CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes.
CYP1B1-IN-4 (compound 15) (100 μM; 37 ℃; 0-60 min) has in vitro stability in both human and rat liver microsomes, while it has low stability in mouse liver microsomes[1].CYP1B1-IN-4 (1 nM-10 μM) also inhibits CYP1A1 with an IC50 value of 3.82 μM[1].CYP1B1-IN-4 (200 μM; 72 h) parental HEK T-REx cell line , and (100 μ M; 72 h) has little cytotoxicity in HEK293 cells[1].Stability Parameters in Human, Rat, or Mouse Liver Microsomes[1]
References:
[1]. Hachey AC, et al. Design of Cytochrome P450 1B1 Inhibitors via a Scaffold-Hopping Approach. J Med Chem. 2022 Dec 15.