PP 242

A potent, specific active-site inhibitor of mTOR with IC50 of 30 and 58 nM for mTORC1 and mTORC2, respectively; shows no activity against PKC-β, RET, or JAK2 but inhibits PKC-α (IC50=50 nM) ; blocks the phosphorylation of Akt at S473 and prevents its full activation, inhibits proliferation of primary cells more completely than rapamycin.