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Merck
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Key Documents

475988

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.

동의어(들):

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

실험식(Hill 표기법):
C16H16N6O · 2H2O
Molecular Weight:
344.37
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥97% (HPLC)

형태

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

off-white

solubility

DMSO: 100 mg/mL

배송 상태

wet ice

저장 온도

−20°C

일반 설명

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.

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

기타 정보

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

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Rikke Illum Høgh et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 34(11), 15531-15546 (2020-10-01)
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