Creative Biolabs

CHIR 99021 [GSK3 Inhibitor]

[CAT#: MOD2005ZP76]

A highly potent, selective GSK3 inhibitor. Wnt signaling activator.

Target:
GSK-3

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Description
Efficient, selective and ATP competitive GSK-3 inhibitors (IC50 values of GSK-3β and GSK-3α are 6.7 and 10 nM, respectively). Wnt signal activator, commonly used with PD 032501 as part of the 2i condition. No cross-reactivity to CDK, selectivity to GSK3 is> 500 times higher than other protein kinases, and selectivity to 20 other enzymes and receptors is> 800 times higher. Promote the self-renewal of embryonic stem cells and reprogram mouse embryonic fibroblasts (MEF) to iPSC.
Synonyms
CHIR99021
Chemical Name
6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5 -methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
The Ki value of CHIR-99021 inhibiting human GSK-3β is 9.8 nM [1]. CHIR-99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for its ATP binding site. In vitro kinase assays showed that CHIR-99021 specifically inhibits GSK3β (IC50 = ~5 nM) and GSK3α (IC50 = ~10 nM), with little effect on other kinases [4]. In the presence of CHIR-99021, the viability of ES-D3 cells decreased by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM, 69.2% at 10 μM, and IC50 at 4.9 μM [2].
Reference
[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.

[2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273.
Assay Description
In ZDF rats, a single oral dose of CHIR-99021 (16 mg/kg or 48 mg/kg) can rapidly reduce plasma glucose, with a maximum reduction of nearly 150 mg/dl at 3-4 hours after administration [1]. Give CHIR99021 (2 mg/kg) once 4 hours before radiation, which can significantly improve the survival rate after 14.5 Gy abdominal radiation (ABI). CHIR99021 treatment can significantly block crypt apoptosis and p-H2AX + cell accumulation, and improve crypt regeneration and villi height. CHIR99021 therapy can improve the survival rate of Lgr5 + cells by blocking apoptosis and effectively prevent the reduction of Olfm4, Lgr5 and CD44 within 4 hours [2].
References
[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.

[2]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.
Molecular Weight
465.34
Form
Powder
Chemical Formula
C22H18Cl2N8
Source
Synthetic
SMILES
CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N
Solubility
Soluble in DMSO (20mM)
IC50
GSK-3β-6.7 nM (IC50); GSK-3α-10 nM (IC50); cdc2-8800 nM (IC50)
CAS NO.
252917-06-9
PubChem Substance ID
9956119
Purity
>98%
Storage
-20°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -30°C for several months.
Research Use Only
For research use only
Target
GSK-3
Official Name
GSK-3
Full Name
Glycogen synthase kinase 3
Alternative Names
Glycogen Synthase Kinase 3; GSK3; Glycogen Synthase Kinase-3
Gene ID
2932(Human); 56637(Mouse); 84027(Rat)
Uniprot ID
P49841(Human); Q9WV60(Mouse); P18266(Rat)

For Research Use Only. Not For Clinical Use.
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