1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N1201R
    Apigenin (Standard)
    Inhibitor
    Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
    Apigenin (Standard)
  • HY-N2260
    Cephaeline dihydrochloride
    Inhibitor 99.67%
    Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
    Cephaeline dihydrochloride
  • HY-N7128
    Flavanone
    Inhibitor 99.73%
    Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
    Flavanone
  • HY-131968
    BMS-986202
    Inhibitor 99.29%
    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium.
    BMS-986202
  • HY-170538
    SNT-5382
    Inhibitor 99.96%
    SNT-5382 is a lysyl oxidase family (LOX) inhibitor and anti-fibrotic agent. SNT-5382 binds to the LTQ cofactor of LOXL2 and inhibits the enzymatic activities of LOXL3, LOXL4, LOXL1, CYP2C9, and CYP2C19. SNT-5382 reduces cardiac and liver fibrosis as well as collagen crosslinks, and improves cardiac function. SNT-5382 can be used for the research of heart failure, myocardial infarction, and nonalcoholic steatohepatitis-related liver fibrosis.
    SNT-5382
  • HY-N0094
    Ipriflavone
    Inhibitor 99.89%
    Ipriflavone is a synthetic isoflavone derivative used to suppress bone resorption.
    Ipriflavone
  • HY-B0876A
    Fomepizole hydrochloride
    Inhibitor 99.85%
    Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning.
    Fomepizole hydrochloride
  • HY-119983
    7H-Dibenzo[c,g]carbazole
    Activator 99.98%
    7H-Dibenzo[c,g]carbazole (DBC) is an azaarene with high lipophilicity. 7H-Dibenzo[c,g]carbazole has carcinogenic activity and induce DNA adducts in fish, DNA adducts, mutations in diploid human fibroblasts and micronuclei in human blood lymphocytes. 7H-Dibenzo[c,g]carbazole is activated by cytochrome P450 enzymes resulting mainly in the generation of phenolic metabolites.
    7H-Dibenzo[c,g]carbazole
  • HY-137258
    (±)-N-3-Benzylnirvanol
    Inhibitor 99.86%
    (±)-N-3-Benzylnirvanol is a racemic mixture of (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol. (+)-N-3-Benzylnirvanol and (–)-N-3-Benzylnirvanol are potent and selective cytochrome P450 inhibitors with Ki values of 0.25 and 5.3 μM for CYP2C19, respectively.
    (±)-N-3-Benzylnirvanol
  • HY-163436
    F44-A13
    Inducer
    F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.
    F44-A13
  • HY-B1324
    Oxiconazole nitrate
    Activator 98.0%
    Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest.
    Oxiconazole nitrate
  • HY-W072025
    CYP2E1-IN-1
    Inhibitor 99.95%
    CYP2E1-IN-1 (Compound 10) is an orally active cytochrome P450 2E1 (CYP2E1) inhibitor with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. CYP2E1-IN-1 activates the Nrf2/HO-1 signaling pathway and inhibits ROS production, thereby alleviating pancreatic injury. CYP2E1-IN-1 has significant anti-inflammatory and antioxidant activities and can effectively reduce inflammation and oxidative stress in severe acute pancreatitis (SAP). CYP2E1-IN-1 can be used in the study of SAP and other inflammatory-related diseases.
    CYP2E1-IN-1
  • HY-B0237
    Aminoglutethimide
    Inhibitor 98.87%
    Aminoglutethimide (DL-Aminoglutethimide) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC50 values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide reduces cortisol levels. Aminoglutethimide can be used in research on Cushing's syndrome, breast cancer, and other conditions.
    Aminoglutethimide
  • HY-15603
    TS-011
    Inhibitor 99.92%
    TS-011 is a selective inhibitor of 20-Hydroxyeicosatetraenoic acid synthesis.
    TS-011
  • HY-155351
    PARP7-IN-15
    Inhibitor 99.03%
    PARP7-IN-15 is an orally active and selective PARP7 inhibitor with an IC50 of 0.56 nM. PARP7-IN-15 inhibits the enzymatic activity of PARP7 and induces anti-tumor activity against lung cancer in vivo. PARP7-IN-15 can be used for the research of lung cancer.
    PARP7-IN-15
  • HY-18063
    ML252
    Inhibitor 99.9%
    ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant .
    ML252
  • HY-148825
    NP10679
    Inhibitor 98.40%
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
    NP10679
  • HY-W355129
    MeIQx
    Inhibitor 99.48%
    MeIQx, a dietary aromatic amine, is mutagenic compound could be isolated from present in fried beef and beef extracts. MeIQx binds covalently to hemoglobin. MeIQx induces liver tumors.
    MeIQx
  • HY-W267897
    7-Benzyloxy-4-(trifluoromethyl)coumarin
    99.47%
    7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies.
    7-Benzyloxy-4-(trifluoromethyl)coumarin
  • HY-15565
    APD668
    Inhibitor 99.73%
    APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.
    APD668
Cat. No. Product Name / Synonyms Application Reactivity

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