Search Result
Results for "
Enzyme inhibitory activity
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N6972
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Cepharanthine
Maximum Cited Publications
13 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-W012530
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Endogenous Metabolite
PDI
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Infection
Metabolic Disease
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Phenylpyruvic acid is a precursor of the antifungal compound phenyllactic acid. Phenylpyruvic acid can improve the antifungal activity of eight lactic acid bacterial strains through the addition into a dedined growth medium. Phenylpyruvic acid demonstrates improved inhibitory activity against fungal bread contaminants Aspergillus niger and Penicillium roqueforti. Phenylpyruvic acid affects enzyme activity of the pentose phosphate pathway involved in the oxidative phase in rat brain homogenates. Phenylpyruvic acid can reduce glucose-6-phosphate dehydrogenase activity .
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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-177295
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LY3549492
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GLP Receptor
Phosphodiesterase (PDE)
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Naperiglipron (LY3549492) is an orally active Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research .
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- HY-N2010
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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-P4279
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Angiotensin-converting Enzyme (ACE)
Cholinesterase (ChE)
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Cardiovascular Disease
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Ovalbumin (154-159) is a protein fragment consisting of residues 154-159 of chicken ovalbumin. Ovalbumin (154-159) is also a poorly conserved sequence (Thr-Asn-Gly-Ile-Ile-Arg) in the α-subunit of the Torpedo acetylcholine receptor, located within the α150-164 epitope region, and exhibits significant angiotensin-converting enzyme (ACE) inhibitory activity .
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- HY-N2157
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(+)-Pteryxin
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Cholinesterase (ChE)
NF-κB
NOD-like Receptor (NLR)
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Nuclear Factor of activated T Cells (NFAT)
p38 MAPK
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca 2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease .
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- HY-N2472
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Castanogenin
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Bacterial
Xanthine Oxidase
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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-137878
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PNP-α-NeuNAc
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Biochemical Assay Reagents
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Others
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2-O-(p-Nitrophenyl)-α-D-N-acetylneuraminic acid (PNP-α-NeuNAc) is a classic chromogenic substrate for neuraminidase. 2-O-(p-Nitrophenyl)-α-D-N-acetylneuraminic acid releases p-nitrophenol upon enzymatic hydrolysis, allowing quantification of enzyme activity and inhibitory effects via spectrophotometry. 2-O-(p-Nitrophenyl)-α-D-N-acetylneuraminic acid (PNP-α-NeuNAc) acts as a sialyl donor in the process of enzyme-catalyzed trans-sialylation .
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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-W041193
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MMP
Lipoxygenase
Tyrosinase
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Infection
Inflammation/Immunology
Cancer
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3-Hydroxy-2-pyrone (Compound 12d) is a metalloenzyme inhibitor. 3-Hydroxy-2-pyrone shows an inhibition rate of approximately 50% for matrix metalloproteinases (MMP) and the inhibition rate for non-heme iron enzyme 5-lipoxygenase (5-LOX) was over 70% at 1 mM. 3-Hydroxy-2-pyrone also has certain inhibitory activity against copper-dependent enzyme tyrosinase. 3-Hydroxy-2-pyrone can be used for the research of cancer, infection and inflammation .
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- HY-N9528
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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-2 (Compound 4) is an inhibitor for insulin-degrading enzyme. IDE-IN-2 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-W012530R
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Reference Standards
Endogenous Metabolite
PDI
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Infection
Metabolic Disease
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Phenylpyruvic acid (Standard) is the analytical standard of Phenylpyruvic acid. This product is intended for research and analytical applications. Phenylpyruvic acid is a precursor of the antifungal compound phenyllactic acid. Phenylpyruvic acid can improve the antifungal activity of eight lactic acid bacterial strains through the addition into a dedined growth medium. Phenylpyruvic acid demonstrates improved inhibitory activity against fungal bread contaminants Aspergillus niger and Penicillium roqueforti. Phenylpyruvic acid affects enzyme activity of the pentose phosphate pathway involved in the oxidative phase in rat brain homogenates. Phenylpyruvic acid can reduce glucose-6-phosphate dehydrogenase activity .
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- HY-W016203
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Sodium phenylpyruvate
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Endogenous Metabolite
PDI
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Infection
Metabolic Disease
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Phenylpyruvic acid sodium is a endogenous metabolite that participates in the synthesis of 3-phenyllactic acid (PLA) by lactate dehydrogenase. Phenylpyruvic acid is a precursor of the antifungal compound phenyllactic acid. Phenylpyruvic acid can improve the antifungal activity of eight lactic acid bacterial strains through the addition into a dedined growth medium. Phenylpyruvic acid demonstrates improved inhibitory activity against fungal bread contaminants Aspergillus niger and Penicillium roqueforti. Phenylpyruvic acid affects enzyme activity of the pentose phosphate pathway involved in the oxidative phase in rat brain homogenates. Phenylpyruvic acid can reduce glucose-6-phosphate dehydrogenase activity .
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- HY-N9314
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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-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-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-Y1668
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Pivalic aldehyde
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Drug Derivative
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Others
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Trimethylacetaldehyde (Pivalic aldehyde) is an analog of Betaine aldehyde. Trimethylacetaldehyde has a significant enzyme inhibitory activity towards betaine aldehyde dehydrogenase. Trimethylacetaldehyde can be used for osmoprotectants of E.coli research .
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- HY-P10601A
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- HY-W275481
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Cytochrome P450
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Others
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γ-Dodecanolactone is a γ-lactone compound. γ-Dodecanolactone exhibits inhibitory activity against CYP1A2 with an IC50 value of 58 µM and a pIC50 value of 4.24. γ-Dodecanolactone can be used in the research of diseases related to the CYP1A2 enzyme .
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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-W064918
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Bacterial
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Infection
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NITD-304 is an orally active anti-tuberculosis agent. NITD-304 exerts inhibitory and bactericidal activities gainst Mycobacterium tuberculosis and multidrug-resistant Mycobacterium tuberculosis. NITD-304 inhibits mycobacterial cell wall biosynthesis and demonstrates synergistic or additive growth inhibitory activity with select antibacterial agents. NITD-304 shows low risk of cardiotoxicity and drug-drug interactions, with no inhibition of major cytochrome P-450 enzymes or hERG channel. NITD-304 can be used for the research of tuberculosis and multidrug-resistant tuberculosis .
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- HY-P11334
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Aminopeptidase
Phosphatase
Angiotensin-converting Enzyme (ACE)
DNA/RNA Synthesis
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Cancer
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Cyanostatin B, a cyanobacterial lipopeptide, is a leucine aminopeptidase M (LAP) inhibitor (IC50 = 12 ng/mL). Cyanostatin B is a weak inhibitor of protein phosphatase (PP2A) and also exhibits weak inhibitory activity against angiotensin-converting enzyme (ACE), with an IC50 value of 130 μg/mL. Cyanostatin B demonstrates both cytotoxic and genotoxic effects on human hepatocytes, although non-toxic to Artemia salina. Cyanostatin B inhibits the proliferation of HepG2 cells, induces DNA single-strand breaks, and causes genomic instability. .
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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-N2472R
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Castanogenin (Standard)
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Xanthine Oxidase
Reference Standards
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-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-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-P10601
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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-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-19885
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Bacterial
Dihydrofolate reductase (DHFR)
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Infection
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AR-102 has inhibitory activity towards Staphylococcus aureus. AR-102 exhibits a competitive potent inhibition of the F98Y mutant DHFR (Ki = 0.22 nM). AR-102 has been determined as ternary complex with NADPH in both wild-type S. aureus DHFR and the TMP-resistant F98Y mutant enzyme .
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- HY-30139
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Biochemical Assay Reagents
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Others
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4-Amino-2-chloropyrimidine is a pyrimidine derivative. 4-Amino-2-chloropyrimidine is a competitive inhibitor for AChE (Ki = 0.18 μM) and BChE (Ki = 1.324 μM). 4-Amino-2-chloropyrimidine fits in the binding pocket of 4BDS. 4-Amino-2-chloropyrimidine has high inhibitory activity on GST enzyme activity (IC50 = 0.037 μM, Ki = 0.047 μM) in vitro .
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- HY-N6972R
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Autophagy
Reference Standards
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-14879E
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NXL-104 sodium
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Beta-lactamase
Bacterial
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Infection
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Ent-Avibactam (NXL-104) sodium is a β-lactamase inhibitor with broad-spectrum antibacterial activity. When combined with Cefazidime (HY-B0593), rel-Avibactam sodium exhibits significant inhibitory effects on Enterobacteriaceae bacteria that produce Ambler A and C types of β-lactamases. The IC50 value of rel-Avibactam sodium is much lower than that of commonly used β-lactamase inhibitors Clavulanic acid (HY-A0256) and Ticarcillin (HY-139805), demonstrating its high efficiency in inhibiting TEM-1 and P99 enzymes .
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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-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-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-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-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-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-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-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-N14562
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Glycosidase
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Metabolic Disease
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Cyclo (D-Pro-L-Val) can inhibit β-glycosidase enzyme activity with IC50 of 75 μg/mL. Cyclo (D-Pro-L-Val) has no or only weak inhibitory effect on other glycosidases .
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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-N2010R
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Gallincin (Standard); NSC 363001 (Standard)
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Reference Standards
Bacterial
HIV
Reactive Oxygen Species (ROS)
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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-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-N0025
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Reactive Oxygen Species (ROS)
Apoptosis
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Metabolic Disease
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Jionoside D is a hydroxycinnamic acid ester with antioxidant property. Jionoside D has scavenging activity of intracellular reactive oxygen species (ROS) and of DPPH radical, and lipid peroxidation inhibitory activity. Jionoside D reduces the apoptotic cells induced by H2O2 in V79-4 cells. Jionoside D increases the activities of cellular antioxidant enzymes, SOD and catalase .
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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-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-N1510R
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Reference Standards
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-155114
-
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HIV
|
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
|
|
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-124093
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Thymidylate Synthase
Bacterial
|
Infection
Cancer
|
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-175262
-
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|
Bacterial
Cytochrome P450
|
Infection
|
|
Mtb-IN-12 (Compound 5m) is a dual-target inhibitor that can target the CYP125 (KD: 40 nM; KI: 0.1 μM) and CYP142 (KD: 160 nM; KI: 0.05 μM) enzymes of Mycobacterium tuberculosis. Mtb-IN-12 exhibits good inhibitory activity against both drug-sensitive strains and multidrug-resistant tuberculosis strains, with low toxicity to macrophages. Mtb-IN-12 can be used in the research of anti-tuberculosis drugs .
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-
- HY-10575
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Cannabinoid Receptor
Cytochrome P450
|
Metabolic Disease
|
|
MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity .
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-
- HY-15163A
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FLT3
JAK
CDK
|
Cancer
|
|
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-176210
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Fungal
Cytochrome P450
|
Infection
|
|
CYP51-IN-24 (Compound 22) is a Sterol 14α-Demethylase (CYP51) inhibitor. CYP51-IN-24 exhibits potent inhibitory activity against wild-type and drug-resistant fungi. CYP51-IN-24 inhibits ergosterol biosynthesis by binding to the fungal CYP51 enzyme. CYP51-IN-24 can be used in research and drug development against drug-resistant fungal infections .
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-
- HY-121656
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Endogenous Metabolite
|
Cancer
|
|
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-176706
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AAK1
|
Neurological Disease
|
|
AAK1-IN-10 (Compound 1-2) is an AAK1 inhibitor. AAK1-IN-10 has significant AAK1 enzyme inhibitory activity (IC50: 9.62 nM). AAK1-IN-10 mainly exerts its effects by inhibiting the activity of connexin-associated kinase 1 (AAK1). AAK1-IN-10 has low cardiotoxicity (IC50 = 13.7 μM). AAK1-IN-10 can be used in the study of diabetic neuropathy and postherpetic pain .
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-
- HY-13269R
-
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HIV
HIV Integrase
|
Infection
Inflammation/Immunology
|
|
BMS-707035 (Standard) is the analytical standard of BMS-707035. This product is intended for research and analytical applications. 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-146000
-
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Influenza Virus
|
Inflammation/Immunology
|
|
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-173283
-
|
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Fungal
|
Infection
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|
Antifungal agent 129 (Compound 4g) is an inhibitor targeting Rhizoctonia solani, with an EC50 value of 4.27 mg/L. It has a good control effect against rice sheath blight in in vitro and in vivo experiments. Preliminary exploration through scanning electron microscopy, molecular docking, enzyme activity determination, and cytotoxicity experiments has revealed that Antifungal agent 129 may exert its inhibitory activity by affecting the cell structure or physiological processes of Rhizoctonia solani. Antifungal agent 129 can be used in the research of plant diseases in the agricultural field, such as rice sheath blight, which are caused by Rhizoctonia solani .
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-
- HY-146755
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Trk Receptor
|
Cancer
|
|
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
|
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
|
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-14879D
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AVE1330A
|
Beta-lactamase
Bacterial
|
Infection
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|
Ent-Avibactam sodium (AVE1330A) is a β-lactamase inhibitor with broad-spectrum antibacterial activity. When combined with Cefazidime (HY-B0593), ent-Avibactam sodium exhibits significant inhibitory effects on Enterobacteriaceae bacteria that produce Ambler A and C types of β-lactamases. The IC50 value of ent-Avibactam sodium is much lower than that of commonly used β-lactamase inhibitors Clavulanic acid (HY-A0256) and Ticarcillin (HY-139805), demonstrating its high efficiency in inhibiting TEM-1 and P99 enzymes .
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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-146001
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Influenza Virus
|
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-130666
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|
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Endogenous Metabolite
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Cardiovascular Disease
|
|
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-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-W482133
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Herbicide
Acetolactate Synthase (ALS)
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Others
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Primisulfuron-methyl is a herbicide. Primisulfuron-methyl shows inhibitory activity against acetolactate synthase (ALS) enzyme. Primisulfuron-methyl can be used to selectively control annual bluegrass of Kentucky bluegrass turf .
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-
- HY-114554
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Phosphodiesterase (PDE)
PKC
Bacterial
|
Infection
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|
KS 619-1 is a Ca 2+/calmodulin-dependent cyclic nucleotide phosphodiesterase inhibitor. KS 619-1 exhibits strong inhibitory activity against this enzyme derived from bovine brain and heart, but shows weak inhibitory effects on calmodulin-independent phosphodiesterase and protein kinase C. KS 619-1 displays weak antibacterial activity against Staphylococcus aureus .
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- HY-N19889
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|
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Others
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Cardiovascular Disease
|
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Plantainoside E is a phenylpropanoid glycoside. Plantainoside E can be isolated from the leaves of Plantago major L. Plantainoside E shows no angiotensin-converting enzyme inhibitory activity. Plantainoside E can be used in hypertension research .
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-
- HY-11033
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|
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Drug Derivative
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Metabolic Disease
|
|
DNP-60502 is a phthalide derivative. DNP-60502 exhibits potent glucose production inhibitory activity by targeting key regulatory enzymes in hepatic glucose metabolism. DNP-60502 can be used for the study of type 2 diabetes .
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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-180854
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-55 (Compound 2e) is an anti-tuberculous agent. Antitubercular agent-55 exhibits significant inhibitory activity against the standard strain of Mycobacterium tuberculosis H37Rv and also has moderate inhibitory activity against multidrug-resistant TB (MDR-TB). Antitubercular agent-55 has a strong affinity for the key enzyme InhA involved in the biosynthesis of mycotic acids. Antitubercular agent-55 can be used for research on tuberculosis infection caused by Mycobacterium tuberculosis.
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- HY-180202
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Herbicide
Transketolase
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Others
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Transketolase-IN-7 (compound 4m) is a potent herbicide that exhibits inhibitory activity against C. rotundus with an IC50 of 6.66 mg/L. Transketolase-IN-7 is a transketolase (TK) inhibitor that interacts with the TK enzyme by forming hydrogen bonds. Transketolase-IN-7 can be used for research of plant herbicides .
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- HY-W040286R
-
|
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Endogenous Metabolite
Reference Standards
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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-123153
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Isocitrate Dehydrogenase (IDH)
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Cancer
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|
GSK990 is an inactive mutant IDH1 inhibitor with no significant inhibitory activity against wild-type or mutant IDH1/IDH2 enzymes. In experiments, GSK990 can serve as an inactive negative control for the IDH1 inhibitor GSK321 (HY-18948). GSK990 is applicable to the research of acute myeloid leukemia .
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- HY-173263
-
|
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Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-86 (Compound 6f) is an inhibitor of enzyme acetylcholinesterase (AChE) with IC50 values of 25.33 μg/mL. AChE-IN-86 exerts inhibitory activity against AChE through forming hydrogen bonds, π-π and π-alkyl interactions with amino acid residues at the key catalytic sites of AChE. AChE-IN-86 can be used for Alzheimer's disease study .
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-
- HY-181880
-
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PROTACs
NAMPT
|
Cancer
|
|
PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research .
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- HY-182245
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Microtubule/Tubulin
Carbonic Anhydrase
Apoptosis
MDM-2/p53
|
Cancer
|
|
Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
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-
- HY-124714
-
|
|
Kallikrein
|
Cancer
|
|
DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor (IC50=0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 (IC50 values are 1.1 nM and 73 nM, respectively). DKFZ-251 transiently acylates the catalytic serine of KLK6 to form a long-lived acyl-enzyme complex that inhibits enzyme function. DKFZ-251 is a phenotypic modulator that alters cell proliferation capacity and regulates epithelial-mesenchymal transition (EMT). DKFZ-251 can be used in research related to head and neck cancer .
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-
- HY-181327
-
|
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PROTACs
Histone Methyltransferase
|
Others
|
|
PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC50 of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC50 of 0.06 μM .
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-
- HY-N17639
-
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TGF-beta/Smad
TGF-β Receptor
|
Others
|
|
Regiafuran C is a compound with both TGF-βRI inhibitory and anti-fibrotic activities. Regiafuran C effectively inhibits renal fibrosis by binding to TGF-βRI and interfering with the TGF-β/Smad and Wnt/β-catenin signaling pathways. Regiafuran C also exhibits free radical scavenging activity, but shows no anti-inflammatory activity in PGE2 competitive enzyme immunoassays. The ability of Regiafuran C to specifically block the Smad3-TGF-βRII interaction and inhibit fibrotic processes allows its use in renal fibrosis research .
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-
- HY-179529
-
|
|
EGFR
Bacterial
|
Infection
Cancer
|
|
EGFR/InhA-IN-1 (Compound 15) is an inhibitor of the anti-cancer target EGFR tyrosine kinase (1M17) (Ki = 0.05 μM) and the anti-tuberculosis target InhA enzyme (1OUZ) (Ki = 0.02 μM). EGFR/InhA-IN-1 exhibits anti-proliferative activity against A549 cells, with an IC50 of 10.38 μM. EGFR/InhA-IN-1 has inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 6.25 μM. EGFR/InhA-IN-1 can be used for research on non-small cell lung cancer and Mycobacterium tuberculosis infection .
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-
- HY-181266
-
|
|
Parasite
Aminopeptidase
|
Infection
|
|
Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research .
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-
- HY-180115
-
|
|
Bacterial
MMP
|
Infection
|
|
LP07 is an antibacterial agent targeting Pseudomonas aeruginosa with MIC values for both wild-type and efflux pump-deficient P. aeruginosa PA14 of both 8 μg/mL. LP07 exerts its antibacterial effect by directly disrupting the structural integrity of the bacterial cell membrane. LP07 moderately inhibits MMP-17 and MMP-19, but has no significant inhibitory effect on other MMP subtypes. LP07 does not inhibit the activity of LpxC enzyme. LP07 can be used for research on Pseudomonas aeruginosa infections .
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-
- HY-117593
-
|
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P-glycoprotein
Cytochrome P450
Drug Isomer
|
Cancer
|
|
NSC 23925B is a P-glycoprotein (P-gp) inhibitor, as well as the most biologically active isomer of NSC23925 (HY-19626), which reverses and prevents P-glycoprotein-mediated multidrug resistance in cancer cells. NSC 23925B shows weak inhibition against most CYP450 enzymes (IC50 > 10 μM), and exhibits moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B can be used for the research of multidrug-resistant cancers .
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-
- HY-P11358
-
|
|
Angiotensin-converting Enzyme (ACE)
Acetyl-CoA Carboxylase
Mitochondrial Metabolism
|
Inflammation/Immunology
|
|
IRW is an orally active tripeptide produced from egg white with angiotensin converting enzyme (ACE) inhibitory properties. IRW can prevent high-fat diet (HFD)-induced Non-alcoholic fatty liver disease (NAFLD) by modulating hepatic lipid metabolism and increasing mitochondrial content. IRW decreases hepatic triglyceride content and lipid droplet size. IRW increases the hepatic mitochondrial complexes and citrate synthase activity, phosphorylation of 5’-AMP-activated protein kinase and microsomal triglyceride transfer protein abundance. IRW increases phosphorylated acetyl CoA carboxylase and mitochondrial complexes, IRW can be used for the research of inflammation .
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-
- HY-17357
-
|
AHR 9434; AL 6515
|
COX
Prostaglandin Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries .
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-
- HY-N5063
-
|
|
Angiotensin-converting Enzyme (ACE)
IKK
Calcium Channel
PKC
Reactive Oxygen Species (ROS)
NF-κB
Apoptosis
Sirtuin
NOD-like Receptor (NLR)
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Plantainoside D, a phenylethanoid glycosides, is a IKK-β inhibitor with diverse biological activities. Plantainoside D shows inhibitory activity of angiotensin-converting enzyme (ACE) with an IC50 of 2.17 mM. Plantainoside D significantly reduces the release of glutamate from nerve terminals in the cerebral cortex of rats by inhibiting the voltage-dependent calcium channel (VDCCs) and protein kinase C (PKC) signaling cascade. Plantainoside D significantly alleviates cell apoptosis by inhibiting the generation of ROS and the activation of NF-κB. Plantainoside D significantly improves acute lung injury (ALI) induced by sepsis by regulating the Sirt3/NLRP3 signaling pathway. Plantainoside D can be used for the study of neuroprotection, antioxidant, anti-inflammation, antihypertension .
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-
- HY-173320
-
|
|
Hsp-targeting Chimeras
Wee1
HSP
|
Cancer
|
|
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
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-
- HY-19230
-
|
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Calmodulin
NO Synthase
CaMK
Calcineurin
Proteasome
Caspase
|
Cardiovascular Disease
|
|
DY-9760e is a calmodulin (CaM) inhibitor. DY-9760e selectively inhibits the activity of various calmodulin-dependent enzymes by antagonizing the Ca²⁺/CaM complex, exhibiting the strongest inhibitory activity against nNOS, CaM kinase II, and calcineurin (Ki: 0.9, 1.4, and 2.0 μM, respectively). DY-9760e inhibits excessive nitric oxide production and protein tyrosine nitration, as well as the activation of calpain and caspase-3. DY-9760e reduces infarct size, improves cardiac function, and inhibits oxidative stress and cell death. DY-9760e can be used in research on the treatment of myocardial infarction, cerebral ischemia, and other diseases .
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-
- HY-N17737
-
|
|
Fatty Acid Synthase (FASN)
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
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Floramanoside F is a type of flavonol glycoside compound. Floramanoside F has a moderate free radical scavenging effect, with a SC₅₀ value of 25.1 μM. Floramanoside F has a relatively weak inhibitory activity on aldose reductase, with a IC₅₀ value greater than 100 μM. Floramanoside F has strong binding affinity with key target enzymes of type 1 diabetic nephropathy (T1DN) (Fasn, Cyp2e1, Cyp4a32), and can inhibit lipid accumulation and oxidative stress, thereby alleviating renal inflammation and fibrosis. Floramanoside F can be used to study type 1 diabetic nephropathy and diabetic complications .
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- HY-17357R
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AHR 9434 (Standard); AL 6515 (Standard)
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Reference Standards
COX
Prostaglandin Receptor
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Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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Nepafenac (AHR 9434; AL 6515) (Standard) is the analytical standard of Nepafenac (HY-17357). This product is intended for research and analytical applications. Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
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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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![N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly](//file.medchemexpress.com/product_pic/hy-w010991.gif)
- HY-N19401
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Cholinesterase (ChE)
Carbonic Anhydrase
Glycosidase
JNK
p38 MAPK
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Metabolic Disease
Inflammation/Immunology
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Vescalagin is a hexahydroxyphenol. Vescalagin is isolable from Camu-camu (Myrciaria dubia) and immature wax apple fruits. Vescalagin exhibits inhibitory activity against a variety of enzymes, with a Ki value of 5.87 nM against AChE, 3.89 nM against BChE, 11.75 nM against hCA I, 16.23 nM against hCA II, and 16.08 nM against α-glucosidase. Vescalagin inhibits hCA I, hCA II and α-glucosidase in a non-competitive manner. Vescalagin downregulates JNK/p38 MAPK to protect pancreatic β-cells and improve insulin secretion in methylglyoxal-treated rats. Vescalagin reduces hyperglycemia and hypertriglyceridemia in rats fed a high-fructose diet. Vescalagin possesses anti-inflammatory and antioxidant properties .
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- HY-17357S
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AHR-9434-d5; AL-6515-d5
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Isotope-Labeled Compounds
COX
Prostaglandin Receptor
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Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
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- HY-179227
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HDAC
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Neurological Disease
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HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging .
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- HY-U00380
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Antibiotic
Beta-lactamase
Bacterial
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Infection
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Tigemonam is an orally active monobactam antibiotic with a Ki of 0.86 μM against Enterobacter cloacae P99 β-lactamase and 50.8 μM against Escherichia coli TEM-1 β-lactamase. Tigemonam binds to penicillin-binding proteins 1a, 3, and 4, inhibits bacterial cell wall synthesis, and exhibits bactericidal activity against aerobic gram-negative bacteria including Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae. Tigemonam resists hydrolysis by multiple β-lactamase enzymes, reduces bacterial load in systemic, pyelonephritic, lung, and thigh muscle infections in rodents, and shows minimal difference between minimum inhibitory and bactericidal concentrations. Tigemonam can be used for the research of gram-negative bacterial infections, acute pyelonephritis, lung infection, and thigh muscle infection .
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- HY-178448
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EGFR
JAK
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Cannabinoid Receptor
Glutathione Peroxidase
Caspase
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Inflammation/Immunology
Cancer
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EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .
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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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Fluorescent Dyes
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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 |
Type |
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- HY-137878
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PNP-α-NeuNAc
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Biochemical Assay Reagents
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2-O-(p-Nitrophenyl)-α-D-N-acetylneuraminic acid (PNP-α-NeuNAc) is a classic chromogenic substrate for neuraminidase. 2-O-(p-Nitrophenyl)-α-D-N-acetylneuraminic acid releases p-nitrophenol upon enzymatic hydrolysis, allowing quantification of enzyme activity and inhibitory effects via spectrophotometry. 2-O-(p-Nitrophenyl)-α-D-N-acetylneuraminic acid (PNP-α-NeuNAc) acts as a sialyl donor in the process of enzyme-catalyzed trans-sialylation .
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- HY-30139
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Biochemical Assay Reagents
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4-Amino-2-chloropyrimidine is a pyrimidine derivative. 4-Amino-2-chloropyrimidine is a competitive inhibitor for AChE (Ki = 0.18 μM) and BChE (Ki = 1.324 μM). 4-Amino-2-chloropyrimidine fits in the binding pocket of 4BDS. 4-Amino-2-chloropyrimidine has high inhibitory activity on GST enzyme activity (IC50 = 0.037 μM, Ki = 0.047 μM) in vitro .
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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-P4279
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Angiotensin-converting Enzyme (ACE)
Cholinesterase (ChE)
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Cardiovascular Disease
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Ovalbumin (154-159) is a protein fragment consisting of residues 154-159 of chicken ovalbumin. Ovalbumin (154-159) is also a poorly conserved sequence (Thr-Asn-Gly-Ile-Ile-Arg) in the α-subunit of the Torpedo acetylcholine receptor, located within the α150-164 epitope region, and exhibits significant angiotensin-converting enzyme (ACE) inhibitory activity .
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- HY-P11358
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Angiotensin-converting Enzyme (ACE)
Acetyl-CoA Carboxylase
Mitochondrial Metabolism
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Inflammation/Immunology
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IRW is an orally active tripeptide produced from egg white with angiotensin converting enzyme (ACE) inhibitory properties. IRW can prevent high-fat diet (HFD)-induced Non-alcoholic fatty liver disease (NAFLD) by modulating hepatic lipid metabolism and increasing mitochondrial content. IRW decreases hepatic triglyceride content and lipid droplet size. IRW increases the hepatic mitochondrial complexes and citrate synthase activity, phosphorylation of 5’-AMP-activated protein kinase and microsomal triglyceride transfer protein abundance. IRW increases phosphorylated acetyl CoA carboxylase and mitochondrial complexes, IRW can be used for the research of inflammation .
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- HY-P10601A
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- HY-P11334
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Aminopeptidase
Phosphatase
Angiotensin-converting Enzyme (ACE)
DNA/RNA Synthesis
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Cancer
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Cyanostatin B, a cyanobacterial lipopeptide, is a leucine aminopeptidase M (LAP) inhibitor (IC50 = 12 ng/mL). Cyanostatin B is a weak inhibitor of protein phosphatase (PP2A) and also exhibits weak inhibitory activity against angiotensin-converting enzyme (ACE), with an IC50 value of 130 μg/mL. Cyanostatin B demonstrates both cytotoxic and genotoxic effects on human hepatocytes, although non-toxic to Artemia salina. Cyanostatin B inhibits the proliferation of HepG2 cells, induces DNA single-strand breaks, and causes genomic instability. .
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- HY-P10601
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N6972
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- HY-W012530
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- HY-N2010
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- HY-N7072
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- HY-N5063
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- HY-N2157
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(+)-Pteryxin
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Coumarins
Phenylpropanoids
Umbelliferae
Plants
Achillea atrata L.
Source Classification
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Cholinesterase (ChE)
NF-κB
NOD-like Receptor (NLR)
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Nuclear Factor of activated T Cells (NFAT)
p38 MAPK
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Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca 2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease .
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- HY-N2472
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- HY-W041193
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- HY-N9528
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- HY-W012530R
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- HY-N9314
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- HY-N2472R
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- HY-N2298
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- HY-N6972R
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Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
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Autophagy
Reference Standards
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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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-N2266
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- HY-N9535A
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-
-
- HY-N14562
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-
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- HY-N2010R
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- HY-N0025
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- HY-N1483A
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- HY-N1510R
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- HY-114554
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- HY-N19889
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- HY-N17639
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Structural Classification
Phenols
Polyphenols
Plants
Moraceae
Morus alba Linn.
Source Classification
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TGF-beta/Smad
TGF-β Receptor
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Regiafuran C is a compound with both TGF-βRI inhibitory and anti-fibrotic activities. Regiafuran C effectively inhibits renal fibrosis by binding to TGF-βRI and interfering with the TGF-β/Smad and Wnt/β-catenin signaling pathways. Regiafuran C also exhibits free radical scavenging activity, but shows no anti-inflammatory activity in PGE2 competitive enzyme immunoassays. The ability of Regiafuran C to specifically block the Smad3-TGF-βRII interaction and inhibit fibrotic processes allows its use in renal fibrosis research .
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- HY-N17737
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-
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- HY-N19401
-
|
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Structural Classification
Phenols
Polyphenols
Myrciaria dubia (Kunth) McVaugh
Myrtaceae
Plants
Source Classification
|
Cholinesterase (ChE)
Carbonic Anhydrase
Glycosidase
JNK
p38 MAPK
|
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Vescalagin is a hexahydroxyphenol. Vescalagin is isolable from Camu-camu (Myrciaria dubia) and immature wax apple fruits. Vescalagin exhibits inhibitory activity against a variety of enzymes, with a Ki value of 5.87 nM against AChE, 3.89 nM against BChE, 11.75 nM against hCA I, 16.23 nM against hCA II, and 16.08 nM against α-glucosidase. Vescalagin inhibits hCA I, hCA II and α-glucosidase in a non-competitive manner. Vescalagin downregulates JNK/p38 MAPK to protect pancreatic β-cells and improve insulin secretion in methylglyoxal-treated rats. Vescalagin reduces hyperglycemia and hypertriglyceridemia in rats fed a high-fructose diet. Vescalagin possesses anti-inflammatory and antioxidant properties .
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17357S
-
|
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Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
|
-
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![N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly](http://file.medchemexpress.com/product_pic/hy-w010991.gif)
