mTOR Inhibitor III, PP242-Calbiochem

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一般描述

A cell-permeable pyrazolopyrimidine compound that acts as a potent, reversible, and ATP-competitive inhibitor against both mTORC1 & mTORC2 (IC₅₀= 30 & 58 nM, respectively, with 100 ?M 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 ?M (maximum of 68% or 77% inhibition observed with 10 or 100 ?M ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 ?M)in vitroand in mice (20 mg/kg i.p.)in vivoin 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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

Feldman, M.E., et al. 2009.PLoS Biology7,391.
Apsel, B., et al. 2008.Nat. Chem. Biol.4,691.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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安全信息