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

Cytochrome P450

CYPs

Cytochrome P450

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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.

Cytochrome P450 Isoform Specific Products:

Cytochrome P450 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146458
    Antibacterial agent 102
    		Inhibitor
    Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice.
    Antibacterial agent 102
  • HY-178053
    AHR agonist 10
    		Agonist
    AHR agonist 10 is a potent AHR agonist (EC50 = 2.01 nM). AHR agonist 10 can elevate the transcript levels of key AHR downstream pathway target genes, including CYP1A1 and CYP1B1. AHR agonist 10 can downregulate the expression levels of CD36, IL-18 and shows low cytotoxicity (>40 μM) to normal cells. AHR agonist 10 can suppress the expression of CCL5, CCL20, IL-6, IL-8, S100A9, TLR4, TNF-α, and TNFR1, demonstrating that AHR agonist 10 effectively modulate inflammatory responses through AHR dependent signaling pathways. AHR agonist 10 can be used for psoriasis research.
    AHR agonist 10
  • HY-117593
    NSC 23925B
    		Inhibitor
    NSC 23925B is a P-glycoprotein (P-gp) inhibitor, as well as the most biologically active isomer of NSC23925 (HY-19626), which reverses and prevents P-glycoprotein-mediated multidrug resistance in cancer cells. NSC 23925B shows weak inhibition against most CYP450 enzymes (IC50 > 10 μM), and exhibits moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B can be used for the research of multidrug-resistant cancers.
    NSC 23925B
  • HY-176497
    GW273297X
    		Inhibitor
    GW273297X is a selective CYP27A1 inhibitor. GW273297X blocks 27-hydroxycholesterol biosynthesis and sterol product formation in human macrophages. GW273297X reduces cancer cells colonization by inhibiting pro-metastatic effects of 27-hydroxycholesterol. GW273297X can be used for the researches of cancer and metabolic disease, such as breast cancer.
    GW273297X
  • HY-116214S1
    Cyprodinil-13C6
    		Inducer
    Cyprodinil-13C6 (CGA-219417-13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil-<sup>13</sup>C<sub>6</sub>
  • HY-121789
    Proadifen
    		Inhibitor
    Proadifen is a compound that inhibits cytochrome P450 activity, which can change the excitability of catecholamine-secreting neurons in the brain and have different effects on neurons in different brain regions.
    Proadifen
  • HY-175760
    CYP1B1-IN-11
    		Inhibitor
    CYP1B1-IN-11 (Compound M2) is a selective CYP1B1 inhibitor with an IC50 of 0.00605 pM. CYP1B1-IN-11 effectively reverses DMBA (HY-W011845)-induced Paclitaxel (HY-B0015) resistance and CYP1B1-IN-11 suppresses tumor cells invasion and migration. CYP1B1-IN-11 can be used for tumor drug resistance research.
    CYP1B1-IN-11
  • HY-136745
    Aromatase-IN-1
    		Inhibitor
    Aromatase-IN-1 is a competitive aromatase (P450arom) inhibitor with a human IC50 of 40 nM and a Ki of 1.05 nM. Aromatase-IN-1 binds via coordination of imidazole nitrogen to the heme iron of aromatase. Aromatase-IN-1 can be used for the research of breast cancer.
    Aromatase-IN-1
  • HY-115754
    S-(N-PhenethylthiocarbaMoyl)-L-cysteine
    		Inhibitor
    S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys), an anticarcinogenic agent, has antileukemic activity. S-(N-PhenethylthiocarbaMoyl)-L-cysteine inhibits DNA synthesis in HL60 cells. S-(N-PhenethylthiocarbaMoyl)-L-cysteine is a P450 inhibitor.
    S-(N-PhenethylthiocarbaMoyl)-L-cysteine
  • HY-162784
    CYP51-IN-19
    		Inhibitor
    CYP51-IN-19 (compound C07) is a potent CYP51 inhibitor. CYP51-IN-19 stimulates reactive oxygen species (ROS) and exhibits potent fungicidal activity.
    CYP51-IN-19
  • HY-183260
    HBV-IN-57
    		Inhibitor
    HBV-IN-57 is an orally active HBV inhibitor with pan-genotypic efficacy against HBV genotypes B/C. HBV-IN-57 inhibits HBV DNA replication and HBV capsid assembly. HBV-IN-57 can be used for the research of chronic hepatitis B.
    HBV-IN-57
  • HY-13832S3
    cis-Atovaquone-d4
    		Inhibitor
    cis-Atovaquone-d4 is deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and  P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
    cis-Atovaquone-d<sub>4</sub>
  • HY-182771
    20-HETE IN-3
    		Inhibitor
    20-HETE IN-3 is an orally bioavailable 20-HETE synthesis inhibitor. 20-HETE IN-3 can be used in the research of obesity.
    20-HETE IN-3
  • HY-106019A
    Liarozole hydrochloride
    		Inhibitor
    Liarozole hydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole hydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole hydrochloride shows antitumoral properties.
    Liarozole hydrochloride
  • HY-151253
    CYP2C1/CYP2C19-IN-2
    		Inhibitor
    CYP2C1/CYP2C19-IN-2 (compound 21d) is a potent CYP2C9/CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C1/CYP2C19-IN-2 can be used in study of anti-ZIKV.
    CYP2C1/CYP2C19-IN-2
  • HY-N3841R
    ε-Viniferin (Standard)
    		Inhibitor
    ε-Viniferin (Standard) is the analytical standard of ε-Viniferin. This product is intended for research and analytical applications. ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, 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.
    ε-Viniferin (Standard)
  • HY-N0382S
    Galangin-13C3
    		Inhibitor
    Galangin-13C3 is the 13C-labeled Galangin. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin-<sup>13</sup>C<sub>3</sub>
  • HY-W703936
    Cloranolol
    		Inhibitor
    Cloranolol is an orally active nonselective β-adrenoceptor blocker. Cloranolol can reduce the content of cytochrome P-450 in rat hepatocytes, prolong hexobarbital anesthesia time, and inhibit aminopyrine-N-demethylation activity. Cloranolol can be used in the research of cardiovascular diseases such as hypertension.
    Cloranolol
  • HY-174342
    ELQ-453
    		Inhibitor
    ELQ-453 is an inhibitor targeting the Qo site of the Plasmodium falciparum cytochrome bc1 complex (CytB) with an IC50 value of 0.57 nM. ELQ-453 blocks the mitochondrial function of the parasite, and suppresses Plasmodium infection in mosquitoes. ELQ-453 is promising for research of malaria.
    ELQ-453
  • HY-W140208
    3-Phenylthiophene
    		Inhibitor
    3-Phenylthiophene (Compound 25) is a CYP2A6 inhibitor with a Ki value of 3.3 μM. The Ki values for CYP2E1, CYP2B6, CYP2C9, and CYP2C19 are 9.7, 14, 112, and 107 μM respectively. It shows no significant inhibition on CYP3A4 and CYP2D6. 3-Phenylthiophene can be used in smoking cessation research.
    3-Phenylthiophene
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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