CHIR99021 is a glycogen synthase kinase 3β (GSK3β) inhibitor with IC50 less than 10 nM(1,2). Compared to other GSK-3 inhibitors, CHIR-99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) with 350-fold selectivity toward GSK-3β compared to CDKs. Inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ) (3). Together with mitogen-activated protein kinase inhibitor, CHIR99021 enables the self-renewal of embryonic stem cells(2).

CAS Number 252917-06-9

Chemical Formula C₂₂H₁₈Cl₂N₈

Chemical Name

6-(2-(4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino)ethylamino)nicotinonitrile

Molecular Weight 465.34

Color Light yellow

QC Specifications MASS Spec Mouse ESC culture for toxicity

Shipping Information on blue ice

Storage -20°C

Stability Stable for up to 6 months from date of receipt when stored as directed.

Reference 1. Ring, D.B., et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo (2003) Diabetes 52: 588-595.

2. Hall, R.K., et al. Regulation of phosphoenolpyruvate carboxykinase and insulin-like growth factor-binding protein-1 gene expression by insulin. The role of winged helix/forkhead proteins (2000) J Biol Chem 275: 30169-30175.

3. Finlay, D., et al. Glycogen synthase kinase-3 regulates IGFBP-I gene transcription through the Thymine-rich Insulin Response Element. BMC Mol Biol 5: 15.