Milvexian, also known as BMS-986177 and JNJ-70033093, is a blood coagulation factor XIa inhibitor. Milvexian demonstrated good selectivity over plasma kallikreinKi = 44 nM (400-fold selective), and chymotrypsinKi = 35 nM (318-fold selective). At a dose of 1.5 mg kg, Milvexian exhibited an overall exposure of 1215 nM h, low clearance of 10.3 mL min kg, and oral bioavailability of 32%.
(+)-JQ-1 carboxylic acid is a potent bromodomain and extra terminal domain (BET) inhibitor. (+)-JQ-1 carboxylic has potential to be used as a precursor to synthesize PROTACs and other conjugates.
DK-139 is an inhibitor of NF-kappaB-mediated GROalpha expression, suppressing the TNFalpha-induced invasive capability of MDA-MB-231 human breast cancer cells.