VER-155008 is an adenosine-derived inhibitor of heat shock protein 70 (Hsp70; IC50 = 0.5 μM) tIt targets the nucleotide-binding domain (NBD) of Hsp70 and similarly binds the NBDs of Hsp70 cognates Hsc70 (Ki = 10 μM) and glucose-regulated protein 78 (Grp78; KD = 80 nM).hat is selective over Hsp90. VER-155008 inhibits the proliferation of human breast and colon cancer cell lines, inducing apoptosis or caspase-independent cell death. It induces the proteasome-dependent degradation of Hsp90 client proteins and potentiates the apoptotic activity of Hsp90 inhibitors.
GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.
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