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| 中文名: | 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]吡啶-3-甲腈;6-((2-((4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)嘧啶-2-基)氨基)乙基)氨基)烟腈 |
| 中文别名: | CT99021;CHIR99021;CHIR 99021;CT-99021; 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]吡啶-3-甲腈 |
| 英文名称： | CHIR-99021(CT99021) |
| 英文别名： | CT99021;CHIR99021;CHIR 99021;CT-99021;6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile |
| CAS No.: | 252917-06-9 |
| 分子式: | C22H18Cl2N8 |
| 分子量: | 465.34 |
| 性状: | 属性溶解性Soluble in DMSO (10 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C., Soluble in DMSO (10 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.存贮条件储存温度-20°C描述产品介绍CHIR-99021 (CT99021)是GSK-3α和β抑制剂，IC50分别为10 nM和6.7 nM，比对CDC2，ERK2及其他激酶的抑制性强500倍。用途A compound that acts as potent, ATP-competitive & highly selective GSK-3 inhibitor生化机理GSK-3 Inhibitor XVI is 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). CHIR99021 exhibits little to 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). |
| 储存: | 储存温度-20°C |
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| 用途: | CHIR-99021(CT99021) is a glycogen synthase kinase 3β (GSK3β) inhibitor that has antiproliferative activity in vitro and in vivo. [1] CHIR-99021 inhibits GSK-3 with IC50 at 7 nM. In a series of carcinoma cell lines, the IC50 of CHIR99021 for proliferation is about 10μM. [1] CHIR-99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) with 350-fold selectivity toward GSK-3β compared to CDKs . [1] |
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