Search Result
Results for "
Enzyme inhibitory activity
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N9528
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- HY-N2472
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Castanogenin
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Bacterial
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Infection
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Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
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- HY-130666
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Endogenous Metabolite
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Cardiovascular Disease
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Chlorambucyl-proline is a chloroplatinyl amino acid derivative with inhibitory activity against bovine pulmonary vasoconstrictor enzyme. Chlorambucyl-proline reacts with the convertase in a 1:1 ratio, and the removal of its radiolabel indicates that the compound has an irreversible inhibitory effect on the enzyme activity. Chlorambucyl-proline binds to the aspartic acid or glutamic acid side chain of the enzyme by forming an ester bond, resulting in irreversible inactivation of the enzyme. The inactivation rate constant of chlororambucyl-proline increases in the pH range of 5-8, indicating that its effect on the enzyme activity is affected by the pH environment .
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- HY-101577
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- HY-147730
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HDAC
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Cancer
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A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
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- HY-P1619
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Elastase
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Others
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ICI 186756 is a compound that inhibits the activity of human neutrophil elastase, has a competitive inhibitory effect on the enzyme, can inhibit enzyme-induced lung changes, and can also modulate hamster lung lesions.
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- HY-115312
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Na+/K+ ATPase
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Others
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Ro 18-5364 is an inhibitor of gastric H+/K+ ATPase, which has the effect of inhibiting the activity of the enzyme. Ro 18-5364 has a very strong inhibitory effect on gastric mucosal H+/K+ ATPase, and the inhibitory effect is more significant at low pH. At the same time, there is no selectivity difference between the two enantiomers of H+/K+ ATPase, and its inhibitory effect can be studied and verified by a variety of experimental methods, including inhibition of enzyme activity, proton transport, and studies on its binding.
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- HY-N9314
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- HY-N2266
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COX
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Inflammation/Immunology
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Benzoylgomisin O isolated from Schisandra rubriflora, has inhibitory activity against 15-LOX, COX-1 and COX-2 enzymes and anti-inflammatory activity .
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- HY-122248
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Parasite
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Others
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Phebestin is a compound with antimalarial activity that has an inhibitory effect on Plasmodium and has shown good results in in vitro and in vivo experiments. It can also bind to related enzymes of Plasmodium.
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- HY-125341
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Microginin 527 is a linear cyanobacterial peptide with potent angiotensin-converting enzyme (ACE) inhibitory activity. Microginin 527 also exhibits inhibitory effects on protein phosphatases and leucine aminopeptidase. With an IC50 value of 31 μM, Microginin 527 is the most active component in this class of compounds .
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- HY-124782
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HDAC
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Infection
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HDAC8-IN-8 (15a) is an HDAC8 inhibitor, with IC50 values of 23.9 μM and 268.2 μM for hHDAC8 and smHDAC8 respectively. And for hHDAC1 and hHDAC6, the IC50 values are 12.1 μM and 2.9 μM respectively. HDAC8-IN-8 can be used in schistosomiasis-related research .
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- HY-117012
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Endogenous Metabolite
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Others
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NE58018 is a compound with bone resorption inhibitory activity. NE58018 exerts its effect by affecting the action of Farnesyl pyrophosphate synthase (FPPS). The structural features of NE58018 combined with aminophosphonates significantly enhance its inhibitory activity. NE58018 affects the roles of Thr201 and Tyr204 residues in substrate binding and catalysis. The interaction of NE58018 enhances the inhibitory effect on the target enzyme .
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- HY-P10447
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Fengycin IX; SNA-60-367-3
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Phospholipase
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Inflammation/Immunology
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Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
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- HY-113734
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Aldehyde Dehydrogenase (ALDH)
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Others
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CM026 is a selective aldehyde dehydrogenase 1A1 inhibitor with submicromolar inhibitory activity against aldehyde dehydrogenase 1A1. Its inhibitory mechanism is related to binding to the aldehyde binding pocket and utilizing a unique glycine residue. It can be used as a chemical tool to study the role of this enzyme in disease.
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- HY-N2010
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- HY-N9535A
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Drug Metabolite
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Metabolic Disease
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(R)-tert-OMe-byakangelicin is a kind of furanocoumarin, which has inhibitory activity to liver drug metabolizing enzyme (DME) activity. (R)-tert-OMe-byakangelicin can be isolated from immature fruits of Angelica sinensis .
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- HY-113658
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Endogenous Metabolite
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Others
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ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitory activity and is a multi-target CA inhibitor .
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- HY-107981
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Antifolate
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Cancer
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LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity .
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- HY-126237
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Fungal
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Infection
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Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines .
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- HY-N2472R
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Bacterial
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Infection
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Medicagenic acid (Standard) is the analytical standard of Medicagenic acid. This product is intended for research and analytical applications. Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
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- HY-N1510
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Glycosidase
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Metabolic Disease
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Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM .
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- HY-137954
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SARS-CoV
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Infection
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GRL-0496 is a potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitor, with an IC50 of 30 nM in both enzyme inhibitory and antiviral assays. GRL-0496 shows SARS-CoV antiviral activity, with an EC50 of 6.9 μM .
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- HY-W040286
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Herbicide
Endogenous Metabolite
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Cinosulfuron is a selective herbicide with excellent inhibitory activity against a variety of broadleaf weeds and is widely used in crop fields to protect the growth of crops. Cinosulfuron can effectively manage weed problems by inhibiting specific enzyme activity. Cinosulfuron is used in agriculture to increase crop yield and quality and ensure efficient use of farmland.
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- HY-167952
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PI3K
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Cancer
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mTOR inhibitor-25 is an enzyme inhibitor that is more selective than PI3K and has good anticancer activity. mTOR inhibitor-25 shows strong inhibitory effects on mTOR and may be used to study leukemia, skin cancer, breast cancer, lung cancer and colon cancer. mTOR inhibitor-25 showed excellent activity in cell proliferation experiments, but its inhibitory ability on PI3K was relatively weak .
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- HY-N2010R
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Bacterial
HIV
Reactive Oxygen Species
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Infection
Cardiovascular Disease
Cancer
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Methyl gallate (Standard) is the analytical standard of Methyl gallate. This product is intended for research and analytical applications. Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.
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- HY-146699
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Bacterial
Thymidylate Synthase
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Infection
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MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis .
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- HY-P10601
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- HY-N2298
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Apoptosis
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Cancer
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Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population .
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- HY-N7072
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Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
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Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
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- HY-105747A
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N-(3-Phenoxypropyl)guanidine nitrate; (3-Phenoxypropyl)guanidine nitrate
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Endogenous Metabolite
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Infection
Neurological Disease
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Guanoxyfen (N-(3-Phenoxypropyl)guanidine) nitrate is a compound that exhibits potent inhibitory activity against the serine protease enzyme TMPRSS2, which plays a crucial role in the infectivity of coronaviruses. Guanoxyfen nitrate is also an effective inhibitor of vasoconstrictor responses to sympathetic nerve stimulation.
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- HY-W195984
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Others
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Cancer
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Z57346765 is a PGK1-specific inhibitor that reduces the activity of metabolic enzymes in PGK1 glycolysis and inhibits PGK1-dependent cell proliferation. Z57346765 exerts inhibitory effects against clear cell renal cell carcinoma (KIRC) .
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- HY-118061
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Bacterial
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Infection
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VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
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- HY-W157689
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Proteolytic Enzyme
IDE
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Infection
Metabolic Disease
Cancer
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IDE-IN-3 (Compound 4) is an inhibitor for insulin-degrading enzyme. IDE-IN-3 is predicted to have CYP3A4, CYP2C19, hERG, NADP+, HIF1α and histidine kinase inhibitory activities, and has potential biological activity in anti-diabetic, anti-tumor, anti-bacterial aspects, according to the in silico prediction .
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- HY-161472
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Aldose Reductase
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Cancer
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Aldose reductase-IN-7 (Compound 6k) targets Aldose reductase. Aldose reductase-IN-7 exhibits potent enzyme inhibitory activity (Ki = 0.186 ± 0.020 μM), showing superiority to Epalrestat (HY-66009), which is currently in clinical use. Aldose reductase-IN-7 is less cytotoxic and possesses potent anticancer activity .
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- HY-N1483A
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Potassium Channel
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Cardiovascular Disease
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Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
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- HY-16745A
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KRP-AM1977 hydrochloride
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Bacterial
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Infection
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Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitory activity against both wild-type and mutated target enzymes.
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- HY-118210
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FAAH
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Metabolic Disease
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PHOP is a fatty acid amide hydrolase (FAAH) inhibitor used to assess inhibitory activity in a fluorometric assay. PHOP can determine FAAH activity by measuring the amount of 4-pyridin-1-ylbutyric acid released by the enzyme in rat brain microsomes. PHOP demonstrates potential as a FAAH inhibitor and can directly measure FAAH activity by reversed-phase HPLC and fluorescence detection, providing a basis for the development of new inhibitors.
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- HY-W040286R
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Endogenous Metabolite
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Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Cinosulfuron is a selective herbicide with excellent inhibitory activity against a variety of broadleaf weeds and is widely used in crop fields to protect the growth of crops. Cinosulfuron can effectively manage weed problems by inhibiting specific enzyme activity. Cinosulfuron is used in agriculture to increase crop yield and quality and ensure efficient use of farmland.
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- HY-121382R
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Others
Bacterial
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Cardiovascular Disease
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Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Cinosulfuron is a selective herbicide with excellent inhibitory activity against a variety of broadleaf weeds and is widely used in crop fields to protect the growth of crops. Cinosulfuron can effectively manage weed problems by inhibiting specific enzyme activity. Cinosulfuron is used in agriculture to increase crop yield and quality and ensure efficient use of farmland.
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- HY-N1510R
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Glycosidase
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Metabolic Disease
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Kaempferol 3-O-gentiobioside (Standard) is the analytical standard of Kaempferol 3-O-gentiobioside. This product is intended for research and analytical applications. Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 μM .
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- HY-151802
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TrxR
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Cancer
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CPUL1 is a TrxR inhibitor, which shows proliferation-inhibitory and anti-metastatic activity against A549 cells. CPUL1 influences EMT (epithelial-mesenchymal transition) via inducing ROS-mediated ERK/JNK signaling by inhibiting TrxR1 enzyme activity. CPUL1 in combination with α-Lipoic Acid (HY-N0492) or Dithiodipropionic acid (HY-W014395) is more effective .
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- HY-110167
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PGE synthase
Ligands for Target Protein for PROTAC
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Cancer
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TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon) .
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- HY-13269
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HIV
HIV Integrase
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Infection
Inflammation/Immunology
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BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) .
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- HY-155114
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HIV
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Infection
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HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1 inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC50: 0.094-12.0 μM) .
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- HY-116264
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Ser/Thr Protease
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Cancer
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CatB-IN-1 is an enzyme inhibitor with significant inhibitory activity against tumor invasion. CatB-IN-1 may reduce the invasiveness of tumor cells by regulating intracellular protein metabolism. CatB-IN-1 demonstrates effective anti-invasive ability in cell models and can significantly reduce the invasive ability of MCF-10A neoT cells. The structure-activity relationship study of CatB-IN-1 shows that its design can target multiple functions of cat hepsin B .
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- HY-125798
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Neu5Ac2en; DANA
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Influenza Virus
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Infection
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N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid (Neu5Ac2en) is a potent neuraminidase (sialidase) inhibitor. N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid shows inhibitory activities against human neuraminidase enzymes with IC50s of 143, 43, 61, and 74 μM for NEU1, NEU2, NEU3, and NEU4, respectively. Anti-influenza virus activity .
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- HY-124093
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Thymidylate Synthase
Bacterial
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Infection
Cancer
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8-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitory activity against folate-dependent S. faecium, L. casei, and MTX (HY-14519) resistant strains. 8-Deazahomofolic acid also inhibits the growth of L1210 leukemia cells, with an IC50 value of 87.5 μM. 8-Deazahomofolic acid can be used in research on bacterial infections and tumors .
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- HY-P4641
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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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 .
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- HY-15163A
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FLT3
JAK
CDK
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Cancer
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Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies .
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- HY-14879D
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AVE1330A
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Bacterial
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Infection
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ent-Avibactam sodium (AVE1330A) is a new β-lactamase inhibitor with broad-spectrum antibacterial activity. ent-Avibactam sodium, in combination with ceftazidime, exhibits significant inhibitory effects on Enterobacteriaceae that produce Ambler class A and class C beta-lactamases. The IC50 value of ent-Avibactam sodium is much lower than the commonly used β-lactamase inhibitors clavulanic acid and ticarbonitrile, showing its ability to inhibit TEM-1 and P99 enzyme efficiency .
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- HY-N6972
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Cepharanthine
Maximum Cited Publications
6 Publications Verification
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Infection
Inflammation/Immunology
Cancer
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Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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- HY-121656
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Endogenous Metabolite
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Cancer
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AKR1C2/3-IN-2 is a potential AKR1C3 inhibitor with selective AKR1C3 activity. AKR1C2/3-IN-2 is able to block AKR1C3-mediated testosterone (T) production and PSA induction, affecting the endocrine activity of prostate cancer cells. AKR1C2/3-IN-2 shows selectivity over other AKR1C enzymes, indicating its potential application in inhibiting drug-resistant prostate cancer. AKR1C2/3-IN-2 has no inhibitory activity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
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- HY-146000
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Influenza Virus
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Inflammation/Immunology
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Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM .
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- HY-117085
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Phosphatase
TMV
Lipoxygenase
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Cancer
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Lobaric acid is a depsipeptide metabolite isolated from Stereocaulon lichen with antioxidant, antiproliferative, antiviral and enzyme inhibitory activities. Lobaric acid scavenges superoxide free radicals (IC50=97.9 μM) and inhibits cancer cell proliferation (EC50 of 15.2-63.9 μg/mL against leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic and lung cancer cell lines). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50=0.87 μM for human recombinant enzyme) and 12(S)-HETE produced by 12(S)-lipoxygenase (IC50=28.5 μM). Lobaric acid (250 μM) also reduced pathological changes in tobacco leaves infected with tobacco mosaic virus (TMV).
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- HY-N6972R
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Infection
Inflammation/Immunology
Cancer
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Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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- HY-146755
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Trk Receptor
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Cancer
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TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
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- HY-14863
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CTA-018
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VD/VDR
Cytochrome P450
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Others
Endocrinology
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Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
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- HY-162720
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HIV
Potassium Channel
Reverse Transcriptase
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Infection
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NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
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- HY-161512
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Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research .
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- HY-156470
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Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
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Cancer
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Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
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- HY-146001
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Influenza Virus
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Inflammation/Immunology
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Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice .
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- HY-117247
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DNA/RNA Synthesis
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Infection
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5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor with inhibitory activity against other folate-related enzymes. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed mild growth inhibition against enterococci, lactic acid bacteria, and L1210 cells in culture. 5,6,7,8-Tetrahydro-8-deazahomofolic acid also showed weak inhibition against thymidylate synthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylate synthase .
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- HY-133031A
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Histone Methyltransferase
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Others
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CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
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- HY-159899
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Bacterial
Antibiotic
Dihydrofolate reductase (DHFR)
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DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase) inhibitor belonging to the class of 2,4-diaminopyrimidine compounds. DHFR-IN-22 exhibits significant inhibitory activity against purified DHFR enzyme and major species of nontuberculous mycobacteria (NTM), namely Mycobacterium avium and Mycobacterium abscessus. It shows an IC50 of 1.1 nM and MIC of 1.5 μg/mL against M. abscessus, and an IC50 of 6.3 nM and MIC of 0.1 μg/mL against M. avium. Additionally, it demonstrates an IC50 of 2100 nM against human DHFR. DHFR-IN-22 holds potential for studying novel strategies to combat NTM infections .
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- HY-W010991
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FAPGG
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Angiotensin-converting Enzyme (ACE)
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Others
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N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
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- HY-170846
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FGFR
VEGFR
Bcr-Abl
FLT3
Cytochrome P450
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Inflammation/Immunology
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FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model .
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Cat. No. |
Product Name |
Type |
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- HY-W010991
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FAPGG
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Chromogenic Substrates
Amino acids and Derivatives
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N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-W010991
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FAPGG
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Angiotensin-converting Enzyme (ACE)
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Others
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N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
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- HY-P10447
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Fengycin IX; SNA-60-367-3
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Phospholipase
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Inflammation/Immunology
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Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
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- HY-P10601
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- HY-P4641
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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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 .
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Target |
Chemical Structure |
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