mTOR Inhibitor III, PP242 – Calbiochem

Descrição detalhada : 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 µM ATP). PP242 inhibits PKCalpha, p110gamma, 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.
Sinónimos : mTOR Inhibitor III, PP242 - Calbiochem; 2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242; 2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242
Fórmula molecula r: C16H16N6O · 2H2O
Armazenamento : -20C
Embalagem : 1X5MG