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CHIR-98014

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Chemical Structure| 252935-94-7 同义名 : CT98014
CAS号 : 252935-94-7
货号 : A486632
分子式 : C20H17Cl2N9O2
纯度 : 98%
分子量 : 486.314
MDL号 : MFCD10565922
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(24.68 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+corn oil 2 mg/mL

生物活性
靶点

  • GSK-3α

    GSK-3α, IC50:0.65 nM

  • GSK-3β

    GSK-3β, IC50:0.58 nM
描述 GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase, consisting of GSK-3 and subunit, which plays a key role in many different biological processes including tumorigenesis, cell survival, and developmental patterning. GSK-3 is constitutively active in non-stimulated cells and can negatively regulate canonical Wnt/-catenin signaling[2][3]. CHIR-98014 (CT98014) is highly selective aminopyrimidine-derivatived inhibitor of GSK-3 with IC50 of 650nM and 580nM for GSK-3 and GSK-3(measured by kinase assays), respectively, and exhibits >1000-fold selectivity for GSK-3 over closely related kinases, such as cdc2. Exposure of insulin receptor–expressing CHO-IR cells or primary rat hepatocytes to CHIR-98014 can result in a 2-3 fold stimulation of the glycogen synthase activity ratio above basal and the EC50 is 106nM and 107nM for CHO-IR cells and rat hepatocytes, respectively. Diabetic and insulin-resistant db/db mice with subcutaneous administration of 30 mg/kg CHIR-98014 exhibited a significant reduction in fasting hyperglycemia within 4 h, as well as improved glucose tolerance accompanied by reduction of plasma insulin levels[1]. Pre-treatment of 0.6 uM CHIR-98014 for 2 days can induce CD34+CD31+ endothelial progenitor differentiation of 19-9-11 iPSCs cultured on Matrigel in LaSR basal medium before culture in StemPro-34 medium for 3 days[4].
作用机制 CHIR-98014 is competitive inhibitor of ATP binding. [1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.28mL

2.06mL

1.03mL

20.56mL

4.11mL

2.06mL
参考文献

[1]Ring DB, Johnson KW, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.

[2]Martinez A, Castro A, et al. Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation. Med Res Rev. 2002 Jul;22(4):373-84.

[3]Domoto T, Pyko IV, et al. Glycogen synthase kinase-3β is a pivotal mediator of cancer invasion and resistance to therapy. Cancer Sci. 2016 Oct;107(10):1363-1372.

[4]Lian X, Bao X, et al. Efficient differentiation of human pluripotent stem cells to endothelial progenitors via small-molecule activation of WNT signaling. Stem Cell Reports. 2014 Nov 11;3(5):804-16.