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-N1882
    4,5-Dimethoxycanthin-6-one
    Inhibitor 98.68%
    4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae).
    4,5-Dimethoxycanthin-6-one
  • HY-14273R
    Isavuconazole (Standard)
    Inhibitor
    Isavuconazole (Standard) is the analytical standard of Isavuconazole. This product is intended for research and analytical applications. Isavuconazole (BAL-4815) is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
    Isavuconazole (Standard)
  • HY-W196803
    Dipropyl disulfide
    99.30%
    Dipropyl disulfide is oxidized to dipropyl thiosulfinate (DPDSO) by rat microsomes. Both flavincontaining monooxygenases (FMO) and cytochrome P450 enzymes (CYPs) are involved in dipropyl disulfide oxidation. Dipropyl disulfide forms two metabolites: propylglutathione sulfide conjugate and propylthiol.
    Dipropyl disulfide
  • HY-B0973
    Dibenzothiophene
    Inhibitor 99.47%
    Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with a Km of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms.
    Dibenzothiophene
  • HY-116862
    Dibenzylfluorescein
    99.54%
    Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 μM (Ex=485 nm,Em=535 nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease.
    Dibenzylfluorescein
  • HY-15996B
    Seviteronel racemate
    Inhibitor 98.11%
    Seviteronel racemate (VT-464 racemate) is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
    Seviteronel racemate
  • HY-17411R
    Limonin (Standard)
    Inhibitor
    Limonin (Standard) is the analytical standard of Limonin. This product is intended for research and analytical applications. Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities.
    Limonin (Standard)
  • HY-19599
    Vorozole
    Inhibitor
    Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor. Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer.
    Vorozole
  • HY-136063R
    Mefentrifluconazole (Standard)
    Inhibitor
    Mefentrifluconazole (Standard) is the analytical standard of Mefentrifluconazole. This product is intended for research and analytical applications. Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM)[1].
    Mefentrifluconazole (Standard)
  • HY-111421
    ODM-204
    Inhibitor
    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
    ODM-204
  • HY-14802
    Talarozole (R enantiomer)
    Inhibitor
    Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.
    Talarozole (R enantiomer)
  • HY-131910
    IHMT-PI3Kδ-372
    Inhibitor
    IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56~83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.
    IHMT-PI3Kδ-372
  • HY-B1751C
    Quinine hydrobromide
    Inhibitor
    Quinidine hydrobromide is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine hydrobromide is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine hydrobromide can be used for malaria research.
    Quinine hydrobromide
  • HY-B1232A
    Metyrapone Tartrate
    Inhibitor
    Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression.
    Metyrapone Tartrate
  • HY-170569
    Cetagliptin
    Inhibitor
    Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research.
    Cetagliptin
  • HY-150787
    BMS-986339
    Inhibitor
    BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis.
    BMS-986339
  • HY-14247B
    Fadrozole hydrochloride hemihydrate
    Inhibitor
    Fadrozole hydrochloride hemihydrate is an orally active, potent, selective and nonsteroidal aromatase inhibitor, with an IC50 of 6.4 nM. Fadrozole hydrochloride hemihydrate inhibits the production of estrogen and progesterone, with IC50 values of 0.03 and 120 μM. Fadrozole hydrochloride hemihydrate shows prevention of spontaneous tumours. Fadrozole hydrochloride hemihydrate can be used for the research of estrogen-dependent disease and cancer.
    Fadrozole hydrochloride hemihydrate
  • HY-107133
    Simmitecan hydrochloride
    Inhibitor
    Simmitecan hydrochloride, a 9-substituted lipophilic Camptothecin (HY-16560) derivative, is a potent topoisomerase I inhibitor. Simmitecan hydrochloride is an anticancer agent.
    Simmitecan hydrochloride
  • HY-14274S
    Anastrozole-d12
    Inhibitor
    Anastrozole-d12 is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM[1][2].
    Anastrozole-d<sub>12</sub>
  • HY-17367S3
    Atazanavir-d5
    Inhibitor
    Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
    Atazanavir-d<sub>5</sub>
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