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-N0920R
    Dihydrokavain (Standard)
    Inhibitor
    Dihydrokavain (Standard) (7,8-Dihydrokawain (Standard)) is the analytical standard of Dihydrokavain (HY-N0920). This product is intended for research and analytical applications. Dihydrokavain is a natural kavalactone compound. Dihydrokavain inhibits COX-1, COX-2, CYP2C9 (IC50 = 130.95 μM), CYP2C19 (IC50 = 10.05 μM) and CYP3A4 (IC50 = 78.59 μM). Dihydrokavain reduces TNFα secretion. Dihydrokavain shows analgesic and anxiolytic effects.
    Dihydrokavain (Standard)
  • HY-101284A
    (E/Z)-DMU2105
    Inhibitor
    (E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity.
    (E/Z)-DMU2105
  • HY-N7136R
    α-​Terpinyl acetate (Standard)
    Inhibitor
    α-Terpinyl acetate (Standard) is the analytical standard of α-Terpinyl acetate. This product is intended for research and analytical applications. α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
    α-​Terpinyl acetate (Standard)
  • HY-162574
    CYP11B2-IN-2
    Inhibitor
    CYP11B2-IN-2 (Compound 10k) is an inhibitor for enzyme aldosterone synthase CYP11B2 with an IC50 of 0.3 nM. CYP11B2-IN-2 CYP11B-IN-2 is labeled with 18F and can be used as a positron emission tomography (PET) tracer for the diagnosis of primary aldosteronism.
    CYP11B2-IN-2
  • HY-134999
    10-Hydroxywarfarin
    Inhibitor
    10-Hydroxywarfarin, a metabolite of (R)-(+)-Warfarin (HY-W015998 ), is a CYP2C9 and vitamin K epoxide reductase complex 1 (VKOR) inhibitor with IC50s of 1.6 µM and 80 ng/mL, respectively.
    10-Hydroxywarfarin
  • HY-B2015R
    Carbosulfan (Standard)
    Inhibitor
    Carbosulfan (Standard) is the analytical standard of Carbosulfan. This product is intended for research and analytical applications.
    Carbosulfan (Standard)
  • HY-B1232R
    Metyrapone (Standard)
    Inhibitor
    Metyrapone (Standard) is the analytical standard of Metyrapone. This product is intended for research and analytical applications. Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression.
    Metyrapone (Standard)
  • HY-N3841A
    δ-Viniferin
    Inhibitor
    δ-Viniferin is a resveratrol dehydrodimer, an isomer of ε-Viniferin (HY-N3841). ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.
    δ-Viniferin
  • HY-163633
    CYP51-IN-18
    Inhibitor
    CYP51-IN-18 (compound 2l) is a potent CYP51 inhibitor with an IC50 of 0.219 μg/mL. CYP51-IN-18 shows significant fungicidal activity against B. cinerea with an EC50 of 0.369 μg/mL.
    CYP51-IN-18
  • HY-W762012
    Octachlorodibenzo-p-dioxin
    Activator
    Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant but is not acutely toxic. In rats, Octachlorodibenzo-p-dioxin (50 μg/kg i.v. or 50-5000 μg/kg p.o.) has a systemic elimination half-life of 3-5 months and accumulates and concentrates in the liver and adipose tissue after low-dose, repeated exposure. Repeated administration of octachlorodibenzo-p-dioxin causes increases in 7-ethoxyresorufin-O-deethylase (7-EROD) activity and total cytochrome P-450 levels.
    Octachlorodibenzo-p-dioxin
  • HY-B1184R
    Mephenytoin (Standard)
    Mephenytoin (Standard) is the analytical standard of Mephenytoin. This product is intended for research and analytical applications. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.
    Mephenytoin (Standard)
  • HY-105375
    FR 901537
    Inhibitor
    FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research.
    FR 901537
  • HY-116232
    2-(3-Pyridyl)-benzimidazole
    Inhibitor
    2-(3-Pyridyl)-benzimidazole is an Aminopyrine N-Demethylase inhibitor.
    2-(3-Pyridyl)-benzimidazole
  • HY-156481
    SU-8000
    Inhibitor
    SU-8000 is an inhibitor that selectively targets 17α-hydroxylase and C17-20-lyase in rat testes. When administered to pregnant rats, SU-8000 can cause hypospadias in male fetuses.
    SU-8000
  • HY-B0105R
    Ketoconazole (Standard)
    Inhibitor
    Ketoconazole (Standard) is the analytical standard of Ketoconazole. This product is intended for research and analytical applications. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole (Standard)
  • HY-N8405
    Isolimonexic acid
    Inhibitor
    Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties.
    Isolimonexic acid
  • HY-164510
    N-Formyldemecolcine
    N-Formyldemecolcine is a colchicine precursor that contains the characteristic tropolone ring and pharmacophore of colchicine. N-Formyldemecolcine can be synthesized de novo by genetically engineering transgenic Nicotiana benthamiana and atypical cytochrome P450s that catalyze the production of colchicine's unique carbon scaffold.
    N-Formyldemecolcine
  • HY-13834
    GW844520
    Inhibitor
    GW844520 is an orally active inhibitor of cytochrome bc1 complex. GW844520 can be used in malaria and anti-plasmodium related research.
    GW844520
  • HY-B2169R
    Melperone (Standard)
    Inhibitor
    Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone (Standard)
  • HY-B2169S2
    Melperone-d4 hydrochloride
    Inhibitor 99.84%
    Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109). Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone-d<sub>4</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity

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