HSP Modulators: VER-155008

VER-155008 Chemical Structure HSP70 Inhibitors and ModulatorsVER-155008

Heat Shock Protein 70/HSP70 Inhibitor

CAS Number: 1134156-31-2

Molecular Formula: C25H23Cl2N7O4

Molecular Weight: 556.4 g/mol

Research Areas: Cancer Research, Heat Shock, Apoptosis, Cell Signalling

Alternative Names: 4-((((2R,5R)-5-(6-amino-8-((3,4-dichlorobenzyl)amino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)methyl)benzonitrile, 5′-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine

 

Biological Description

VER-155008 is an ATP/adenosine analogue and a competitive Heat shock protein 70 (Hsp70) inhibitor with IC50 of 0.5 uM. It destabilizes oncoproteins, including Raf-1, Her-2, in several cancer cell lines. VER-155008 activates caspase-dependent and independent apoptosis in colon cancer cells. Selectivity for Hsp70 is uncertain as it has been found to bind Hsc70, Grp78, and Hsp90β.

 

References:

  1. Williamson DS, et al. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. J Med Chem. 2009;52(6):1510-3.
  2. Massey AJ, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010;66(3):535-45.