hsp90-cdc37

Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor (IC50: 140 nM) that inhibits cell migration and reverses drug resistance.

Hsp90-Cdc37-IN-4 is a novel derivative of triptolide that inhibits the protein-protein interaction (PPI) between Hsp90 and Cdc37. It selectively inhibits casein kinase 2 (CK 2), reducing the phosphorylation of its substrate Cdc37 at the serine 13 site. Additionally, Hsp90-Cdc37-IN-4 induces cell cycle arrest in the G0/G1 phase and triggers apoptosis via the mitochondrial pathway. This compound exhibits significant anti-breast cancer activity.

DDO-6079 is an efficient CDC37 inhibitor. It suppresses the HSP90-CDC37 and CDC37-CDK4/6 chaperone complexes by binding to an allosteric site on CDC37. Additionally, DDO-6079 reduces the thermal stability of CDK6.

CAY10747 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) and a derivative of celastrol .1It decreases protein levels of the Hsp90-Cdc37 complex and the Hsp90-Cdc37 clients phosphorylated Akt and Cdk4 in A549 cells when used at a concentration of 5 μM. CAY10747 inhibits proliferation of A549, MCF-7, HOS, and HepG2 cells (IC50s = 0.41, 0.64, 0.9, and 0.94 μM, respectively) and induces apoptosis in A549 cells. 1.Li, N., Xu, M., Wang, B., et al.Discovery of novel celastrol derivatives as Hsp90-Cdc37 interaction disruptors with antitumor activityJ. Med. Chem.62(23)10798-10815(2019)

DDO-5936 is a potent and specific inhibitor of the protein-protein interaction (PPI) between HSP90 and Cdc37.