Catalog No.S7458 Synonyms: CCT0129397
Molecular Weight(MW): 387.82
VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
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|Description||VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.|
VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-49009 causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis.  VER-49009 inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis. 
|In vivo||In athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, VER-49009 (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2. |
Fluorescence Polarization Assay:Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.
|In vitro||DMSO||77 mg/mL (198.54 mM)|
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