VER-50589 (VER50589) is a potent, selective small-molecule inhibitor of Hsp90 with IC50 of 21 nM and Kd value of 4.5 nM.
Cellular uptake of VER-50589 was 4-fold greater than for VER-49009.
VER-50589 caused significant reduction in cellular levels of Raf-1, and the client protein CDK4.
VER-50589 caused induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5.
VER-50589 exhibited mean cellular antiproliferative GI(50) values of 78 nM against a human cancer cell line panel, induced cell cycle arrest and apoptosis.
VER-50589 induced growth inhibition in HCT116 human colon cancer xenografts
