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-107204R
    Furafylline (Standard)
    Inhibitor
    Furafylline (Standard) is the analytical standard of Furafylline. This product is intended for research and analytical applications. Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM.
    Furafylline (Standard)
  • HY-115824
    7ETMC
    Inhibitor
    7ETMC is a cytochrome P450 inhibitor with selective inhibition of human cytochrome P450s 1A1 and 1A2. 7ETMC has inhibitory effects on P450s 1A1 and 1A2 with IC?? values of 0.46μM and 0.50μM, respectively, within the first six minutes, and has no inhibitory activity against P450s 2A6 and 2B1. Except for 7-ethynyl-3-methyl-4-phenylcoumarin, the remaining inhibitors show mechanism-based inhibition of P450s 1A1 and 1A2.
    7ETMC
  • HY-E70498
    Human CYP4F3,Low-Reductase
    Human CYP4F3, Low-Reductase, a recombinant CYP4F3, is a member of the CYP enzyme family. CYP4F3 is an enzyme mainly expressed in polymorphonuclear leukocytes.
    Human CYP4F3,Low-Reductase
  • HY-156182
    JNK-IN-14
    JNK-IN-14 is a potent JNK inhibitor with IC50 values of 1.81, 12.7 and 10.5 nM for JNK1, JNK2 and JNK3, respectively. JNK-IN-14 induces early-stage apoptosis. JNK-IN-14 shows cell population arrest at the G2/M phase and slightly inhibits beclin-1 production at K562 leukemia cells relative to SP600125 (HY-12041), showing higher inhibitory ability.
    JNK-IN-14
  • HY-B0940R
    Ethylvanillin (Standard)
    Ethylvanillin (Standard) is the analytical standard of Ethylvanillin. This product is intended for research and analytical applications. Ethylvanillin is a flavoring that is three times more potent than Vanillin and is used in the production of chocolate.
    Ethylvanillin (Standard)
  • HY-E70494
    Human CYP2C8,High-Reductase+b5
    Human CYP2C8, High-Reductase+b5, a recombinant CYP2C8, is a member of the CYP enzyme family and is involved in the metabolism of xenobiotics in the body.
    Human CYP2C8,High-Reductase+b5
  • HY-E70462
    Human CYP2C19,High-Reductase
    Human CYP2C19, High-Reductase, a recombinant CYP2C19, is a member of the CYP enzyme family. CYP2C19 catalyzes metabolism of xenobiotics, including some proton pump inhibitors and antiepileptic drugs.
    Human CYP2C19,High-Reductase
  • 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-E70464
    Human CYP3A4,Low-Reductase
    Human CYP3A4, Low-Reductase, a recombinant CYP3A4, is a multifunctional enzyme with a wide range of substrates.
    Human CYP3A4,Low-Reductase
  • HY-B2015S
    Carbosulfan-d18
    Inhibitor
    Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
    Carbosulfan-d<sub>18</sub>
  • 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-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-E70506
    Human CYP2C19,High-Reductase+b5
    Human CYP2C19, High-Reductase+b5, a recombinant CYP2C19, is a member of the CYP enzyme family. CYP2C19 catalyzes metabolism of xenobiotics, including some proton pump inhibitors and antiepileptic drugs.
    Human CYP2C19,High-Reductase+b5
  • 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-76316R
    Bergaptol (Standard)
    Inhibitor
    Bergaptol (Standard) is the analytical standard of Bergaptol. This product is intended for research and analytical applications. Bergaptol is an inhibitor of debenzylation of the CYP3A4 enzyme with an IC50 of 24.92 μM. Recent studies have shown that it has anti-proliferative and anti-cancer properties.
    Bergaptol (Standard)
  • HY-17356S
    Fenofibrate-d6
    Inhibitor 99.70%
    Fenofibrate-d6 is the deuterium labeled Fenofibrate. 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-d<sub>6</sub>
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