产品描述:
UCL-TRO-1938 is an allosteric activator of PI3Kα.{65710} It binds to PI3Kα in a surface plasmon resonance (SPR) assay (Kd = 36 µM) and induces PI3Kα activation in a cell-free assay when used at concentrations of 25 and 50 µM, an effect that can be reversed by the PI3Kα inhibitor BYL719 (Item No. 16986). UCL-TRO-1938 increases PtdIns-(3,4,5)-P3 and phosphorylated Akt levels in mouse embryonic fibroblasts (MEFs; EC50s = 5 and 2-4 µM, respectively). Ex vivo, UCL-TRO-1938 increases tissue survival and decreases infarct size in perfused rat hearts. In vivo, UCL-TRO-1938 (10 mg/kg) reduces infarct size in a mouse model of ischemia-reperfusion injury induced by left anterior descending (LAD) coronary artery occlusion. It also increases the number of motor neurons and innervation of neuromuscular junctions in a rat model of sciatic nerve crush injury.