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Merck
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Key Documents

528117

Sigma-Aldrich

PI 3-K inhibitor IX, PIK-90

The PI 3-K inhibitor IX, PIK-90, also referenced under CAS 677338-12-4, controls the biological activity of PI 3-K. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

동의어(들):

PI 3-K inhibitor IX, PIK-90, N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI

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About This Item

실험식(Hill 표기법):
C18H17N5O3
CAS Number:
Molecular Weight:
351.36
UNSPSC 코드:
12352200

Quality Level

분석

≥98% (HPLC)

형태

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

pale yellow

solubility

DMSO: 0.5 mg/mL

배송 상태

wet ice

저장 온도

−20°C

일반 설명

A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

제조 메모

Slight warming may be required to for complete solubility.

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Fan, Q.W., et al. 2007. Cancer Res.67, 7960.
Fan, Q.W., et al. 2006. Cancer Cell9, 341.
Knight, Z.A., et al. 2006. Cell125, 733.

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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Keishi Kishimoto et al.
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