VER-49009

VER-49009 is a Hsp90 inhibitor, with an IC₅₀ of 25 nM and a K_d of 78 nM. IC50 & Target: IC50: 25 nM (Hsp90)^[1]
Kd: 78 nM (Hsp90)^[2] In Vitro: VER-49009 is a Hsp90 inhibitor, with an IC₅₀ of 25 nM. VER-49009 binds to the ATPase of full length yeast Hsp90 protein, with an IC₅₀ of 140 nM^[1]. VER-49009 inhibits Hsp90, with a K_d of 78 nM. VER-49009 also shows antiproliferative activities against various human cancer cells, with a mean GI₅₀ of 685 ± 119 nM. VER-49009 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI₅₀ values of 444 ± 91.1 nM, and shows higher GI₅₀s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. VER-49009 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression^[2]. VER-49009 inhibits the proliferation (1, 2.5 μM), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 μM)^[3]. In Vivo: VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with client protein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors^[2].