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-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-N15528
    Pipercroside A
    Inhibitor
    Pipercroside A is found in Piper crocatum Ruiz & Pav. Pipercroside A is a CYP51 inhibitor. Pipercroside A has antifungal activity.
    Pipercroside A
  • 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
  • HY-117789
    Keto-itraconazole
    Inhibitor
    Keto-itraconazole (keto-ITZ) is a metabolism of Itraconazole (HY-17514) with a potent inhibitor activity of CYP3A. Keto-itraconazole shows unbound IC50 value of 4.6 nM when coincubated with human liver microsomes and midazolam.
    Keto-itraconazole
  • HY-B0035B
    Sulfamethazine 100 µg/mL in acetonitrile
    Activator
    Sulfamethazine 100 μg/mL in acetonitrile (Sulfadimidine 100 μg/mL in acetonitrile) is an antimicrobial agent that induces CYP3A4 expression and is acetylated by N-acetyltransferase. It exhibits sex-dependent pharmacokinetics and is metabolized by CYP2C11 in males.
    Sulfamethazine 100 µg/mL in acetonitrile
  • HY-B0852S2
    Tebuconazole-d6
    Tebuconazole-d6 is a deuterium labeled Tebuconazole (HY-B0852). Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.
    Tebuconazole-d<sub>6</sub>
  • HY-126308
    (E/Z)-DMU2139
    Inhibitor
    (E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM).
    (E/Z)-DMU2139
  • HY-128706
    (+)-Menthofuran
    Inhibitor
    (+)-Menthofuran (compound 1) is a furan terpenoid that can be found in mint oils.
    (+)-Menthofuran
  • HY-W008364R
    Olivetol (Standard)
    Inhibitor
    Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
    Olivetol (Standard)
  • HY-157170
    CYP450-IN-1
    Inhibitor
    CYP450-IN-1 (compound 2e) is a potent inhibitor of CYP450.
    CYP450-IN-1
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