PROTAC Mcl1 degrader-1

Description: PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with µM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 µM. Target: BCL, PROTACs. Smiles: O=C1NC(=O)C(N2C(=O)C=3C=CC=C(NCCCCCCNC(=O)CCCCC(=O)NCCN4C(=O)C5=CC=CC=6C(SC7=CC=C(Br)C=C7)=CC=C(C4=O)C56)C3C2=O)CC1. References: Wang Z, et al. Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands. J Med Chem. 2019 Aug 21.