PP242 has been shown to be a an ATP-competitive FRAP (mTORC1/mTORC2) inhibitor (IC50 = 8 nM). PP242 is the first selective inhibitor that targets the ATP domain of FRAP. This compound shows selectivity for FRAP over other PI 3-kinase (PI 3K family kinases) (IC50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 μM for p110γ, DNA-PK, PI 3-kinase p110δp110δ, p110α and p110β respectively). Furthermore, PP242 hydrate inhibits both S6K and 4EBP1 phosphorylation this activity displays an overall decrease in cap-dependent protein translation. PP242 hydrate is an inhibitor of JAK2 and PKC α. PP242 hydrate is an inhibitor of JAK2, PKC alpha, PKC beta and Ret.
See how others have used PP242 (CAS 1092351-67-1). Click on the entry to view the PubMed entry .
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