mTOR Inhibitor III, PP242 - Calbiochem 化学特性,用途語,生産方法
一般的な説明
A cell-permeable pyrazolopyrimidine compound that acts as a potent, reversible, and ATP-competitive inhibitor against both mTORC1 & mTORC2 (IC
50 = 30 & 58 nM, respectively, with 100 μM ATP). PP242 inhibits PKCα, p110γ, and JAK2 with 6-, 13-, and 14-fold less potency and exhibits much reduced or no activity against a panel of 216 other kinases at a concentration of 1 μM (maximum of 68% or 77% inhibition observed with 10 or 100 μM ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 μM)
in vitro and in mice (20 mg/kg i.p.)
in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1
-/- cells or in cultures treated with Rapamycin (Cat. Nos.
553210,
553211,
553212), 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.
mTOR Inhibitor III, PP242 - Calbiochem 上流と下流の製品情報
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