S63845

Description

S63845 is an inhibitor of myeloid cell leukemia 1 (Mcl-1; K_i = 0.19 nM), a pro-survival protein that is overexpressed in many cancers. It induces cell death in multiple myeloma, leukemia, and lymphoma cell lines (IC₅₀s = <0.1-282 nM) via mitochondrial apoptosis. S63845 acts synergistically with trametinib , lapatinib , PLX4032 , and erlotinib to reduce proliferation of SK-MEL-2, BT474, A2058, and PC9 cells, respectively. S63845 (6.25-25 mg/kg) reduces tumor volume in an MV4-11 acute myeloid leukemia mouse xenograft model in a dose-dependent manner.

Uses

S-63845 is used in killing senescent cells and treating senescence-associated diseases or disorders using a combination of a BCL inhibitor and an MCL-1 inhibitor.Potent and selective MCL1 inhibitor