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Sigma-Aldrich

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.

Synonim(y):

2-(4-amino-1-izopropylo-1H-pirazolo[3,4-d]pirymidyn-3-ylo)-1H-indol-5-ol, dihydrat, TORKinib, inhibitor mTOR III, PP242

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About This Item

Wzór empiryczny (zapis Hilla):
C16H16N6O · 2H2O
Masa cząsteczkowa:
344.37
Kod UNSPSC:
12352200
NACRES:
NA.77
Informacje o cenach i dostępności nie są obecnie dostępne.

Poziom jakości

Próba

≥97% (HPLC)

Formularz

solid

producent / nazwa handlowa

Calbiochem®

warunki przechowywania

OK to freeze
protect from light

kolor

off-white

rozpuszczalność

DMSO: 100 mg/mL

Warunki transportu

wet ice

temp. przechowywania

−20°C

Opis ogólny

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.

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Inne uwagi

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

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 2

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable


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