In vitro activity: MSDC-0160 reduces resistance in the insulin/IGF-1 signaling pathway and restores IGF-1-induced Akt and GSK-3 phosphorylation. MSDC-0160 in combination with IGF-1 and 8 mM glucose increases β-cell specific gene expression of insulin, pdx1, nkx6.1, and nkx2.2, and maintains insulin content without altering glucose-stimulated insulin secretion. Furthermore, MSDC-0160 promotes human β-cell differentiation and reduces the expression of markers of apoptosis.
Kinase Assay: MSDC-0160 at 50μM alone also prevents the loss of insulin content significantly. Besides that, treatment of MSDC-0160 increases the phosphorylation of AMPK and reduces mTOR phosphorylation. Moreover, MSDC-0160 is also found to display pro-survival effects in human islets via reducing the level of cleaved caspase-3 and increasing the expression of apoptosis-related genes such as bcl2.
Cell Assay: MSDC-0160 exerts prevention of nuclear translocation with β-catenin localized on the cell membrane or cytoplasm in human β-cells | 
