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Merck
CN

361571

CHIR99021

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

别名:

InSolution GSK-3抑制剂XVI,CHIR99021, 6-(2-(4-(2,4-二氯苯基)-5-(4-甲基-1H-咪唑-2-基)-嘧啶-2-基氨基)乙基-氨基)-烟酰胺腈

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关于此项目

经验公式(希尔记法):
C22H18Cl2N8
化学文摘社编号:
分子量:
465.34
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:
Assay:
≥95% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
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产品名称

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

Quality Level

assay

≥95% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

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

shipped in

ambient

storage temp.

−70°C

SMILES string

Clc1c(ccc(c1)Cl)c2nc(ncc2c4[nH]cc(n4)C)NCCNc3ncc(cc3)C#N

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

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General description

一种细胞可渗透的氨基嘧啶化合物,可作为有效、ATP竞争性和高度选择性的GSK-3抑制剂(对于GSK-3α和GSK-3β,IC50分别为10和6.7 nM)。对46种其他酶几乎没有活性(对于20种激酶,IC50 >8.8 µM,对于23种非激酶,Ki ≥5 µM),并且仅与22种药理学相关受体(Kd ~4 µM)弱结合。该化合物可口服获得,并显示可有效改善体内鼠和大鼠2型糖尿病模型中的葡萄糖代谢。另提供该化合物的固体形式(目录号361559)。

Biochem/physiol Actions

主要靶标
GSK-3 α 和 β
可逆性:是
细胞可渗透性:是
靶标IC50:10和6.7 nM,针对GSK-3&alpha

Packaging

用惰性气体包装

Physical form

GSK-3抑制剂XVI,CHIR99021(目录号361559)在DMSO中的25 mM(5 mg/430 µL)溶液。

Other Notes

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.

Legal Information

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

Disclaimer

毒性:刺激性(B)

存储类别

10 - Combustible liquids

wgk

WGK 2

flash_point_f

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

flash_point_c

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


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货号GTIN
361571-5MG04055977213577

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