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A-1155463 is a proteolytically stable, cell-permeable and high affinity BH3 mimetic Ligand of BCL protein BCL-XL, binding to the target potently and selectively with a Ki value of <0.01nM (<10 pM), highly selective against closely related proteins of BCL-2 (Ki = 74nM, >7000-fold selectivity), BCL-W (Ki = 8 nM, >800-fold selectivity), and MCL-1 (Ki >444nM, >40000-fold selectivity). A-1155463, together with A-1331852 (Our Prod No: CT-A133), represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity. In living cells, A-1155463, as anticipated, experts an effort to disrupt the tight-binding BCL-XL-BIM, but not BCL-2–BIM, complexes, killing BCL-XL–dependent Molt-4 cells (EC50=70nM) without measurable cytotoxicity against BCL-2–dependent RS4 (ref. 1), inducing the hallmarks of intrinsic apoptosis (ref. 1).
Catalog NO: CT-A115
CAS NO: 1235034-55-5
Mol. Formula: C35H32FN5O4S2
MW: 669.8 (or refer to Certificate of Analysis, batch-specific)
** in vivo quality material, beige powder, clean HPLC (>99.5%) and 1H-NMR (See All QC Docs Attached), Hydrochloride salt, validated by a spot-on Quantitative Microanalysis. Bulk Stock! Prompt.