umi-77

Description: UMI-77 (UMI 77; UMI77) is a novel, potent and selective Mcl-1 (Myeloid cell leukemia-1) inhibitor with Ki of 490 nM. Myeloid cell leukemia-1 (Mcl-1) is a member of the prosurvival Bcl-2 family and is a potent anti-apoptotic protein. Mcl-1 acts as an important survival factor in a broad range of human cancers. As a small-molecule Mcl-1 inhibitor, UMI-77 potently and selectively displaced fluorescent labeled BID-BH3 peptide from Mcl-1 protein in FP-based binding assays, with Ki value of 0.49uM and bound to the BH3 binding pocket of Mcl-1 protein. UMI-77 bound to A1/Bfl-1, Bcl-w, Bcl-2 and Bcl-xL with Ki values of 5.33, 8.19, 23.83 and 32.99uM. In a pull-down assay, UMI-77 at 10 uM effectively and dose-dependently inhibited the interactions between BL-Noxa and cellular Mcl-1.

Reference: Mol Cancer Ther. 2014 Mar; 13(3):565-75.