UCL-TRO-1938 is a selective allosteric activator of PI3Kα with an EC50 value of ~60 μM (assessed by in vitro lipid kinase activity). The EC50 values on cells are shown to be 2-4 μM and 5 μM to stimulate downstream AKT phosphorylation and increase PIP3, respectively. In MEF cells, UCL-TRO-1938 shows an EC50 of 0.5 μM to increase ATP levels over 24 h. UCL-TRO-1938 transiently activates PI3K signalling in all rodent and human cells tested, resulting in cellular responses such as proliferation and neurite outgrowth. In rodent models, acute treatment with UCL-TRO-1938 provides cardioprotection from ischaemia reperfusion injury and, upon local administration, enhances nerve regeneration following nerve crush.

Keywords: UCL-TRO-1938 | Supplier | PI3Kα activator | UCL-TRO 1938 | UCL-TRO1938 | CAS [2919575-27-0] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | Cardioprotection | Neuroregeneration | Growth factor signalling