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-P11812
    MLS peptide
    MLS peptide is a Mitochondria-targeting peptide. MLS peptide participates in respiratory chain function via encoding Cytochrome C oxidase.
    MLS peptide
  • HY-116811
    AZ-11665362
    Inhibitor
    AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC50 of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases.
    AZ-11665362
  • HY-100189
    LS2265
    LS2265 is a taurine derivative of fenofibrate and can induce proliferation of peroxisomes in liver cells of rats.
    LS2265
  • HY-134664
    8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate
    Inhibitor
    8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible CYP2A6 inhibitor with IC50s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC50s of 60.2 and 38.6 μM, respectively.
    8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate
  • HY-121057
    3-Hydroxyflunitrazepam
    3-Hydroxyflunitrazepam (3-OH FNTZ) is the major metabolite of Flunitrazepam (FNTZ), generated via 3-hydroxylation by CYP3A4 (Km = 286 μM), and represents the dominant metabolic pathway (>80%) in liver microsomes. Its formation is significantly inhibited by CYP3A4 inhibitors such as Ketoconazole (HY-B0105) (IC50 = 0.11 μM) and Ritonavir (HY-90001) (IC50 = 0.041 μM), indicating a strong dependence on CYP3A4 activity and potential drug interactions.
    3-Hydroxyflunitrazepam
  • HY-B1812S2
    Veratrole-d10
    Substrate
    Veratrole-d10 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.
    Veratrole-d<sub>10</sub>
  • HY-149866
    HIV-1 inhibitor-58
    Inhibitor
    HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch.
    HIV-1 inhibitor-58
  • HY-G0007S1
    Omeprazole sulfone-13C,d3
    Control
    Omeprazole sulfone-13C,d3 is the deuterium and 13C labeled Omeprazole sulfone. Omeprazole sulfone (Omeprazole sulphone) is one of the major circulating metabolites of Omeprazole (HY-B0113) in vivo, and belongs to class 4 non-mutagenic impurities. Omeprazole sulfone does not bind to the aryl hydrocarbon receptor (AhR), nor does it induce the expression of CYP1A1 or CYP1A2. However, Omeprazole sulfone promotes the migration of gastric epithelial cells under basal conditions and reverses the inhibitory effect of Indomethacin (HY-14397) on cell migration. Omeprazole sulfone does not promote cell proliferation, nor does it upregulate COX-2 expression or activate signaling pathways such as ERK, P38 MAPK and PI3K. Omeprazole sulfone maintains basal ulcer healing under non-acid-dependent conditions and can be used in studies related to gastric ulcer repair.
    Omeprazole sulfone-<sup>13</sup>C,d<sub>3</sub>
  • HY-170912
    Topo I/II-IN-2
    Activator
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-N2229R
    Rhapontigenin (Standard)
    Inhibitor
    Rhapontigenin (Standard) is the analytical standard of Rhapontigenin. This product is intended for research and analytical applications. Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50 = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively.
    Rhapontigenin (Standard)
  • HY-121698
    GW694481
    Inhibitor
    GW694481 is an ApoA1 upregulator with IC50 values of 2.1 μM for CYP2C9 inhibition and 17.0 μM for CYP3A4 inhibition. GW694481 upregulates ApoA1 expression in human hepatic cells.GW694481 can be used for the research of atherosclerosis.
    GW694481
  • HY-149081
    ERα degrader 6
    Inhibitor
    ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research.
    ERα degrader 6
  • HY-A0016S
    Dronedarone-d6 hydrochloride
    Inhibitor
    Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone-d<sub>6</sub> hydrochloride
  • HY-B1324A
    Oxiconazole
    Activator
    Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest.
    Oxiconazole
  • HY-147999
    GlcN-6-P Synthase-IN-1
    Inhibitor
    GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform.
    GlcN-6-P Synthase-IN-1
  • HY-N0893S
    Tetrahydrocurcumin-d6
    Inhibitor
    Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4.
    Tetrahydrocurcumin-d<sub>6</sub>
  • HY-152250
    Antibacterial agent 132
    Inhibitor
    Antibacterial agent 132 has anticandidal effects against C. parapsilosis (ATCC 22019) and C. krusei (ATCC 6258) with MIC90 values of <0.06 μg/mL and 62.50 μg/mL, respectively. Antibacterial agent 132 inhibits aromatase enzyme with an IC50 of 0.047μM.
    Antibacterial agent 132
  • HY-135739
    Benzobarbital
    Activator
    Benzobarbital is an active low-toxicity inductor of the liver monooxygenase system. Benzobarbital raises cytochrome P-450 concentration. Benzobarbital can be used in the research of post-ischemic liver disease.
    Benzobarbital
  • HY-17367AR
    Atazanavir sulfate (Standard)
    Inhibitor
    Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir sulfate (Standard)
  • HY-W762015
    1,2,3,6,7,8-Hexachlorodibenzofuran
    Inducer
    1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 1,2,3,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC50s = 1.47 and 1.24 nM, respectively). 1,2,3,6,7,8-Hexachlorodibenzofuran reduces weight, induces thymic atrophy, and induces the expression of genes encoding the cytochrome P450 (CYP) isoform CYP1A1 and 4-chlorobiphenyl hydroxylase in rats (EC50s = 3.2, 0.9, 0.35, and 0.21 µmol/kg, respectively).
    1,2,3,6,7,8-Hexachlorodibenzofuran
Cat. No. Product Name / Synonyms Application Reactivity

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