PP242

PP242 is a potent, selective and ATP-competitive small molecule inhibitor of the mammalian target of rapamycin (mTOR), a serine/threonine kinase that regulates cell growth. It inhibits both mTOR complexes, mTORC1 and mTORC2, with IC50 values of 0.03 µM and 0.058 µM, respectively, and is notably more effective at inhibiting mTORC1 than rapamycin. PP242 blocks the phosphorylation of Akt at S473, suppressing mTOR activation and cap-dependent translation. Besides mTOR, PP242 inhibits kinases JAK2, PRKCA, PRKCB (PKCβ I/II), DNAPK, EGFR, and VEGFR2 at higher concentrations, but its principal target is mTOR. It is primarily used in cancer research and cell signaling pathways as a research tool and is not approved for clinical or diagnostic use[1][2][3][9][10].

Other names

2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol