNaV1.7, hNaV1.6, hNaV1.3, hNaV1.1, hNaV1.2 and hNaV1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the NaV1.7 activator OD1 in a rodent pain model .
|
-
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
-
- HY-P5921
-
|
TsTx-Kα
|
Potassium Channel
|
Neurological Disease
|
|
Tityustoxin-Kα (TsTx-Kα) is an inhibitor of potassium voltage-gated channels. Tityustoxin-Kα shows a dose-dependent block of the sustained outward current in cultured hippocampal neurons .
|
-
- HY-P1086
-
|
|
Transmembrane Glycoprotein
|
Others
|
|
Cadherin Peptide, avian is a calcium-dependent glycoprotein. Cadherin Peptide, avian takes part in homophilic cell-cell adhesion and dose-dependently inhibits bovine brain microvessel endothelial cells (BBMECs) adhesion .
|
-
- HY-P5859
-
|
α-PMTX
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
α-Pompilidotoxin (α-PMTX) is a neurotoxin that can be obtained from the venom of Anoplius safnariensis. α-Pompilidotoxin reversibly and dose-dependently enhances excitatory postsynaptic currents (EPSCs). α-Pompilidotoxin is a useful tool in the field of neuroscience research .
|
-
- HY-P10032A
-
-
- HY-P0262A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
|
|
Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
|
-
- HY-P10517A
-
|
SFT acetate
|
HIV
|
Infection
|
|
Sifuvirtide (SFT) acetate is a potent HIV fusion inhibitor. Sifuvirtide acetate inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide acetate can be used in the research of anti-HIV drugs .
|
-
- HY-P1440A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.
|
-
- HY-P1257A
-
|
|
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-P2080C
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30)-Myr is the Myr-modified GIP (1-30), which is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P10228
-
|
|
Fungal
Bacterial
|
Infection
|
|
S-Thanatin is an insect antimicrobial peptide with potent broad-spectrum antibacterial activity. S-Thanatin can inhibit the activity of Gram-negative bacteria, Gram-positive bacteria, and fungi, without cytotoxicity. The antibacterial activity of S-Thanatin is not affected by PH value, but monovalent cations (Na +/K +) can reduce its antibacterial activity against Gram-negative bacteria in a dose-dependent manner .
|
-
- HY-P10711
-
|
|
Autophagy
|
Cancer
|
|
ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation .
|
-
- HY-P0249
-
-
- HY-P0249B
-
-
- HY-P3730A
-
|
|
CDK
|
Cancer
|
|
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) acetate, a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991222
-
|
|
Phosphatase
|
Cardiovascular Disease
|
|
AMG-529 is a humanized monoclonal antibody against ASGR1 that binds to ASGR1, blocks ligand binding, and causes a dose-dependent increase in ALP (a biomarker of ASGR1 inhibition). AMG-529 can be used for the research of cardiovascular diseases .
|
-
(5)
-
- HY-P991561
-
|
|
CD47
|
Cancer
|
|
AO-176 is a humanized anti-CD47 IgG2 monoclonal antibody. AO-176 induces tumor phagocytosis through blocking the CD47-SIRPα interaction. AO-176 preferentially binds to tumor versus normal cells and directly kills tumor by a cell autonomous mechanism not ADCC (antibody-dependent cell-mediated cytotoxicity). AO-176 demonstrates dose-dependent antitumor activity in tumor xenograft models. AO-176 can be used for the researches of cancer, such as lymphoma .
|
-
(5)
-
- HY-P992007
-
|
RN909
|
GCGR
|
Metabolic Disease
|
|
PF-06293620 (RN909) is a monoclonal antibody antagonist of the glucagon receptor. PF-06293620 produces dose-dependent, durable lowering of fasting plasma glucose and reduces HbA1c levels. PF-06293620 can be used for the research of type 2 diabetes mellitus .
|
-
(5)
-
- HY-P992052
-
|
|
|
Inflammation/Immunology
|
|
Anti-CD11a Antibody (AL-57) is a monoclonal antibody targeting human CD11a. Anti-CD11a Antibody (AL-57) binds to HA cells in a dose-dependent manner but did not bind to LA cells. Anti-CD11a Antibody (AL-57) preferentially binds to the active conformation of LFA-1 and blocks LFA-1-mediated adhesion and lymphocyte proliferation. Anti-CD11a Antibody (AL-57) can be used for the research of inflammatory and autoimmune diseases .
|
-
(5)
-
- HY-P991855
-
|
|
TGF-β Receptor
|
Metabolic Disease
|
|
RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation .
|
-
(5)
-
- HY-P991944
-
|
|
CCR
|
Cancer
|
|
ZL-1218 is a selective humanized IgG1 antibody, targeting CCR8. ZL-1218 induces antibody-dependent cellular cytotoxicity (ADCC), leading to NK cell-mediated depletion of CCR8-expressing regulatory T cells (Tregs). ZL-1218 blocks the binding of the CCR8 ligand CCL1 to CCR8 and reduces Treg recruitment by inhibiting the chemotaxis of CCR8 + cells. ZL-1218 reduces intratumoral Treg levels in a dose-dependent manner. ZL-1218 exerts enhanced antitumor activity when combined with the anti-PD-1 antibody. ZL-1218 can be used for solid tumour research .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B1777
-
-
-
- HY-B0094
-
-
-
- HY-N0262
-
-
-
- HY-N0407
-
-
-
- HY-N3017
-
-
-
- HY-N0340
-
|
Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
Alkaloids
Structural Classification
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
mAChR
|
|
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
-
- HY-P2970
-
|
|
Ananas comosus(L.) Merr.
Structural Classification
Natural Products
Classification of Application Fields
Bromeliaceae
Plants
Inflammation/Immunology
Disease Research Fields
Cancer
|
Apoptosis
PARP
Caspase
Bcl-2 Family
Bacterial
Interleukin Related
|
|
Stem bromelain (EC 3.4.22.32) is a cysteine protease and antibacterial agent. Stem bromelain can be isolated from the stem of the pineapple (Ananas comosus). Stem bromelain induces dose-dependent secretion of IL-12p70, and IL-6, induces Apoptosis, causes cleavage of full-length PARP protein, Caspase 3, and Caspase 9, increases Bax, and decreases Bcl-2. Stem bromelain possesses various fibrinolytic, antiedema, antithrombotic, and anti-inflammatory activities. Stem bromelain also exhibits in vivo antitumor and antileukemic activities, as well as antimetastatic effects. Stem bromelain has antimycobacterial activity. Stem bromelain provides protection against lead poisoning .
|
-
-
- HY-B1777A
-
-
-
- HY-W042191
-
-
-
- HY-113439
-
12-HETE
2 Publications Verification
|
Microorganisms
Source Classification
|
Apoptosis
|
|
12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway .12-HETE has both anti-thrombotic and pro-thrombotic effects . 12-HETE is a neuromodulator .
|
-
-
- HY-A0191
-
-
-
- HY-W005255
-
-
-
- HY-107830
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Metabolic Disease
Disease Research Fields
Steroids
Source Classification
|
Endogenous Metabolite
Collagen
|
|
Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
|
-
-
- HY-N4183
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Leguminosae
Phenols
Polyphenols
Plants
Glycyrrhiza uralensis Fisch.
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Caspase
Estrogen Receptor/ERR
|
|
Licoflavone C is a broad-spectrum antiviral inhibitor with estrogen-like properties. Licoflavone C binds to viral endonuclease (CEN) and inhibits the replication of various bunyaviruses including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus in a non-substrate competitive manner. The IC50 values of Licoflavone C against SFTSV CEN and SFTSV CEN are 35.5 μM and 135.8 μM, respectively, and its Kd value against SFTSV CEN is 9.53 μM. After viral entry into cells, Licoflavone C reduces viral loads in mouse tissues in a dose-dependent manner, and exhibits extremely low cytotoxicity and genotoxicity. Licoflavone C induces apoptosis by increasing caspase 3/7 activity, blocks the cell cycle, and alleviates chemotherapy-induced chromosomal damage. Licoflavone C is applicable to the research on severe fever with thrombocytopenia syndrome and related viral infection mechanisms .
|
-
-
- HY-B1309
-
-
-
- HY-W015892
-
-
-
- HY-N9182
-
-
-
- HY-N1393
-
-
-
- HY-N6745
-
-
-
- HY-N2252
-
-
-
- HY-B0094R
-
-
-
- HY-N6954
-
-
-
- HY-126359
-
|
SLPC; 18:0-18:2 PC
|
Structural Classification
Classification of Application Fields
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Lipid
Source Classification
|
Endogenous Metabolite
|
|
1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine (SLPC; 18:0-18:2 PC) is an endogenous phospholipid marker molecule in the glycerophospholipid metabolic pathway. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine is a core component of the phospholipid bilayer of biological membranes and a key responsive lipid for radiation injury and cardiometabolic diseases. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine constitutes the phospholipid bilayers of cell membranes and high-density lipoprotein (HDL), and regulates the core activity of lipoprotein functional homeostasis. The content of 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine in mouse serum shows a significant dose-dependent decrease with increasing ionizing radiation dose, and its level in human HDL also decreases significantly in metabolic syndrome. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can serve as a biological dosimeter marker for ionizing radiation injury, and is used for rapid and accurate assessment of radiation absorbed dose in exposed individuals. 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can also act as a lipidomics research target for cardiometabolic diseases such as lipid metabolic syndrome and early-onset coronary heart disease .
|
-
-
- HY-N0775
-
-
-
- HY-N7583
-
-
-
- HY-N0092R
-
-
-
- HY-N3389
-
-
-
- HY-N11911
-
-
-
- HY-N0262R
-
-
-
- HY-N12461
-
-
-
- HY-107164
-
-
-
- HY-W008820R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Disease markers
Endocrine diseases
Nervous System Disorder
Endogenous metabolite
Source Classification
|
Reference Standards
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-W004287
-
|
|
Structural Classification
Natural Products
other families
Plants
Source Classification
|
Amyloid-β
Cholinesterase (ChE)
Parasite
|
|
Methyl tridecanoate is a fatty acid methyl ester. Methyl tridecanoate exhibits an IC50 of 3.26 μM and a Ki of 2.30 μM against AsOBP21f in Anopheles sinensis. Methyl tridecanoate induces electroantennographic responses in female Anopheles sinensis. Methyl tridecanoate shows a dose-dependent attractive effect on Anopheles sinensis. Methyl tridecanoate weakly inhibits β-amyloid aggregation and AChE activity. Methyl tridecanoate can be used in the research of malaria and Alzheimer's disease .
|
-
-
- HY-N5099
-
-
-
- HY-N7934
-
-
-
- HY-N3734
-
|
|
Terpenoids
Labiatae
Samanea saman (Jacq.) Merr.
Diterpenoids
Plants
|
Beta-secretase
Phosphatase
|
|
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
|
-
-
- HY-142088
-
|
|
Natural Products
Microorganisms
Source Classification
|
Endogenous Metabolite
|
|
Beauverolide Ka, a cyclotetradepsipeptide, is a metabolite of Beauveria bassiana fungus. Beauverolide Ka stimulates glucose uptake in cultured rat L6 myoblasts at 50 μM. Beauverolide Ka exhibits protecting effects on HEI-OC1 cells at 10 μM and shows dose-dependent activity in both L6 myoblasts and myotubes .
|
-
-
- HY-N11922
-
-
-
- HY-B0163
-
-
-
- HY-N6681
-
-
-
- HY-P2005
-
-
-
- HY-N5054
-
-
-
- HY-N5060R
-
-
-
- HY-125916
-
-
-
- HY-N0407R
-
|
6'-Cinnamoylcatalpol (Standard)
|
Structural Classification
Iridoids
Terpenoids
Scrophulariaceae
Plants
Picrorhiza scrophulariiflora Pennell
Source Classification
|
Reference Standards
STAT
|
|
Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
-
- HY-121020
-
|
|
Structural Classification
Flavonoids
Flavones
Plants
Compositae
Artemisia capillaris Thunb.
Source Classification
|
SARS-CoV
|
|
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin induces dose-dependent relaxation of ileum and pulmonary artery smooth muscle, causes slight urinary bladder smooth muscle contraction at highest tested concentrations. Arcapillin binds to the active site of SARS-CoV-2 Mpro via interactions with Gln139, His163, and His164, exhibits antiviral activity against SARS-CoV-2 and MERS-CoV. Arcapillin can be used for the research of gastrointestinal disorders, COVID-19, and Middle East respiratory syndrome (MERS) .
|
-
-
- HY-N6609
-
-
-
- HY-N8816
-
-
-
- HY-N1159
-
-
-
- HY-N2383
-
|
(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
Glycosidase
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
|
-
- HY-12956B
-
-
- HY-121377
-
-
- HY-N0775R
-
-
- HY-N4209
-
-
- HY-116498
-
|
|
Microorganisms
Source Classification
|
Others
|
|
Penigequinolone A is an alkaloid isolated from Penicillium. It is lethal to P. penetrans (LD50=100 mg/L) but has no effect on C. elegans at concentrations up to 1000 mg/L.1 Penigequinolone A also accelerates the root growth of rice seedlings in a dose-dependent manner.
|
-
- HY-N14645
-
-
- HY-W042191R
-
-
- HY-125396
-
-
- HY-N13739
-
|
|
Terpenoids
Sesquiterpenes
Asteraceae
Taraxacum coreanum Nakai
Plants
Source Classification
|
Tyrosinase
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
- HY-N11910
-
-
- HY-N15347
-
|
|
Natural Products
Microorganisms
Source Classification
|
NF-κB
p38 MAPK
Interleukin Related
TNF Receptor
NO Synthase
COX
|
|
Talaromyketide B is a polyketide compound with anti-inflammatory activity, discovered in the soil bacterium Talaromyces sp. KYS-41. Talaromyketide B inhibits the activation of the NF-κB and MAPK signaling pathways and dose-dependently suppresses pro-inflammatory cytokines, such as IL-1β, IL-6, IL-10, and TNF-α, as well as the transcriptional activity of inflammatory mediators, including iNOS and COX-2. Talaromyketide B holds potential for research in the fields of immunity and inflammatory diseases .
|
-
- HY-16913
-
-
- HY-N15309
-
|
Torvoside K
|
Structural Classification
Solanum torvum Swartz
Solanaceae
Plants
Steroids
Source Classification
|
Fungal
|
|
Torvoside C (Torvoside K) is a compound found in Solanum torvum with antifungal activity. The ZOIs and MIC values of Torvoside C against the tested fungi (Alternaria brassicicola, Alternaria geophila, Aspergillus flavus, etc.) range from 33.4% to 87.4% and 31.25 to 250 μg/mL, respectively. Additionally, it exhibits a dose-dependent inhibitory effect on the production of mycotoxins aflatoxin B1 and fumonisin B1, which are produced by A. flavus and F. verticillioides, respectively. Torvoside C can be used for research in the field of antifungal infection .
|
-
- HY-112650
-
-
- HY-W015892R
-
|
γ-Caprolactone (Standard)
|
Structural Classification
Natural Products
other families
Plants
Source Classification
|
Reference Standards
Interleukin Related
TNF Receptor
Insecticide
|
|
γ-Hexalactone (Standard) is the analytical standard of γ-Hexalactone (γ-Caprolactone) (HY-W015892). This product is intended for research and analytical applications. γ-Hexalactone is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage in human lymphocytes and HepG2 cells, modulates cytokine secretion in human lymphocytes, and reduces recombinant PON1 activity. γ-Hexalactone serves as a dose-dependent oviposition inhibitor against Bactrocera oleae. γ-Hexalactone can be used for the research of Bactrocera oleae pest management .
|
-
- HY-N1393R
-
|
NSC 3778 (Standard); O-Methylsalicylic acid (Standard); Salicylic acid methyl ether (Standard)
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Reference Standards
Carbonic Anhydrase
Phospholipase
|
|
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) (Standard) is the analytical standard of 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
|
-
- HY-N6954R
-
-
- HY-N0340R
-
|
Hyoscine butylbromide (Standard); (-)-Scopolamine butylbromide (Standard); Butylscopolamine bromide (Standard)
|
Alkaloids
Structural Classification
Other Alkaloids
Datura metel L.
Solanaceae
Plants
Source Classification
|
Reference Standards
mAChR
|
|
Scopolamine butylbromide (Standard) is the analytical standard of Scopolamine butylbromide (HY-N0340). This product is intended for research and analytical applications. Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
|
-
- HY-B1777AR
-
|
|
Structural Classification
Natural Products
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
Bacterial
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
|
Spermine (tetrahydrochloride) (Standard) is the analytical standard of Spermine (tetrahydrochloride). This product is intended for research and analytical applications. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro. Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells .
|
-
- HY-126638
-
|
NSC 324645
|
Human Gut Microbiota Metabolites
Microorganisms
Endogenous metabolite
Source Classification
|
Parasite
|
|
Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
|
-
- HY-N5045
-
-
- HY-107830R
-
|
|
Structural Classification
Microorganisms
Steroids
Source Classification
|
Reference Standards
Endogenous Metabolite
Collagen
|
|
Methyl cholate (Standard) is the analytical standard of Methyl cholate. This product is intended for research and analytical applications. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
|
-
- HY-N11950
-
-
- HY-N17528
-
-
- HY-N17468
-
-
- HY-N5099R
-
-
- HY-W800105
-
-
- HY-N15634
-
-
- HY-N12481
-
-
- HY-N18279
-
-
- HY-N18953
-
|
|
Structural Classification
Natural Products
Endogenous metabolite
Source Classification
|
Interleukin Related
|
|
Heparin disaccharide I-H trisodium (Compound SHS-5) is a heparin-derived disaccharide. Heparin disaccharide I-H trisodium blocks the spontaneous secretion of IL-8 and IL-1β in intestinal epithelial cells at the post-translational stage without reducing mRNA expression levels or intracellular contents. Heparin disaccharide I-H trisodium exhibits dose-dependent anti-inflammatory activity in intestinal epithelial cell models .
|
-
- HY-N6609B
-
|
|
Structural Classification
Alkaloids
Tiliacora racemosa Colebr.
Plants
Isoquinoline Alkaloids
Menispermaceae
Source Classification
|
nAChR
|
|
Magnocurarine chloride is a neuromuscular junction blocker that inhibits muscle contraction by functionally blocking signal transmission without directly damaging nerve or muscle tissues. In frog, mouse and rabbit models, Magnocurarine chloride exerts a dose-dependent paralytic effect, which progresses gradually from limb weakness and loss of righting reflex to respiratory depression and even cardiac arrest. Although high doses cause complete cessation of movement, Magnocurarine chloride does not affect the spinal multineuronal reflex in frogs. Magnocurarine chloride exhibits biological activity similar to that of tubocurarine (HY-125901) in various animal models .
|
-
- HY-117733
-
|
|
Structural Classification
Arecaceae Bercht. & J. Presl
Ketones, Aldehydes, Acids
Terpenoids
Arecaceae
Diterpenoids
Plants
Source Classification
Zingiberaceae
|
Tie
VEGFR
|
|
Zerumin A is an anti-angiogenic agent that acts on multiple molecular targets related to angiogenesis (including kdr/VEGFR2, angpt1, angpt2, tie1, and tie2). Zerumin A specifically inhibits the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by regulating the VEGF-VEGFR and ANGPT-TIE signaling pathways, and dose-dependently inhibits angiogenesis (10-20 μM significantly inhibits zebrafish embryo angiogenesis). Zerumin A can be used in the research of cancer and angiogenesis-related inflammatory diseases. Zerumin A can be naturally extracted from the 95% ethanol extract of the fruits, seeds, and pericarp of Alpinia caerulea (R.Br.) Bentham (a plant of the Alpinia genus in the Zingiberaceae family) .
|
-
- HY-N17778
-
|
|
Structural Classification
Flavonols
Flavonoids
Leguminosae
Genista corsica (Loisel.) DC.
Plants
Source Classification
|
Others
|
|
(2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol is a flavonoid and a selective inhibitor of human liver cancer cell growth, with an IC50 of 38.6 μg/mL (121.5 μM). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol inhibits cancer cell growth with dose-dependent cytotoxic activity, and its anticancer activity is comparable to that of Cisplatin (HY-17394). (2R,3R)-7,3',4'-Trihydroxy-5-methoxy-flavanonol can be used in research on liver cancer and other types of cancer.
|
-
- HY-N16632
-
-
- HY-N9541
-
|
|
Alkaloids
Microorganisms
Pyrrole Alkaloids
Source Classification
|
Others
|
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
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- HY-N16853
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1777AS
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Spermine-d8 (tetrahydrochloride) is the deuterium labeled Spermine tetrahydrochloride. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro. Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells .
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- HY-113439S
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2 Publications Verification
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12-HETE-d8 is the deuterium labeled 12-HETE. 12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway .12-HETE has both anti-thrombotic and pro-thrombotic effects . 12-HETE is a neuromodulator .
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- HY-157029S
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-B0006S1
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Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
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- HY-157031S
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-B0094S
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Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
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- HY-W777283
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Idebenone- 13C,d3 is the deuterium labeled and 13C-labeled Idebenone (HY-N0303). Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM) . Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells . Idebenone quickly crosses the blood-brain barrier.
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- HY-B1777S
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Spermine- 15N2 (NSC 268508- 15N2) is the 15N-labeled Spermine (HY-B1777). Spermine is a natural antioxidant and anti-inflammatory agent. Spermine is known to inhibit some bacterial cultures, especially strains of Staphylococcus aureus. Spermine induces neurotoxicity in the striarum dose-dependently. Spermine can reversibly inhibits DNA synthetic response, mixed lymphocyte response and the induction of cytolytic lymphocyte response in primary cultures of murine spleen cells. Spermine tetrahydrochloride is a polyamine nitric oxide donor that can provide nitric oxide to platelets and inhibit platelet activation to a certain extent concentration-dependently. Spermine tetrahydrochloride occurs in mammalian tissues, plants, bacteria, ribosomes and bacteriophage. Spermine tetrahydrochloride inhibits primary human embryo lung fibroblasts in vitro .
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- HY-B1914S
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Tebufenpyrad-d3 is the deuterium labeled Tebufenpyrad (HY-B1914). Tebufenpyrad can induce mitochondrial dysfunction and oxidative damage. Tebufenpyrad induces dose-dependent cell death on N27 cells, with an EC50 value of 3.98 μM .
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- HY-121356S
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Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
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- HY-121356S1
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Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
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- HY-13570BS1
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Betamethasone acetate-d5 is deuterium labeled Betamethasone acetate (HY-13570B). Betamethasone acetate is a glucocorticoid with prenatal application for preventing respiratory distress syndrome (RDS) in premature infants. Betamethasone acetate exhibits dose-dependent effects on somatic and brain development in offspring when administered prenatally to pregnant rats. Betamethasone acetate can be used for the study of antenatal intervention .
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- HY-B0162S
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Ivabradine-d6 is the deuterium labeled Ivabradine . Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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- HY-B0006S
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Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
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- HY-10119S
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Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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- HY-B0006S2
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Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
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- HY-B0607S
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Nitisinone-d3 (NTBC-d3) is deuterium labeled Nitisinone. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
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- HY-B0094S3
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Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
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- HY-W015912S
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2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
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- HY-W777526
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Nitisinone- 13C6 is a 13C-labeled Nitisinone (HY-B0607). Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
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- HY-124547S
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2,4-D methyl ester-d3 is the deuterium labeled 2,4-D methyl ester (HY-124547). 2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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- HY-N1393S
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2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)- 13C6 is the 13C-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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- HY-W746556
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Methyl cholate-d5 is the deuterium labeled Methyl cholate. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
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- HY-W720629
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Cyanamide- 15N2 is the 15N-labeled Cyanamide (HY-Y0070). Cyanamide is a cell division and plant growth inhibitor, as well as an allelochemical derived from Vicia villosa. Cyanamide inhibits root growth and biomass accumulation in a dose-dependent manner by disrupting the formation of mitotic spindles and phragmoplast complexes, reducing the number of mitotic cells and blocking the cell cycle. The effects of Cyanamide are partially reversible after removal from low-concentration environments. Cyanamide is also a specific inhibitor of aldehyde dehydrogenase (ALDH). Although Cyanamide has no direct effect on tumor growth, it can significantly enhance the anti-tumor efficacy of Cyclophosphamide (HY-17420) at non-toxic doses by inhibiting the inactivation of Cyclophosphamide. Cyanamide enables Cyclophosphamide to exert equivalent therapeutic effects at lower doses, effectively inhibiting the growth of primary and metastatic tumors and prolonging the lifespan of tumor-bearing mice. Cyanamide is commonly used in studies related to ha-1 hepatoma and rls lymphosarcoma .
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- HY-N1393S1
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2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)-d3 is deuterium-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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- HY-100658S
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Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
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| Cat. No. |
Product Name |
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Classification |
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- HY-157029S
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Alkynes
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Alkynes
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-113798
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Alkynes
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ICI 198583 is a thymidylate synthase (TS) inhibitor with a Ki value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia .
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- HY-129737
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Azide
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A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
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| Cat. No. |
Product Name |
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Classification |
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- HY-137131
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DC-Cholesterol hydrochloride
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Cholesterol
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DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
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- HY-142118
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AP 12009
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Antisense Oligonucleotides
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Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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- HY-145720
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ALN-CC5
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siRNAs
siRNA drugs
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Cemdisiran (ALN-CC5) is an N-acetylgalactosamine-conjugated RNAi agent and also a complement component C5 inhibitor. Cemdisiran targets C5 mRNA, cleaves C5 mRNA via the endogenous RNA interference pathway, and inhibits the production of C5 protein in the liver. Cemdisiran exerts a dose-dependent inhibitory effect on total C5 concentrations in cynomolgus monkeys. When used in combination with Pozelimab (HY-P99786) in cynomolgus monkeys, Cemdisiran achieves a more sustained and complete inhibitory effect on complement activity. Cemdisiran can be used in the research of paroxysmal nocturnal hemoglobinuria and other complement-mediated diseases .
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- HY-130345
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Phospholipids
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C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension .
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- HY-149906
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GEM91
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Antisense Oligonucleotides
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Trecovirsen is an antiviral agent targeting HIV gag mRNA, which hybridizes with complementary HIV gag mRNA at the initiation site. Trecovirsen induces a reversible, dose-dependent prolongation of activated partial thromboplastin time via its polyanionic properties. Trecovirsen is applicable to research related to HIV infection .
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- HY-159692
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IONIS-1063734
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Antisense Oligonucleotides
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AZD8701 (IONIS-1063734) is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs), with a human IC50 of 65.2 nM. AZD8701 binds to intronic sites of all FOXP3 pre-mRNA isoforms and mediates dose-dependent FOXP3 knockdown via free uptake. AZD8701 can be used in cancer-related research .
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- HY-142118A
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AP 12009 sodium
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Antisense Oligonucleotides
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Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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- HY-150739A
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CpG ODNs
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ODN 21158 sodium is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 sodium inhibits IFN-α secretion in a dose dependent manner .
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- HY-150739
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CpG ODNs
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ODN 21158 is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 inhibits IFN-α secretion in a dose dependent manner .
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- HY-158821A
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Antisense Oligonucleotides
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ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases .
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- HY-145649A
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AD-85481 sodium; ALN-AGT sodium
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siRNAs
siRNA drugs
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Zilebesiran (AD-85481; ALN-AGT) sodium is a long-acting liver-targeted small interfering RNA (siRNA) antihypertensive agent. Zilebesiran sodium binds to the hepatic asialoglycoprotein receptor (ASGPR), activates the RNA-induced silencing complex to degrade hepatic angiotensinogen mRNA, thereby inhibiting the gene expression and synthesis of angiotensinogen. Zilebesiran sodium dose-dependently reduces serum angiotensinogen levels and 24-hour ambulatory blood pressure, with its effect persisting throughout the circadian cycle. Zilebesiran sodium is applicable to research related to hypertension .
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- HY-158821
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Antisense Oligonucleotides
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ISTH0036 is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases .
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- HY-158821B
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Antisense Oligonucleotides
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ISTH0036 sodium scrambled negative control is the sequence scrambled negative control of ISTH0036 sodium (HY-158821A). ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
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- HY-158821D
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Antisense Oligonucleotides
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Cy3 labled ISTH0036 sodium is a Cy3 labled ISTH0036 sodium (HY-158821A). ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
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- HY-158821C
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Antisense Oligonucleotides
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FAM labled ISTH0036 sodiumis a FAM labled ISTH0036 sodium (HY-158821A). ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
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