product name
GSK-3抑制剂XVI，CHIR99021, InSolution, ≥95%, 25 mM
质量水平
检测方案
≥95% (HPLC)
形式
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light
运输
ambient
储存温度
−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
一般描述
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）。
生化/生理作用
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
包装
用惰性气体包装
警告
毒性：刺激性（B）
外形
GSK-3抑制剂XVI，CHIR99021（目录号361559）在DMSO中的25 mM（5 mg/430 µL）溶液。
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
(refers to pure substance)
闪点(°C)
(refers to pure substance)
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