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CAS No.: 252935-94-7

CHIR-98014 Catalog No. CSN23355

Synonyms: CT98014;CHIR-98024 isomer;CT-98024 isomer

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.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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]
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0563 mL
- 10.2814 mL
- 20.5628 mL
- 5 mM
- 0.4113 mL
- 2.0563 mL
- 4.1126 mL
- 10 mM
- 0.2056 mL
- 1.0281 mL
- 2.0563 mL

技术信息

CAS号

252935-94-7

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H17Cl2N9O2

运输

蓝冰

分子量

486.31

别名

CT98014;CHIR-98024 isomer;CT-98024 isomer

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

5% DMSO+corn oil

2 mg/mL

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