Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Cytochrome P450 (CYP) inhibitors act on heme enzymes that oxidize drugs, steroids and other lipophilic compounds. The name comes from the 450 nm absorption peak of a carbon monoxide-bound pigment, described in liver microsomes in 1964. Hepatic enzymes such as CYP3A4, CYP2C9 and CYP1A2 metabolize a large share of drugs and many environmental chemicals. Other members synthesize steroid hormones, among them CYP17A1, which is required for androgen production. The P450 system can also convert chemicals into toxic or carcinogenic metabolites, which links it closely to toxicology. Abiraterone inhibits CYP17A1, while clarithromycin and itraconazole serve as CYP3A4 inhibitors in drug-interaction studies. Alizarin is listed for its inhibition of enzymes in the CYP1 family.
Synonyms: Vfend; Pfizer
Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion.
Synonyms: TAK700
TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme.
Synonyms: CB-7630
Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1).
Synonyms: VN/124-1; TOK-001
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.
Synonyms: GS9350
Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate.
Synonyms: E)-2,3',4,5'-tetramethoxystilbene
TMS is a potent, selective and competitive inhibitor of cytochrome P450 1B1, an enzyme overexpressed in certain tumors (IC50= 6 nM). 5N/A- and 520-fold selective over P450 1A1 and 1A2 respectively.
Synonyms: 5-Hydroxypsoralen; 4-Hydroxybergapten
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
Synonyms: PF4981517
PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively).
CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
Synonyms: R115866; Rambazole
Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase.
Synonyms: TAK 700
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.
Synonyms: FYX-051,FYX051; FYX 051
Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.
Synonyms: 5-Methoxypsoralen
Bergapten is a natural compound that acts as an inhibitor of cytochrome P450 isoforms in both mouse and human systems. It exhibits anti-inflammatory and anti-tumor properties, making it a valuable tool for studying metabolic processes and evaluating therapeutic strategies in cancer research and inflammation-related studies. Its ability to modulate CYP activity underscores its relevance in pharmacological investigations and toxicology assessments.
Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA.
Synonyms: ABT-335
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.
Synonyms: DMP 266; EFV; L-743726; L-743,726
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
Synonyms: L2214
Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
Synonyms: DBT; Diphenylene sulfide
Dibenzothiophene is a noncompetitive inhibitor of cytochrome P450 1A (CYP1A), effectively inhibiting CYP1A-mediated ethoxyresorufin O-deethylation (EROD) activity with a Km value of 0.592 μM. This compound interacts with the aryl hydrocarbon receptor (AHR) pathway and has been shown to enhance the embryotoxicity of β-naphthoflavone. Its acute toxicity in animal models underscores its relevance in research. Dibenzothiophene is primarily utilized in studies investigating the mechanisms of developmental toxicity in various organisms.
Bergamottin is a furanocoumarin found in grapefruit juice and lemon, lime, and bergamot oils that has diverse biological activities.
Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi.
Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM.
Synonyms: BRN-0308518; Firmazolo; Inamil
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
Synonyms: Proadifen hydrochloride; NSC 170997
Proadifen hydrochloride is a Cytochrome P450 inhibitor (IC50 = 19μM).
EMT inhibitor-2 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.
Synonyms: VT-1129
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
