SNX-2112

SNX-2112 is a potent synthetic heat shock protein 90 inhibitor with an IC50 of 0.92 μM for K562 cells. The heat shock protein 90 (Hsp90) chaperone not only regulates the conformational maturation but also stables the structures of oncogenic kinases as well as transcription factors. SNX-2112 is an active metabolite of the compounds SNX-5542. SNX-2112 is rapidly transformed form SNX-5542 after administration. In a panel of tumor cell lines, SNX-2112 degraded HER2 and mutant epidermal growth factor receptor and inhibited extracellular signal-modulated kinase and Akt activation.SNX-2112 inducen a Rb-dependent G1 arrest with subsequent apoptosis. which accumulates in tumors relative to normal tissues.