Biological Activity
Potent and highly selective inhibitor of glycogen synthase kinase 3 (GSK-3) (IC50 values are 6.7 and 10 nM for GSK-3β and GSK-3α respectively). Exhibits >500-fold selectivity for GSK-3 over closely related kinases; also displays >800-fold selectivity against 45 additional enzymes and receptors. In combination with tranylcypromine (Cat. No. 3852), enables reprogramming of mouse embryonic fibroblasts, transduced by Oct4 and Klf4 only, into iPSCs. Enhances mouse and human ESC self-renewal when used in combination with PD 0325901 (Cat. No. 4192). Allows formation of extended pluripotent stem (EPS) cells in combination with (S)-(+)-Dimethindene maleate (Cat.No. 1425), minocycline hydrochloride (Cat.No. 3268) and human leukemia inhibitory factor.
Compound Libraries
CHIR 99021 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 465.34 |
| Formula | C22H18Cl2N8 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 252917-06-9 |
| PubChem ID | 9956119 |
| InChI Key | AQGNHMOJWBZFQQ-UHFFFAOYSA-N |
| Smiles | ClC(C=C3Cl)=CC=C3C1=NC(NCCNC4=CC=C(C#N)C=N4)=NC=C1C2=NC(C)=CN2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.31 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 465.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.74 mL | 21.49 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Pan et al (2011) AKT kinase activity is required for lithium to modulate mood-related behaviors in mice. Neuropsychopharmacology 36 1397 PMID: 21389981
Ring et al (2003) Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes 52 588 PMID: 12606497
Li et al (2009) Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells 27 2992 PMID: 19839055
Ye et al (2012) Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embyronic stem cells from refractory mouse strains. PLoS One 7 e35892 PMID: 22540008
Yang et al (2017) Derivation of pluripotent stem cells with in vivo embryonic and extraembryonic potency. Cell. 169 243 PMID: 28388409
Keywords: CHIR 99021, supplier, CHIR99021, glycogen, synthase, kinase, 3, gsk-3, gsk-3a, gsk-3alpha, gsk-3α, gsk-3b, gsk-3beta, gsk-3β, inhibitors, inhibits, highly, selective, potent, organoids, Glycogen, Synthase, Kinase, 3, Glycogen, Synthase, Kinase, Reprogramming, Glycogen, Synthase, Kinase, 3, Tocris Bioscience
