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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
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
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.
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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全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 361571-5MG | 04055977213577 |
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