Drug intelligence / Profile preview

VER-155008

Development stage
Preclinical
Lead developer
Vernalis
Modality
Small Molecules
Administration
Intraperitoneal (preclinical Animal Studies)[5], Not Established For Human Use
01

Overview

VER-155008 is a potent small molecule inhibitor of the heat shock protein 70 (Hsp70) family of molecular chaperones. It is an adenosine-derived compound that binds to the ATPase pocket of Hsp70 and inhibits its intrinsic ATPase activity. VER-155008 exhibits high affinity for Hsp70 (IC50 = 0.5 μM), as well as inhibitory activity against heat shock cognate 71 kDa protein (Hsc70) and glucose-regulated protein 78 kDa (Grp78), though with lower potency for these targets[1][2][3]. The inhibition of Hsp70 disrupts its anti-apoptotic functions in cancer cells and leads to reduced cell proliferation and increased apoptosis in various tumor cell lines including colon, breast cancer[1], and non-small-cell lung cancer[4]. In preclinical studies, it has also shown potential neuroprotective effects by reducing memory deficits and axonal degeneration in mouse models of Alzheimer's disease[5].

Other names
4-[[(2R,3S,4R,5R)-5-[6-amino-8-[(3,4-dichlorophenyl)methylamino]purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxymethyl]benzonitrile
02

Targets

HSPA8 (Heat shock cognate 71 kDa protein)Hsp70 (70 kDa heat shock protein)HSPA5 (Heat shock protein family A member 5)

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