Alobresib is an inhibitor of bromodomain and extra-terminal domain (BET) proteins.1,2 It inhibits proliferation of MEC-1 chronic lymphocytic leukemia cells (CLL; IC50 = 46.4 nM).1 Alobresib (400 nM) decreases the levels of Blk and Myc and increases the levels of IκBα in patient-derived CLL cells co-cultured with nurse-like cells (NLC). It inhibits proliferation of USPC-ARK-1 and USPC-ARK-2 uterine serous carcinoma (USC) cells with IC50 values of 31 and 27 nM, respectively.2 Alobresib (10 and 20 mg/kg, p.o.) reduces tumor growth in a USPC-ARK-2 USC mouse xenograft model.
1.Kim, E., Hacken, E.T., Sivina, M., et al.The BET inhibitor GS-5829 targets chronic lymphocytic leukemia cells and their supportive microenvironmentLeukemia34(6)1588-1598(2020) 2.Bonazzoli, E., Predolini, F., Cocco, E., et al.Inhibition of BET bromodomain proteins with GS-5829 and GS-626510 in uterine serous carcinoma, a biologically aggressive variant of endometrial cancerClin. Cancer Res.24(19)4845-4853(2018)