I-BET282

I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD)^[1]. In Vitro: I-BET282 has a weak inhibition of the hERG potassium ion channel (pIC₅₀ 4.4-5.1 in a variety of assay formats). I-BET282 shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4^[1]. In Vivo: I-BET282 (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Cl_b, LBF, Vss, t_1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively. I-BET282 (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC_0-t, C_max and T_max values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively^[1].