Brief Description

VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 with GI50 of 5.3-14.4 uM in human breast and colon cancer cell lines.
IC50 value: 5.3-14.4 uM(GI50); 80 nM(Kd)
Target: Hsp70 inhibitor
in vitro: VER-155008 inhibited the proliferation of human breast and colon cancer cell lines with GI(50)s in the range 5.3-14.4 microM, and induced Hsp90 client protein degradation in both HCT116 and BT474 cells. As a single agent, VER-155008 induced caspase-3/7 dependent apoptosis in BT474 cells and non-caspase dependent cell death in HCT116 cells. VER-155008 potentiated the apoptotic potential of a small molecule Hsp90 inhibitor in HCT116 but not HT29 or MDA-MB-468 cells. VER-155008 (HCT116 GI50 = 5 μM), has similar potencies in both Grp78 and Hsp70. Inhibition of Hsp70/Hsc70 activity with VER 155008 attenuated the protection afforded by N-acetyl cysteine in a dose-responsive manner.
in vivo: VER-155008 demonstrated rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level.

Solubility

DMSO

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Storage conditions

Store at -20°C 2 years

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