Catalog No.: PC-43340Not For Human Use, Lab Use Only.
I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF).
I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF).
I-BET762 inhibits binding of BET proteins to acetylated histones, disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, suppresses TNF-inducible key proinflammatory cytokine (il1b, il1a) and chemokine genes (ccl5, cxcl10, cxcl2/3) in BMDMs.
I-BET762 inhibits the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in vivo in mouse model of EAE.
I-BET762 inhibits myeloma cell proliferation both in vitro and myeloma xenograft models.
