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-B0859
    MCPA
    Activator 98.17%
    MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds.
    MCPA
  • HY-148070
    FLT3-IN-17
    Inhibitor 99.11%
    FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers.
    FLT3-IN-17
  • HY-152118
    CYP1B1-IN-4
    Inhibitor 99.09%
    CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes.
    CYP1B1-IN-4
  • HY-P10032A
    NN1177 TFA
    Inhibitor 98.66%
    NN1177 (NNC9204-1177) TFA is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 TFA can induce a dose-dependent body weight loss in diet-induced obese (DIO) mice.
    NN1177 TFA
  • HY-N1457
    Chrysosplenetin
    Inhibitor 99.68%
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
    Chrysosplenetin
  • HY-17356R
    Fenofibrate (Standard)
    Inhibitor
    Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate (Standard)
  • HY-W040468
    2-Phenyl-2-(1-piperidinyl)propane
    Inhibitor 99.72%
    2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM).
    2-Phenyl-2-(1-piperidinyl)propane
  • HY-41268
    3-Methoxyphenylethylamine
    Substrate 99.39%
    3-Methoxyphenylethylamine is an organic compound that is used as an intermediate for pharmaceuticals, dyestuffs, and liquid crystal materials.
    3-Methoxyphenylethylamine
  • HY-W027773
    7-Methoxy-4-(trifluoromethyl)coumarin
    ≥98.0%
    7-Methoxy-4-(trifluoromethyl)coumarin (MFC) is a fluorescent substrate for cytochrome P450 and can quantify CYP activity.
    7-Methoxy-4-(trifluoromethyl)coumarin
  • HY-A0064S
    Verapamil-d3 hydrochloride
    Inhibitor 99.57%
    Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil-d<sub>3</sub> hydrochloride
  • HY-145786
    Abiraterone decanoate
    Inhibitor 99.69%
    Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.
    Abiraterone decanoate
  • HY-128859
    EMT inhibitor-2
    Inhibitor 98.83%
    EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
    EMT inhibitor-2
  • HY-17508R
    Clarithromycin (Standard)
    Inhibitor
    Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
    Clarithromycin (Standard)
  • HY-156530
    CYP11A1-IN-1
    Inhibitor 99.64%
    CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1, with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.
    CYP11A1-IN-1
  • HY-N2129
    N-Nornuciferine
    Inhibitor 99.94%
    N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits CYP2D6 with IC50 and Ki of 3.76 and 2.34 μM, respectively.
    N-Nornuciferine
  • HY-N1356A
    (R)-Reticuline
    99.41%
    (R)-Reticuline is an isomer of Reticuline (HY-N1356). Reticuline displays anti-inflammatory and cardiovascular effects through JAK2/STAT3 and NF-κB signaling pathways. Salutaridine is a key intermediate in morphine biosynthesis. Salutaridine can be converted from (R)-Reticuline in the poppy plant. The conversion system relies on membrane-bound cytochrome P-450 enzymes and also requires reducing cofactors NADPH, molecular oxygen, etc.
    (R)-Reticuline
  • HY-136373
    Metazachlor
    99.76%
    Metazachlor (BAS 479H) is a herbicide belonging to the chloroacetamides class. Metazachlor can inhibit the synthesis of very long chain fatty acids during the germination and emergence of weed seeds, thereby interfering with cell division and tissue differentiation, and thus hindering the normal growth and development of weeds.
    Metazachlor
  • HY-144652
    IDO1-IN-19
    Inhibitor 98.82%
    IDO1-IN-19 (Compound 17) is an orally active IDO1 inhibitor with an IC50 of CYP2C9 of 8.64 μM. IDO1-IN-19 also acts funciton on cardiac channels, with IC50s of 12 μM (IKr), 40 μM (INa), 8.3 μM (ICa), respectively. IDO1-IN-19 has the potential to study cancer diseases.
    IDO1-IN-19
  • HY-B2169
    Melperone
    Inhibitor 99.84%
    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
  • HY-106019C
    Liarozole dihydrochloride
    Inhibitor 99.04%
    Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.
    Liarozole dihydrochloride
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