BAY-958

BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1; displays 52/82/291/>900/>900-fold selectivity compared to CDK2/1/4/6/7; exhibits good antiproliferative activity in vitro, for example against HeLa cells (IC50=1000 nM) and MOLM-13 cells (IC50=280 nM); displays efficient cytotoxic activity against CLL cells in vitro, decreases CLL MCL-1 protein levels and triggers apoptosis rather than inhibiting proliferation; decreases splenic human CLL numbers in xenografted NSG mice, shows significant CLL cell cytotoxicity in TCL1 transgenic mice.

References 1. Lücking U, et al. ChemMedChem. 2017 Nov 8;12(21):1776-1793. 2. Göthert JR, et al. Oncotarget. 2018 May 29;9(41):26353-26369. View Related Products by Target Cyclin-dependent Kinase (CDK)