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Merck

361571

Sigma-Aldrich

CHIR99021

≥95% (HPLC), liquid, GSK-3 inhibitor, Calbiochem

別名:

InSolution GSK-3 Inhibitor XVI, CHIR99021, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile

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About This Item

実験式(ヒル表記法):
C22H18Cl2N8
CAS番号:
分子量:
465.34
MDL番号:
UNSPSCコード:
12352200
NACRES:
NA.28

製品名

GSK-3 Inhibitor XVI, CHIR99021, InSolution, ≥95%, 25 mM

品質水準

アッセイ

≥95% (HPLC)

フォーム

liquid

メーカー/製品名

Calbiochem®

保管条件

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

輸送温度

ambient

保管温度

−70°C

InChI

1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32)

InChI Key

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

詳細

A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo. The solid form of this compound (Cat. No. 361559) is also available.

生物化学的/生理学的作用

Cell permeable: yes
Primary Target
GSK-3 α and β
Reversible: yes
Target IC50: 10 and 6.7 nM against GSK-3&alpha

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

物理的形状

A 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.

その他情報

Mussmann, R., et al. 2007. J. Biol. Chem.282, 12030.
Ring, D.B., et al. 2003. Diabetes52, 588.
Bennett, C.N., et al. 2002. J. Biol. Chem.277, 30998.
Cline, G.W., et al. 2002.
Diabetes51, 2903.

法的情報

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

保管分類コード

10 - Combustible liquids

WGK

WGK 2

引火点(°F)

188.6 °F - closed cup - (refers to pure substance)

引火点(℃)

87 °C - closed cup - (refers to pure substance)


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

毒物及び劇物取締法

劇物

消防法

第4類:引火性液体
第三石油類
危険等級III
非水溶性液体

労働安全衛生法名称等を表示すべき危険物及び有害物

名称等を表示すべき危険物及び有害物

労働安全衛生法名称等を通知すべき危険物及び有害物

名称等を通知すべき危険物及び有害物

Jan Code

361571-5MG:


試験成績書(COA)

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Wnt signaling plays important roles in development, homeostasis, and tumorigenesis. Mutations in β-catenin that activate Wnt signaling have been found in colorectal and hepatocellular carcinomas. However, the dynamics of wild-type and mutant forms of β-catenin are not fully understood. Here
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Currently, there are no treatments that ameliorate cardiac cell death, the underlying basis of cardiovascular disease. An unexplored cell type in cardiac regeneration is cardiac Purkinje cells; specialized cells from the cardiac conduction system (CCS) responsible for propagating electrical signals.
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The Wnt/β-catenin pathway is a highly conserved, frequently mutated developmental and cancer pathway. Its output is defined mainly by β-catenin's phosphorylation- and ubiquitylation-dependent proteasomal degradation, initiated by the multi-protein β-catenin destruction complex. The precise mechanisms underlying destruction complex function have

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