VER-50589

VER-50589 is a Hsp90 inhibitor, with an IC₅₀ of 21 nM and a K_d of 4.5 nM. IC50 & Target: IC50: 21 nM (Hsp90)^[1]
Kd: 4.5 nM (Hsp90)^[1] In Vitro: VER-50589 is a Hsp90 inhibitor, with an IC₅₀ of 21 nM and a K_d of 4.5 nM. VER-50589 inhibits intrinsic ATPase of full-length recombinant yeast Hsp90, with an IC₅₀ of 143 ± 23 nM in the presence of 400 μM ATP. VER-50589 shows antiproliferative activities against various human cancer cells, with the lowest GI₅₀ of 32.7 ± 0.2 nM for CH1 human ovarian cells, and mean GI₅₀ of 78 ± 15 nM. VER-50589 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI₅₀ value of 19 ± 2.4 nM, and shows higher GI₅₀s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. Furthermore, VER-50589 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-50589 also causes G1 and G2-M block (115 or 575 nM) and induces cytostasis in HCT116 colon cancer cells. In addition, VER-50589 causes great uptake in HCT116 cells^[1]. In Vivo: VER-50589 (4 mg/kg, i.p.) exerts a complete HSP90 inhibition in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors. VER-50589 (100 mg/kg, i.p.) shows reduced tumor volume and tumor weights in the HCT116 colon carcinoma xenografts compared to the control mice group^[1].