S63845 is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM, with no appreciable binding affinity to BCL-2 or BCL-XL (Ki>10 uM).
S63845 binds to the BH3-binding groove of Mcl-1.
S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma (IC50<0.1 uM), leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway.
S63845 is well tolerated and shopws high effectivity against mouse cancer models.
