Search Result
Results for "
Enzymes Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1021
Inhibitors & Agonists
17
Biochemical Assay Reagents
66
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B1433
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- HY-163438
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- HY-108647
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p38 MAPK
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Inflammation/Immunology
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EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation .
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-
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- HY-124861
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ME1
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Others
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Metabolic Disease
Cancer
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Malic enzyme inhibitor ME1 (ME1; compound 1) is a potent inhibitor of Malic enzyme (ME1) with an IC50 of 0.15 μM .
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-
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- HY-20070
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TNF Receptor
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Others
Inflammation/Immunology
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BMS-566394 is a potent inhibitor of tumor necrosis factor-α (TNF-α) converting enzyme (TACE) that helps reduce the production of TNF-α, thereby alleviating inflammation and immune-mediated diseases and can be used in the study of inflammatory and autoimmune diseases .
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- HY-B1433S
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- HY-155372
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-39 is a potent inhibitor of α-glucosidase enzyme with an IC50 of 869.06 ppm. α-Glucosidase-IN-39 can used in study antidiabetic .
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-
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- HY-158172
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E1/E2/E3 Enzyme
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Others
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Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ligase Casitas B-lineage lymphoma proto-oncogene B (CPL-B). Cbl-b-IN-18 inhibits the phosphorylation of CPL-B (IC50< 100 nM) .
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-
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- HY-P1044
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LVV-hemorphin-4
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Others
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Neurological Disease
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Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect .
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-
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- HY-150226
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Proteasome
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Inflammation/Immunology
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Enzyme-IN-1 (compound 1) is a peptide-based inhibitor of N-terminal nucleophile (Ntn) hydrolases. Specifically, Enzyme-IN-1 inhibits the chymotrypsin-like activity (CT-L) of the 20S proteasome. Enzyme-IN-1 may has potential antiinflammatory properties .
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-
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- HY-U00459A
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IRE1
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Others
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GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
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-
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- HY-121624
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Glutathione S-transferase
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Infection
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Anthglutin is a gamma-glutamyltransferase inhibitor isolated from Penicillium oxalicum cultures. The Ki values ??of Anthglutin for different enzymes are: porcine kidney enzyme 5.7 μM, human kidney enzyme 18.3 μM, human liver soluble enzyme 13.6 μM, and conjugated enzyme 10.2 μM. Anthglutin had no significant effect on intestinal absorption of methionine in rats .
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- HY-113535
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- HY-119545
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- HY-P1619
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Others
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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-10827
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-
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- HY-U00459
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IRE1
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Cancer
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GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
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-
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- HY-U00459B
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IRE1
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Cancer
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GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
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-
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- HY-101681
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-
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- HY-129430
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Others
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Others
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N-Methylprotoporphyrin IX is a potent inhibitor of ferrochelatase enzyme .
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- HY-122032
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-
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- HY-120148A
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Others
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Others
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SM19712 serves as an inhibitor of the nonpeptide endothelin converting enzyme.
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-
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- HY-114304
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COH000
1 Publications Verification
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E1/E2/E3 Enzyme
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Cancer
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COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro .
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-
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- HY-116750
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Tyrosinase
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Others
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6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC50 value of 124 μM. 6-Hydroxykaempferol has a Ki value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .
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-
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- HY-U00041
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-
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- HY-108321
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- HY-P2366
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-
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- HY-16450
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-
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- HY-107337
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-
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- HY-155288
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Others
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Cancer
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DosatiLink-1 is an Abelson murine leukemia (ABL) enzyme inhibitor .
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- HY-155289
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Others
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Cancer
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DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor .
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- HY-123736
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MMP
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Others
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Ro 32-7315 is a TNF-α converting enzyme (TACE) inhibitor .
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- HY-E70390
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masp-2, c1 esterase, c1-esterase
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Wnt
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Cardiovascular Disease
Inflammation/Immunology
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C1s Enzyme is a subunit of the complement C1 complex, which activates the complement as a serine protease. C1s Enzyme cleaves LRP5 and LRP6, and thus activates the Wnt/β-Catenin signaling pathway. C1s Enzyme promotes the macrophage M2 polarization and inhibits M1 polarization. C1s Enzyme enhances efferocytosis, exhibits anti-inflammatory activity .
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- HY-153045
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Deubiquitinase
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Cancer
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BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .
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- HY-E70203
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-
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- HY-U00074
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- HY-B0279
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-
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- HY-P0143
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-
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- HY-107582
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Others
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Cancer
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JW480 is a potent and selective inhibitor of a serine hydrolase enzyme KIAA1363 .
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- HY-156628
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-
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- HY-155290
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Others
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Cancer
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PonatiLink-1-24 is an Abelson murine leukemia (ABL) enzyme inhibitor .
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- HY-123657
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-
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- HY-134382
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7-Deaza-2'-deoxyadenosine-5'-O-diphosphate
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Others
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Others
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7-CH-dADP is a competitive inhibitor or regulator of enzymes that interact with dADP .
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- HY-112860
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-
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- HY-107994A
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Carboxymethoxylamine; Aminooxyacetate
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GABA Receptor
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Cancer
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Aminooxyacetic acid (Carboxymethoxylamine) is a malate-aspartate shuttle (MAS) inhibitor. Aminooxyacetic acid also inhibits the GABA degradating enzyme GABA-T.
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- HY-125432
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-
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- HY-149694
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Aurora Kinase
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Cancer
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Aurora Kinase Inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth .
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- HY-N2021
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- HY-B0093
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- HY-B0093A
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- HY-B0331A
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- HY-A0043
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- HY-A0043A
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- HY-13989
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- HY-B1202
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AY-22284
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Aldose Reductase
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Endocrinology
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Alrestatin is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.
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- HY-B1202A
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AY-22284A
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Aldose Reductase
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Endocrinology
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Alrestatin sodium is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.
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- HY-100615
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- HY-18690A
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- HY-100312
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- HY-106446
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- HY-132606A
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DCR-PHXC sodium
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Lactate Dehydrogenase
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Others
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Nedosiran sodium is a GalNAc-dsRNA conjugate designed to inhibit production of the hepatic lactate dehydrogenase (LDH) enzyme.
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- HY-161243
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- HY-A0043B
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- HY-18081
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FAAH
Autophagy
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Metabolic Disease
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PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile .
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- HY-138067
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SARS-CoV
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Inflammation/Immunology
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SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
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- HY-107994
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Carboxymethoxylamine hemihydrochloride; Aminooxyacetate hemihydrochloride
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GABA Receptor
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Cancer
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Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
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- HY-A0116S
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- HY-132884
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Others
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Cancer
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TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
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- HY-107762
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Others
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Cardiovascular Disease
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CGS35066 is a potent and selective aminophosphonate inhibitor of endothelin-converting enzyme-1 (ECE-1). CGS 35066 inhibits the activity of human ECE-1 and rat kidney neutral endopeptidase 24.11 (NEP) in vitro with IC50 values of 22 nM and 2.3 μM, respectively .
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- HY-108285
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Others
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Inflammation/Immunology
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(Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents .
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- HY-18948
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GSK321
1 Publications Verification
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Isocitrate Dehydrogenase (IDH)
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Cancer
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GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia .
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- HY-N2021A
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- HY-B0477
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- HY-B0331AS
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- HY-124909A
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Others
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Cancer
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FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect .
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- HY-121517
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Others
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Neurological Disease
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URB754 is a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) with an IC50 of 200 nM .
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- HY-116023
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- HY-159078
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DNA/RNA Synthesis
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Cancer
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PolQi1 is a Polϴ (polymerase theta) inhibitor. PolQi1 targets the polymerase domain of the enzyme .
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- HY-119025
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- HY-155098
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SHP2
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Cancer
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CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .
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- HY-119991
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- HY-122134
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Fungal
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Infection
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SC-58272 is a potent and selective dipeptide N-myristoyltransferase (Nmt) inhibitor with an IC50 of 56 nM for C. albicans (strain B311) Nmt. SC-58272 shows 250-fold selective for the fungal enzyme compared to human enzyme .
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- HY-153973
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 2 (example 118) is a WRN (Werner Syndrome ATP dependent helicase enzyme) inhibitor, with pIC50 ≥ 7.0 .
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- HY-112861
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- HY-101790
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- HY-W010538
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Parasite
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Infection
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trans-4-Methylcyclohexanamine is an intermediate and can be used for the development of T. cruzi enzyme inhibitor .
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- HY-107318
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- HY-124927
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Others
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Cancer
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ARN14988 is a potent inhibitor of acid ceramidase (ACDase) (IC50=12.8 nM for the human enzyme) .
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- HY-144799
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- HY-106816
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- HY-N3247
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Parasite
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Others
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Monomethyl kolavate is a Trypanosoma brucei GAPDH enzyme (TbGAPDH) inhibitor with theIC50 value of 2 µM .
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- HY-145933
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Glutaminase
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Inflammation/Immunology
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BJJF078 is an aminopiperidine derivative. BJJF078 is a potent inhibitor of recombinant human and mouse Transglutaminase enzyme (TG2) activity, IC50 values of 41 and 54 nM, respectively. BJJF078 also inhibits the close related enzyme TG1, with an IC50 of 0.16 μM. BJJF078 can be used for Multiple sclerosis (MS) research .
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- HY-144800
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SARS-CoV
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Infection
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FWM-1 is a potent SARS-COV-2 NSP13 helicase enzyme inhibitor with binding free energy equals -328.6 kcal/mol. FWM-1 effectively disrupts the binding of ATP to the SARS-COV2 helicase enzyme .
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- HY-B0382
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- HY-B1093
-
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Parasite
Cholinesterase (ChE)
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Infection
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Fenchlorphos, an organophosphate, is an insecticide. Fenchlorphos is an inhibitor of the enzyme acetylcholinesterase (AChE). Fenchlorphos is able to cause mitochondrial dysfunction .
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- HY-16437
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- HY-109059
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BAY1142524
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Others
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Cardiovascular Disease
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Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
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- HY-128586
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- HY-125965
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Bacterial
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Infection
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BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme .
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- HY-18207
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- HY-150621
-
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Others
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Cancer
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AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor .
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- HY-147365
-
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Others
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Others
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Acifluorfen-methyl is an inhibitor of the heme and chlorophyll biosynthetic enzyme protoporphyrinogen oxidase (Protox). Acifluorfen-methyl is a photobleaching herbicide .
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- HY-113898
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- HY-120803
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MBR 12325
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Others
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Others
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Mefluidide is a potent inhibitor of KCS6, CER60 and CER1 enzymes and can be used in herbicide research .
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- HY-G0024A
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Vildagliptin carboxy acid metabolite TFA
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Cytochrome P450
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Metabolic Disease
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Vildagliptin carboxylic acid metabolite (M20.7) TFA is a potent P450 enzyme activity inhibitor .
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- HY-P2072
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- HY-162674
-
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SARS-CoV
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Infection
|
MERS-CoV-IN-2 (compound 3c) is a MERS-CoV 3CLpro inhibitor (IC50=17nM). MERS-CoV-IN-2 inhibits the activity of the 3CLpro enzyme by binding to the active site of the enzyme, specifically the S4 subsite, thereby exhibiting antiviral activity against SARS-CoV-2 and MERS-CoV .
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- HY-120631A
-
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Others
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Others
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BMS-538305 hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting strong biological activity by forming a reversible covalent complex with the enzyme. BMS-538305 hydrochloride demonstrates its mechanism of action through the covalent attachment between the nitrile carbon of the inhibitor and the enzyme residue S630, as unveiled by the X-ray crystal structure analysis.
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- HY-18211
-
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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CGS 35601 is the inhibitor for endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), with IC50s of 55, 2, and 22 nM, respectively. CGS 35601 suppresses the big endothelin-1 (big ET-1)- and angiotensin I-induced pressor response, and enhances circulation of atrial natriuretic peptide (ANP), regulates the cardiovascular function in SD rats .
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- HY-163529
-
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HSV
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Infection
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HN0037 is a selective and orally active helicase-primase inhibitor. HN0037 inhibits HSV replication by targeting the viral helicase-primase enzyme complex .
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- HY-13344
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-
- HY-18206
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-
- HY-B0331
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-
- HY-B0231BS
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-
- HY-N0125
-
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Cytochrome P450
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Cancer
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Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
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-
- HY-107373
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L-β-Chloroalanine
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Bacterial
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Infection
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β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
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- HY-B0231AS
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-
- HY-13344A
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-
- HY-108321S
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-
- HY-B0331B
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-
- HY-113681
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-
- HY-131816
-
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Others
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Others
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5'-dUMPS is a competitive inhibitor or regulator of enzymes that interacts with 2′-deoxypyrimidine-5′-monophosphate .
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- HY-129500
-
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Others
|
Cardiovascular Disease
|
Zofenoprilat arginine is an antihypertensive agent that enhances the effect of bradykinin on coronary flow, particularly in the presence of sulfhydryl-containing converting enzyme inhibitors.
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-
- HY-117374
-
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HDAC
|
Cancer
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HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM .
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- HY-126362
-
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Glucosidase
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Others
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ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease .
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- HY-154807
-
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Bacterial
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Infection
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DQn-1 is a potent antifolate with activity against Mycobacterium tuberculosis (Mtb) (MIC90=0.03 µM). DQn-1 directly inhibits DHFR enzyme activity, with IC50s of 8.7 and 7.6 nM for Mtb and human DHFR enzyme, respectively .
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- HY-119689
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CNP520
|
Beta-secretase
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Neurological Disease
|
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively . Umibecestat can be used for the research of alzheimer's disease.
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- HY-10484
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MLN4924 hydrochloride
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NEDD8-activating Enzyme
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Cancer
|
Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM .
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- HY-70062
-
Pevonedistat
Maximum Cited Publications
142 Publications Verification
MLN4924
|
NEDD8-activating Enzyme
|
Cancer
|
Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM .
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- HY-B0744
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DFMO; MDL71782; RMI71782; α-difluoromethylornithine
|
Parasite
|
Infection
Cancer
|
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
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- HY-B0744A
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DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride
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Parasite
|
Infection
Cancer
|
Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
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- HY-U00197
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JTE522; JTP19605; RWJ57504
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COX
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Inflammation/Immunology
|
Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
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-
- HY-B0242S1
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Sulphanilamide-d4
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Bacterial
Antibiotic
|
Infection
|
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
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- HY-101790A
-
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NEDD8-activating Enzyme
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Cancer
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ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity .
|
-
- HY-122591
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PTUPB
1 Publications Verification
|
COX
|
Metabolic Disease
Cancer
|
PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively .
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- HY-33914
-
-
- HY-132824
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-
- HY-B0263S1
-
-
- HY-121232
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-
- HY-113813
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-
- HY-117250
-
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Others
|
Infection
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EcDsbB-IN-10 (compound 12) is an inhibitor of EcDsbB (E. coli DsbB) enzyme, with a Ki of 0.8 nM and an IC50 of 18.85 nM .
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- HY-131812
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2'-Deoxyadenosine 5'-O-thiophosphate
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Others
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Others
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5'-dAMPS is an analogue of 5'-dAMP and thus a potential substrate, competitive inhibitor or regulator of enzymes that interact with dAMP .
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- HY-131810
-
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Others
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Others
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5'-AMPS is an analogue of 5'-AMP and a substrate and competitive inhibitor or regulator of enzymes that interact with 5'-AMP .
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- HY-123227
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- HY-153692
-
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DNA/RNA Synthesis
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Cancer
|
WRN inhibitor 1 (example 7) is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity. WRN inhibitor 1 has the potential to study cancer .
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-
- HY-158235
-
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Tyrosinase
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Others
|
Tyrosinase-IN-27 (compound 6f) is a tyrosinase (TYR) inhibitor (IC50: 0.88 μM) that statically quenches TYR. Tyrosinase-IN-27 increases the hydrophobicity of the enzyme microenvironment by binding to TYR, reducing the content of α-helices in the enzyme and changing its secondary structure. Tyrosinase-IN-27 can be used in the food industry to effectively inhibit the browning of lotus root slices .
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-
- HY-121151
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(±)-Amethopterin; (±)-CL14377; (±)-WR19039
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Others
|
Others
|
(±)-Methotrexate ((±)-Amethopterin) is a racemate of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of Folic acid into Tetrahydrofolate, and inhibiting DNA synthesis .
|
-
- HY-126826
-
-
- HY-147730
-
|
HDAC
|
Cancer
|
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.
|
-
- HY-148190
-
CGT-8012
|
Dipeptidyl Peptidase
|
Endocrinology
|
Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete .
|
-
- HY-156579
-
|
DNA/RNA Synthesis
|
Cancer
|
WRN inhibitor 3 (example 110), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 3 can be used for the research of cancer .
|
-
- HY-156580
-
|
DNA/RNA Synthesis
|
Cancer
|
WRN inhibitor 4 (example 107), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 4 can be used for the research of cancer .
|
-
- HY-156581
-
|
DNA/RNA Synthesis
|
Cancer
|
WRN inhibitor 5 (example 157), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 5 can be used for the research of cancer .
|
-
- HY-18206A
-
-
- HY-N0356
-
(-)-Catechin 3-gallate; (-)-Catechin 3-O-gallate
|
COX
|
Cancer
|
(-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
|
-
- HY-10825
-
DG051
1 Publications Verification
|
Aminopeptidase
|
Metabolic Disease
|
DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
|
-
- HY-U00171
-
SQ28,603; Squibb 28603
|
Neprilysin
|
Metabolic Disease
|
SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
|
-
- HY-B0279S
-
-
- HY-W020215
-
-
- HY-107337S
-
-
- HY-154865
-
|
Lactate Dehydrogenase
|
Cancer
|
Anticancer agent 121, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research .
|
-
- HY-154866
-
|
Lactate Dehydrogenase
|
Cancer
|
Anticancer agent 122, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research .
|
-
- HY-P3201
-
-
- HY-156447
-
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-40 (compound 5) is a noncompetitive α-glucosidase enzyme inhibitor with an IC50 of 24.62 μM .
|
-
- HY-124481
-
|
COX
|
Inflammation/Immunology
|
Oleocanthal is a COX-1/2 enzyme inhibitor and a nonsteroidal anti-inflammatory agent. Oleocanthal is obtained from virgin olive oil .
|
-
- HY-105266
-
-
- HY-162524
-
|
Tyrosinase
|
Others
|
Tyrosinase-IN-28 (Compound 4l) is an inhibitor for tyrosinase with IC50 of 72.55 μM, by affecting both substrate binding and enzyme catalysis .
|
-
- HY-131814
-
|
Others
|
Others
|
5'-dGMPS is an analogue of 5'-dGMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dGMP .
|
-
- HY-131815
-
|
Others
|
Others
|
5'-dIMPS is an analogue of 5'-dIMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dIMP .
|
-
- HY-131813
-
2'-Deoxycytidine 5'-monophosphate
|
Others
|
Others
|
5'-dCMPS is an analogue of 5'-dCMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dCMP .
|
-
- HY-101733
-
-
- HY-23093
-
-
- HY-118164
-
-
- HY-112179
-
|
Others
|
Inflammation/Immunology
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition .
|
-
- HY-76200S
-
UK-109496-d3
|
Fungal
|
Infection
|
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
|
-
- HY-B0744B
-
DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate
|
Parasite
|
Cancer
|
Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women .
|
-
- HY-18030
-
-
- HY-114161
-
-
- HY-125826
-
|
Others
|
Metabolic Disease
|
Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature[1].
|
-
- HY-N4090
-
-
- HY-145705
-
|
DNA/RNA Synthesis
|
Cancer
|
Pencitabine (Pen) is an orally active anticancer agent. Pencitabine interferes with DNA synthesis and function by inhibiting multiple nucleotide-metabolizing enzymes and by misincorporation into DNA .
|
-
- HY-126233
-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
PAT-347 is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood .
|
-
- HY-121180
-
-
- HY-132157
-
|
PARP
|
Others
|
8-Chloroquinazolin-4-ol (Compd 18) is a PARP-1 enzyme inhibitor, with an IC50 of 5.65 μM .
|
-
- HY-W039939
-
2-ADG, 98%
|
Biochemical Assay Reagents
|
Others
|
2-Azido-2-deoxy-D-glucose, 98% is a glycosylation inhibitor, which can be used to study the mechanisms of glycosylating enzymes.
|
-
- HY-167716
-
|
Others
|
Infection
|
Zidovudine diphosphate is an antiretroviral agent that exhibits the activity of inhibiting the reverse transcriptase enzyme used by HIV to synthesize DNA, thereby preventing the formation of viral DNA.
|
-
- HY-B0882S
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-18205
-
-
- HY-147388
-
|
Others
|
Metabolic Disease
|
hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea .
|
-
- HY-118694
-
-
- HY-107352
-
-
- HY-15345
-
THU dihydrate; NSC-112907 dihydrate
|
Others
|
Cancer
|
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
|
-
- HY-109592
-
-
- HY-114161A
-
-
- HY-116872
-
|
Bacterial
|
Infection
|
MAC13772 is a potent inhibitor of the enzyme BioA (IC50=250 nM), the antepenultimate step in biotin biosynthesis. MAC13772 is a novel antibacterial compound .
|
-
- HY-106887
-
|
Others
|
Neurological Disease
|
SCH 32615 is an enkephalinase (the enzymes responsible for the degradation of endogenous enkephalins) inhibitor. SCH 32615 can enhance surgery- and pregnancy-induced analgesia in mice .
|
-
- HY-117281
-
-
- HY-147361
-
|
Apoptosis
Lactate Dehydrogenase
|
Cancer
|
LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression .
|
-
- HY-15345A
-
THU; NSC-112907
|
Others
|
Cancer
|
Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .
|
-
- HY-B0279S1
-
-
- HY-105163
-
MPV-2213ad
|
Cytochrome P450
|
Endocrinology
|
Finrozole (MPV-2213ad) is a nonsteroidal, orally active and competitive aromatase enzyme inhibitor. Finrozole can be used for urinary symptoms research .
|
-
- HY-W332206
-
|
Others
|
Metabolic Disease
|
Cafenstrole acts as a herbicide. Cafenstrole is a potent inhibitor of microsomal elongase enzyme involved in the biosynthesis of fatty acids with alkyl chains longer han C18 .
|
-
- HY-159655
-
-
- HY-N2336
-
-
- HY-129056
-
|
Thrombin
|
Cardiovascular Disease
|
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia . Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion .
|
-
- HY-136885
-
|
MMP
|
Infection
|
(S,S)-TAPI-0 is a matrix metalloproteinase (MMP) inhibitor that inhibits the growth of Chlamydia trachomatis by inhibiting PDF enzyme activity. (S,S)-TAPI-0 can be used to study Chlamydia infection .
|
-
- HY-114536
-
NSC 104800
|
Others
|
Others
|
Mitolactol (NSC 104800) is an angiotensin converting enzyme (ACE) inhibitor with the activity of inhibiting ACE (IC50 of 1.4×10?? M) and inhibiting the pressor response of angiotensin I when administered intravenously at 0.3 mg/kg in rats.
|
-
- HY-B1852
-
|
Bacterial
Fungal
|
Infection
|
Sulfometuron-methyl is a herbicide and also a powerful inhibitor of the enzyme acetolactate synthase (ALS). It exhibits antibacterial and antifungal activities, capable of inhibiting the activity of Salmonella. typhimurium ALS II and Escherichia. coli ALS III .
|
-
- HY-19072
-
|
Others
|
Cardiovascular Disease
|
BRL-36378 is an ACE inhibitor that inhibits angiotensin-converting enzyme activity. BRL-36378 can be used in ligand-based virtual screening to identify new leading structures for chemical optimization .
|
-
- HY-16742B
-
|
Antibiotic
Bacterial
Topoisomerase
|
Infection
|
Gepotidacin mesylate hydrate is an orally active triazaacenaphthylene antibiotic and bacterial type II topoisomerase inhibitor. Gepotidacin mesylate hydrate inhibits bacterial DNA replication by blocking topoisomerase enzymes. Gepotidacin mesylate hydrate selectively inhibits topoisomerase IV and the B subunit of DNA gyrase .
|
-
- HY-13296
-
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
- HY-B1368
-
4-Chloro-DL-phenylalanine; PCPA; CP-10188
|
Tryptophan Hydroxylase
|
Neurological Disease
Cancer
|
Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research .
|
-
- HY-112305
-
|
ATM/ATR
|
Cancer
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-111421
-
-
- HY-100365
-
SHP-141
|
HDAC
|
Cancer
|
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma .
|
-
- HY-N6702
-
-
- HY-132886
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-6 is a SARS-CoV-2 3CLpro inhibitor that shows the most potent enzyme inhibitory IC50 value of 73 nM.
|
-
- HY-145197
-
|
Glutathione Peroxidase
|
Cardiovascular Disease
|
MPO-IN-3 is a potent myeloperoxidase (MPO) inhibitor (WO2013068875A1, example 191). Myeloperoxidase (MPO) is a heme-containing enzyme belonging to the peroxidase superfamily .
|
-
- HY-116559
-
|
Others
|
Others
|
TIBI is a potent and ATP-competitive inhibitor of Rio1 (IC50: 0.09 μM, Ki: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1 .
|
-
- HY-P2605
-
-
- HY-B0279R
-
-
- HY-131811
-
5'-O-Thiophosphonocytidine
|
Others
|
Others
|
5’CMPS (5’-O-Thiophosphonocytidine) is a 5’-CMP analog that is a potential competitive inhibitor or regulator of enzymes that interact with cytidine 5’phosphate .
|
-
- HY-W772850
-
4-Chloro-DL-phenylalanine hydrochloride; PCPA hydrochloride; CP-10188 hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
Cancer
|
Fenclonine hydrochloride is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine hydrochloride can be used in carcinoid syndrome research .
|
-
- HY-18054
-
|
11β-HSD
|
Inflammation/Immunology
|
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease .
|
-
- HY-127146
-
|
Antibiotic
Bacterial
|
Infection
|
Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
|
-
- HY-133217
-
|
Bacterial
|
Infection
|
Benastatin C is a polyketide synthase-derived benastatin that has been found in Streptomyces and has diverse biological activities. It inhibits glutathione S-transferase (GST; IC50=24 μg/mL for the rat liver enzyme).2 Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50=10 μg/mL). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.
|
-
- HY-160633
-
|
Others
|
Infection
|
PfFAS-II inhibitor 1 (Compound 3) is a Plasmodium falciparum type II fatty acid biosynthesis pathway (PfFAS-II) inhibitor, with an IC50 of 0.63 μM for PfFabI enzyme. PfFAS-II inhibitor 1 has antimalarial activity .
|
-
- HY-112435
-
|
PI4K
Parasite
|
Infection
|
UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM .
|
-
- HY-130569
-
|
Drug Metabolite
|
Inflammation/Immunology
Cancer
|
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .
|
-
- HY-A0116A
-
Trandolaprilat hydrate; RU 44403 hydrate
|
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
|
Cardiovascular Disease
|
Trandolaprilate hydrate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate hydrate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity .
|
-
- HY-A0116
-
-
- HY-N1102
-
6-Hydroxypeganine
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
Vasicinol is a reversible inhibitor of sucrase (IC50: 250 μM). Vasicinol is a HbF inducer. Vasicinol also inhibits Angiotensin-converting Enzyme (ACE). Vasicinol is apyrroquinazoline alkaloid that can be isolated from Adhatoda vasica .
|
-
- HY-163529A
-
|
HSV
|
Infection
|
(S)-HN0037 is the (S)-isomer of HN0037 (HY-163529), a selective and orally active helicase-primase inhibitor that inhibits HSV replication by targeting the viral helicase-primase enzyme complex .
|
-
- HY-76316
-
-
- HY-100640
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a agent which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
|
-
- HY-12988
-
C527
1 Publications Verification
|
Deubiquitinase
|
Cancer
|
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
|
-
- HY-112734
-
|
Cytochrome P450
|
Cancer
|
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
|
-
- HY-125999
-
|
Others
|
Neurological Disease
|
EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor. EPI-589 has the potential for the treatment of amyotrophic lateral sclerosis (ALS) .
|
-
- HY-114424
-
-
- HY-114424A
-
-
- HY-118660
-
|
Antibiotic
Bacterial
|
Infection
|
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells .
|
-
- HY-101255
-
ODQ
3 Publications Verification
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells .
|
-
- HY-145326
-
|
Fungal
|
Others
|
Antibacterial agent 67 (IC50 = 0.03 μM) has a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 μM).
|
-
- HY-148700
-
|
DNA/RNA Synthesis
|
Cancer
|
Werner syndrome RecQ helicase-IN-2 (example 57) is a potent Werner syndrome RecQ DNA helicase enzyme (WRN) inhibitor and can be used in cancer research .
|
-
- HY-155521
-
|
Bacterial
|
Infection
|
Enzyme-IN-2 (compound 15) is a ureases inhibitor (Ki=2.36 μM) with anti-ureolytic activity (IC50=0.75 μM) .
|
-
- HY-156414
-
-
- HY-157728
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research .
|
-
- HY-B0279S2
-
-
- HY-B0331AR
-
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
Enalapril (maleate) (Standard) is the analytical standard of Enalapril (maleate). This product is intended for research and analytical applications. Enalapril (MK-421) maleate, the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor.
|
-
- HY-13635A
-
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-P1998
-
|
Others
|
Others
|
Pepsinostreptin is an enzyme inhibitor with the activity of inhibiting pepsin. Pepsinostreptin can form a 1:1 complex with pepsin and significantly inhibit its activity. The activity of pepsinostreptin makes it have important application potential in the study of protease inhibition and related biological processes .
|
-
- HY-109040
-
VT-1129
|
Fungal
Cytochrome P450
|
Infection
|
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes .
|
-
- HY-133624
-
|
Drug Metabolite
|
Cancer
|
1,1,3-Tribromoacetone is an impurity of Methotrexate (HY-14519) . Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .
|
-
- HY-B0378A
-
RS-10085
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
|
Cardiovascular Disease
|
Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects - .
|
-
- HY-N0529
-