PP242 --- mTORC1/mTORC2 inhibitor

Bioss Antibodies

PP242 --- mTORC1/mTORC2 inhibitor [1092351-67-1]

16

Research Use Only

98.0

PP242 is a highly potent, selective and ATP-competitive mTORC1/mTORC2 inhibitor (IC50 = 8 nM). It has > 10 folds selectivity over the other PI-3K family kinases (IC50 0.102 microM, 0.408 microM, 1.27 microM, 1.96 microM and 2.2 microM for p110gamma, DNA-PK, p110delta, p110alpha and p110beta, respectively). Except some weak inhibitory activity against PKCalpha, JAK2, PKCbetaI, PKCbetaII and RET (0.05-0.22 microM), PP242 exhibits excellent selectivity over 215 other protein kinases. PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in vitro and in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1-/- cells or in cultures treated with Rapamycin, which targets only mTORC1, but not mTORC2. Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E, resulting in a selective inhibition of cap-dependent, but not cap-independent, protein translation.

-20°C

51202000