475988
mTOR Inhibitor III, PP242
The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonyme(s) :
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
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About This Item
Formule empirique (notation de Hill):
C16H16N6O · 2H2O
Poids moléculaire :
344.37
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produits recommandés
Niveau de qualité
Pureté
≥97% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
off-white
Solubilité
DMSO: 100 mg/mL
Conditions d'expédition
wet ice
Température de stockage
−20°C
Description générale
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 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.
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Autres remarques
Feldman, M.E., et al. 2009. PLoS Biology7, 391.
Apsel, B., et al. 2008. Nat. Chem. Biol.4, 691.
Apsel, B., et al. 2008. Nat. Chem. Biol.4, 691.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 2
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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