Catalog No.: PC-24668Not For Human Use, Lab Use Only.
BMS-986458 is a potent, highly selective, orally bioavailable CRL4 CRBN E3 ubiquitin ligase-dependent BCL6 ligand directed degrader with CRBN binding IC50 of 41 nM, and BCL-6 degradation of 0.2 nM in OCI-LY-1 cells (2 h).
BMS-986458 is a potent, highly selective, orally bioavailable CRL4 CRBN E3 ubiquitin ligase-dependent BCL6 ligand directed degrader with CRBN binding IC50 of 41 nM, and BCL-6 degradation of 0.2 nM in OCI-LY-1 cells (2 h).
BMS-986458 demonstrates an exquisite selectivity for BCL6 degradation. In a panel of known CRBN neosubstrate assays, no degradation of CK1α, GSPT1, IKZF1, IZKF3, nor SALL4.
BMS-986458 potently exhibits antiproliferative effect against OCI-LY-1 cells with GI50 of 1.2 nM.
BMS-986458 rapidly degrades BCL6 protein to levels that drive broad anti-tumor effects in 80% of BCL6 expressing NHL cell lines and all ex vivo patient derived xenograft (PDX) models evaluated.
