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CAS No.: 252917-06-9

CHIR 99021 Catalog No. CSN13470

Synonyms: CHIR-99021;CT99021;CHIR-911

CHIR-99021 is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM, exhibiting > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 GSK-3α

IC50:10nM GSK-3β

IC50:6.7nM
描述GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase, consisting of GSK-3α andβsubunit, 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/β-catenin signaling. CHIR 99021 （CT99021）is highly selective aminopyrimidine-derivatived inhibitor of GSK-3 with IC50 of 10nM and 6.7nM for GSK-3α and GSK-3β(measured by kinase assays), respectively, and exhibits >500-fold selectivity for GSK-3 over closely related kinases, such as cdc2^[8]Bennett CN, Ross SE, Longo KA, Bajnok L, Hemati N, Johnson KW, Harrison SD, MacDougald OA. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. doi: 10.1074/jbc.M204527200. Epub 2002 Jun 7. PMID: 12055200. https://pubmed.ncbi.nlm.nih.gov/12055200/. CHIR-99021 can mimic Wnt signaling in preadipocytes. Analysis of cytosolic and membranous fractions show that the free cytosolic -catenin was evaluated in 3T3-L1 preadipocytes treated with 3uM CHIR-99021 for 4 h ^[4]. Chir-99021 can activate glycogen synthase in cells. The concentrations of CHIR-99021 causing half-maximal glycogen synthase stimulation (EC50) were 76 nmol/l for CHO-IR cells. A single oral dose of CHIR 99021 (30mg/kg) rapidly lowered plasma glucose in ZDF rats^[8]. In combination with different small molecules, CHIR-99021 can facilitate cardiomyocyte differentiation from human embryonic stem cells and iPS cells^[10]^[9], reprogramming, like generation of functional astrocytes from mammalian fibroblasts^[10] and maintaining undifferentiated mouse ES cells in the absence of LIF^[11].
作用机制CHIR 99021 can inhibit GSK3 by competing for their ATP-binding sites.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human 769-P cell	-	Growth inhibition assay	-	Inhibition of human 769-P cell growth in a cell viability assay, IC50=584.99 nM.	SANGER
human A172 cell	-	Growth inhibition assay	-	Inhibition of human A172 cell growth in a cell viability assay, IC50=3.75498 μM.	SANGER
human A498 cell	-	Growth inhibition assay	-	Inhibition of human A498 cell growth in a cell viability assay, IC50=1.3 μM.	SANGER

更多
动物研究
剂量
Rat^[3] (p.o.): 16 mg/kg - 48 mg/kg

给药途径
p.o.

动物药代数据
Animal Mice^[7]
C_max 15.09 μM
T_1/2 0.87 h
AUC 10.93 μM/kg·h
参考文献

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
- 2.1490 mL
- 10.7448 mL
- 21.4897 mL
- 5 mM
- 0.4298 mL
- 2.1490 mL
- 4.2979 mL
- 10 mM
- 0.2149 mL
- 1.0745 mL
- 2.1490 mL

技术信息

CAS号

252917-06-9

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

C22H18Cl2N8

运输

蓝冰

分子量

465.34

别名

CHIR-99021;CT99021;CHIR-911;CHIR-73911;GSK 3 inhibitor XVI;GSK 3IXV

溶解度

DMSO	127.5 mg/mL (274.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	55 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

human 769-P cell	-	Growth inhibition assay	-	Inhibition of human 769-P cell growth in a cell viability assay, IC50=584.99 nM.	SANGER
human A172 cell	-	Growth inhibition assay	-	Inhibition of human A172 cell growth in a cell viability assay, IC50=3.75498 μM.	SANGER
human A498 cell	-	Growth inhibition assay	-	Inhibition of human A498 cell growth in a cell viability assay, IC50=1.3 μM.	SANGER
human A704 cell	-	Growth inhibition assay	-	Inhibition of human A704 cell growth in a cell viability assay, IC50=3.0812 μM.	SANGER
human ALL-PO cell	-	Growth inhibition assay	-	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=4.83858 μM.	SANGER
human BCPAP cell	-	Growth inhibition assay	-	Inhibition of human BCPAP cell growth in a cell viability assay, IC50=1.67 μM.	SANGER
human BxPC-3 cell	-	Growth inhibition assay	-	Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=4.70391 μM.	SANGER
human COLO-829 cell	-	Growth inhibition assay	-	Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=2.7654 μM.	SANGER
human D-247MG cell	-	Growth inhibition assay	-	Inhibition of human D-247MG cell growth in a cell viability assay, IC50=948.52 nM.	SANGER
human D-336MG cell	-	Growth inhibition assay	-	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=846.2 nM.	SANGER
human GCT cell	-	Growth inhibition assay	-	Inhibition of human GCT cell growth in a cell viability assay, IC50=306.72 nM.	SANGER
human HCC1395 cell	-	Growth inhibition assay	-	Inhibition of human HCC1395 cell growth in a cell viability assay, IC50=1.78 μM.	SANGER
human HCC1569 cell	-	Growth inhibition assay	-	Inhibition of human HCC1569 cell growth in a cell viability assay, IC50=3.48305 μM.	SANGER
human HepG2 cells	-	Function assay	3 h	Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting	22261023
human HOP-62 cell	-	Growth inhibition assay	-	Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=3.36054 μM.	SANGER
human KYSE-180 cell	-	Growth inhibition assay	-	Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=1.73 μM.	SANGER
human LOXIMVI cell	-	Growth inhibition assay	-	Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=588.32 nM.	SANGER
human MHH-ES-1 cell	-	Growth inhibition assay	-	Inhibition of human MHH-ES-1 cell growth in a cell viability assay, IC50=4.04545 μM.	SANGER
human MIA-PaCa-2 cell	-	Growth inhibition assay	-	Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50=1.76 μM.	SANGER
human MOLT-16 cell	-	Growth inhibition assay	-	Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.88556 μM.	SANGER
human NCI-H2122 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=2.28 μM.	SANGER
human NKM-1 cell	-	Growth inhibition assay	-	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=4.13971 μM.	SANGER
human OE19 cell	-	Growth inhibition assay	-	Inhibition of human OE19 cell growth in a cell viability assay, IC50=3.96451 μM.	SANGER
human RCC10RGB cell	-	Growth inhibition assay	-	Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=4.29479 μM	SANGER
human RPMI-7951 cell	-	Growth inhibition assay	-	Inhibition of human RPMI-7951 cell growth in a cell viability assay， IC50=2.7 μM.	SANGER
human RS4-11 cell	-	Growth inhibition assay	-	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=1.95 μM.	SANGER
human S-117 cell	-	Growth inhibition assay	-	Inhibition of human S-117 cell growth in a cell viability assay, IC50=921.31 nM.	SANGER
human SCC-9 cell	-	Growth inhibition assay	-	Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=2.95 μM.	SANGER
human SK-LMS-1 cell	-	Growth inhibition assay	-	Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=2.64 μM.	SANGER
human SK-OV-3 cell	-	Growth inhibition assay	-	Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=4.9934 μM.	SANGER
human SNU-423 cell	-	Growth inhibition assay	-	Inhibition of human SNU-423 cell growth in a cell viability assay， IC50=2.5 μM.	SANGER
human SW1710 cell	-	Growth inhibition assay	-	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=5.42456 μM.	SANGER
human SW982 cell	-	Growth inhibition assay	-	Inhibition of human SW982 cell growth in a cell viability assay, IC50=214.16 nM.	SANGER
human TE-15 cell	-	Growth inhibition assay	-	Inhibition of human TE-15 cell growth in a cell viability assay, IC50=3.95343 μM.	SANGER
human TYK-nu cell	-	Growth inhibition assay	-	Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=1.079 μM.	SANGER

靶点	Description	IC50
GSK-3α		IC50:10nM
GSK-3β		IC50:6.7nM

CHIR 99021 Catalog No. CSN13470

靶点选择性

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