CYP26 Inhibitor

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC₅₀s of 5.4 and 0.46 nM, respectively.

Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC₅₀=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.

Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke.

Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC₅₀=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.

Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC₅₀ of 1.4 μM.

R-116010 is a potent and selective retinoic acid (RA) metabolism inhibitor and can inhibit hydroxylase CYP26. R-116010 can enhance the anti-tumor effect of retinoic acid drugs. R-116010 can be used for the research of cancer, metabolic and neurological disease, such as neuroblastoma.