Catalog No.: PC-73076Not For Human Use, Lab Use Only.
DDO-5936 (DDO5936) is a cell-active, specidic small-molecule inhibitor of Hsp90-Cdc37 protein-protein interaction (PPI) without ATPase inhibition, binds to Hsp 90 with Kd of 3.86 uM.
DDO-5936 (DDO5936) is a cell-active, specidic small-molecule inhibitor of Hsp90-Cdc37 protein-protein interaction (PPI) without ATPase inhibition, binds to Hsp90 with Kd of 3.86 uM.
DDO-5936 exhibits little effect on Hsp90 ATPase activity, DDO-5936 targets a surface binding site on Hsp90 to inhibit the Hsp90-Cdc37 PPI.
DDO-5936 binding affinity was remarkably decreased for the E47A mutant (KD> 100 μM) and moderately lower for the R46A mutant (KD =6.53 μM) and Q133A mutant (KD=5.18 μM).
DDO-5936 represses cell proliferation through a strong correlation with the Hsp90-Cdc37 expression level, and selectively down-regulates kinase clients of Hsp90, arrests the cell cycle in HCT116 cells in a Cdc37-dependent manner.
DDO-5936 (50-100 mg/kg, ip) dose-dependently impairs the growth of xenografted HCT116 cells in nude mice.
