Signaling Pathway

Cytochrome P450

Cytochrome P450

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Cytochrome p450s comprise 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 know 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 Inhibitors & Modulators (31)

Product Name Catalog No. Brief Description
10-Undecenoic acid

HY-B0914

10-Undecenoic acid was used as a starting reagent in the syntheses of Pheromone (11Z)-hexadecenal.

3-Cyano-7-ethoxycoumarin

HY-D0055

3-Cyano-7-ethoxycoumarin is a fluorogenic cytochrome P-450 substrate that generates blue fluorescent product upon enzyme cleavage.

5-Methoxypsoralen

HY-N0370

5-Methoxypsoralen, a naturally occurring linear furocoumarin, has been successfully used in combination with ultraviolet (UV) A irradiation [psoralen plus UV (PUVA)] to manage psoriasis and vitiligo; inhibit proliferation in the human hepatocellular carcinoma cell line.

Abiraterone

HY-70013

Abiraterone (CB-7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM.

Abiraterone acetate

HY-75054

Abiraterone acetate (CB-7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM.

Bergaptol

HY-76316

Bergaptol
A hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.

Carbosulfan

HY-B2015

Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers).

CDD3505

HY-100901

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

CDD3506

HY-100902

CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

Cecropin B

HY-P0092

Cecropin B can inhibit the expression of CYP3A29.

Chlorzoxazone

HY-B1462

Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort.

Choline Fenofibrate

HY-14739

Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.

Clarithromycin

HY-17508

Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor.

Cobicistat

HY-10493

Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes (Ki=939 nM).

Dafadine-A

HY-16670

Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).

Dihydromethysticin

HY-N0921

Dihydromethysticin is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23.

Fenofibrate

HY-17356

Fenofibrate is PPARα agonist with EC50 of 18 μM and 30 μM for mouse and human PPARα, respectively.

FICZ

HY-12451

FICZ(6-Formylindolo[3,2-b]carbazole) is a tryptophan-derived, high affinity Ah receptor ligand; efficient inducer of CYP1A1 gene expression in short time incubation (0.5 h) experiments.

Galangin

HY-N0382

Galangin is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.

Methoxsalen

HY-30151

Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight.