S55746

S55746 is a novel orally active small molecule that acts as a potent and selective inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2). By binding to and inhibiting Bcl-2 activity in tumor cells—particularly hematological malignancies such as chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL)—S55746 restores apoptotic processes that are often impaired in cancer. Mechanistically classified as a BH3-mimetic compound or apoptosis stimulant/proto-oncogene protein c-bcl-2 inhibitor, it induces apoptosis by releasing pro-apoptotic proteins like BIM from sequestration by Bcl-2. This leads to activation of the intrinsic apoptotic pathway via caspase processing and PARP cleavage. The drug has demonstrated significant anti-tumor activity in preclinical models and early-phase clinical trials[1][3][6][8].

Other names

(S)-N-(4-hydroxyphenyl)-3-(6-(3-(morpholinomethyl)-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)benzo[d][1,3]dioxol-5-yl)-N-phenyl-5,6,7,8-tetrahydroindolizine-1-carboxamide