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CHIR99021(CT 99021)

更新时间:2025-08-22 19:20:33

常用名 CHIR-99021 (CT99021) CAS号 252917-06-9
价格 ¥需询单/500mg ¥需询单/1g ¥需询单/5g ¥需询单/10g 纯度 98.0%
备货期 需询单 库存 现货
 产品详情(用途,包装等)
CHIR99021(CT 99021),CAS:252917-06-9

Synonyms: CT99021; CHIR99021; CHIR 99021; CT-99021; GSK-3 Inhibitor XVI; CHIR-99021

Chemical Name: 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile; 6-((2-((4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile
Molecular Formula:C22H18Cl2N8
Molecular Weight: 465.34
Appearance:Light yellow to yellow solid
Purity(HPLC):>98%
Biological Activity:
Potent and highly selective inhibitor of glycogen synthase kinase 3 (GSK-3) (IC50 values are 6.7 and 10 nM for GSK-3β and GSK-3α respectively). Exhibits >500-fold selectivity for GSK-3 over closely related kinases; also displays >800-fold selectivity against 45 additional enzymes and receptors. In combination with tranylcypromine, enables reprogramming of mouse embryonic fibroblasts, transduced by Oct4 and Klf4 only, into iPSCs. Enhances mouse and human ESC self-renewal when used in combination with PD 0325901.

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that plays a key inhibitory role in both the insulin and Wnt signaling pathways. CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. When tested against twenty different protein kinases, this inhibitor shows greater than 500-fold selectivity for GSK3.CHIR99021 activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle.A single oral dose (30 mg/kg) of CHIR99021 enhances in vivo glucose metabolism in a rodent model of type 2 diabetes.CHIR99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells.

Application: 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). CHIR-99021 (CT99021) is a glycogen synthase kinase 3β (GSK3β) inhibitor that has antiproliferative activity in vitro and in vivo. 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.

供应商信息

凯立德生物医药技术(上海)有限公司

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地区: 上海市 上海市 浦东新区
联系人:Chemleader
联系人电话:+8621-58180488
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凯立德生物医药技术(上海)有限公司(Chemleader Biomedical Co., Limited)成立于2010年, 是一家全球领先的科研化学品和生物活性化合物供应商。
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参考价格:$79/10mM*1mLinDMSO
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