5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine

Uses

VER 155008 is a novel adenosine-derived inhibitor of heat-shocked protein 70, Hsp70 resulting in an inhibition of cell proliferation of human cancer cell lines.

Uses

VER-155008 has been used as a heat shock protein 70 (HSP70) inhibitor:

• to study its effects on human embryonic kidney 293 (HEK293T)?cells
• to study its effects on viral mRNA synthesis and protein expression in Vero E6 cells
• to determine its effects on the attenuation of seizures in rats

Definition

ChEBI: 4-[[(2R,3S,4R,5R)-5-[6-amino-8-[(3,4-dichlorophenyl)methylamino]-9-purinyl]-3,4-dihydroxy-2-oxolanyl]methoxymethyl]benzonitrile is a purine nucleoside.

Biological Activity

ver 155008 is a potent inhibitor of heat shock protein 70 (hsp70) family of chaperones, which have been shown to contribute to cancer cell survival via anti-apoptotic functions, that inhibits hsp70 (with the value of 50% inhibition concentration ic50 of 0.5 μm) as well as heat shock cognate 71 kda protein (hsc70) and 78 kda glucose-regulated protein (grp78) but to a lesser extent. x-ray crystallography analysis reveals that ver 155008 binds to the atpase pocket of hsp70 leading to the inhibition of the intrinsic atpase activity of hsp70. study results also have demonstrated that ver 155008 induces cell proliferation and apoptosis in human cancer cell lines.massey aj, williamson ds, browne h, murray jb, dokurno p, shaw t, macias at, daniels z, geoffroy s, dopson m, lavan p, matassova n, francis gl, graham cj, parsons r, wang y, padfield a, comer m, drysdale mj, wood m. a novel, small molecule inhibitor of hsc70/hsp70 potentiates hsp90 inhibitor induced apoptosis in hct116 colon carcinoma cells. cancer chemother pharmacol. 2010; 66(3): 535-545

Biochem/physiol Actions

VER‐155008 positively promotes memory recovery and axonal regrowth. It is also involved in inhibiting cell cycle progression and proliferation in non-small-cell lung cancer (NSCLC).

storage

Desiccate at RT