Description
InformationBDA-366 is a small-moleculeBcl2-BH4domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).TargetsBcl2-BH4 (Cell-free assay) 3.3 nM(Ki)In vitroBDA-366 induces robust apoptosis in MM(Multiple myeloma) cell lines and primary MM cells by inducing BCL2 conformational change. BDA-366 induces a conformational change in the BCL2 molecule that converts it to a death protein, and inhibits lung cancer growth in vitro and in vivo. BDA-366 did not bind to other Bcl2 family members, including Bcl-XL, Mcl-1, or Bfl-1/A1, indicating the specificity of its Bcl2 binding. BDA-366 induces apoptotic cell death in a Bax-dependent manner and induces calcium (Ca2+) release via inhibition of Bcl2/IP3R interaction.In vivoDelivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγ mice, without significant cytotoxic effects on normal hematopoietic cells or body weight. Also, BDA-366 suppresses lung cancer growth via induction of apoptosis in animal models. The BH4 antagonist BDA-366 exhibits potent efficacy against human lung cancer in vivo without platelet reduction.Cell Research(from reference)Cell lines：human MM RPMI8226 and U266 cell lines Concentrations：0, 0.1, 0.25, 0.5 µM Incubation Time：48 h