Birabresib, also known as OTX015 and MK-8628, a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD2/3/4). BRDs 2, 3, and 4 are considered potential cancer targets because of their pivotal role in regulating the transcription of growth-promoting genes and cell cycle regulators. OTX015 is the first BRD2/3/4 inhibitor to enter clinical trials. OTX015 showed antiproliferative activity in a large panel of cell lines derived from mature B-cell lymphoid tumors with median IC50 of 240 nmol/L, without significant differences among the different histotypes.
Epigenetic Reader Domain Inhibitors Related Products:
ICG-001; (+)-JQ1; I-BET151; PFI-1; Molibresib; Apabetalone; C646; Curcumin; Bromosporine; UNC1215; GSK6853; CPI-637; BI-9564; PFI-4; XMD8-92; MS436; CPI-203; KG-501; Mivebresib; GSK2801