CHIR 99021
Tocris Bioscience, part of Bio-Techne | Catalog # 4423
Highly selective GSK-3 inhibitor; acts as Wnt activator
Key Product Details
Description
Highly selective GSK-3 inhibitor; acts as Wnt activator
Alternative Names
CHIR99021,CT99021
Product Description
CHIR 99021 is a 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). Acts as Wnt activator. 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 the irreversible inhibitor of LSD1 (Cat. No. 3852), CHIR 99021 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). It promotes differentiation of hPSCs in cardiomyocytes and allows formation of extended pluripotent stem (EPS) cells (see protocols below). Used in a protocol to generate brain organoids from human iPSCs. Also used in iPS cell differentiation protocol that produces CD34+ hematopoietic cells with multilineage engraftment ability.CHIR 99021 synthesized to cGMP guidelines and CHIR 99021 in solution also available.
For more information on how to use CHIR 99021, see our protocols: Transdifferentiating Fibroblasts into Neurons, Culturing Transcriptomically Distinct Pluripotent mESCs, Converting Fibroblasts into Cardiomyocytes (9C Cocktail), Human iPSC-derived Myoblasts, Reprogramming MEFs into Skeletal Muscle Progenitors, highly-efficient-generation-cipscs-mefs, Generation of β cells from hPSCs, generation-and-propagation-eps-cells-lcdm-cocktail, generating-vascular-organoids, 3D Culture of Lung Alveolar Cells, Differentiation of Hematopoietic Progenitors from hPSCs, Generating Midbrain Dopaminergic Neurons from hPSCs, Generation of Kidney Organoids from hPSCs.
Scientific Data Images for CHIR 99021
Cardiomyocyte derived from human induced pluripotent stem cells (hiPSCs) using CHIR 99021.
Cells cultured in Media supplemented with Activin A (Catalog # 338-AC, R&D Systems), N21-MAX Insulin Free (Catalog # AR010, R&D Systems), BMP-4 (Catalog # 314-BP, R&D Systems), bFGF (Catalog # 233-FB, R&D Systems) and DKK-1 (Catalog # 5439-DK, R&D Systems). Stained for F-Actin (Phalloidin, green), Troponin T (red, Human Troponin T (Cardiac) Antibody, Catalog # MAB1874, R&D Systems) and counterstained with DAPI (blue, Catalog # 5748, Tocris).External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of CHIR-99021 is reviewed on the chemical probes website.
Product Specifications
Molecular Weight
465.34
Formula
C22H18Cl2N8
Storage
Store at -20°C
Purity
≥98%
Chemical Name
6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile
CAS Number
252917-06-9
PubChem ID
9956119
InChI Key
AQGNHMOJWBZFQQ-UHFFFAOYSA-N
SMILES
ClC(C=C1Cl)=CC=C1C2=NC(NCCNC3=CC=C(C#N)C=N3)=NC=C2C4=NC=C(C)N4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.31 | 20 |
Preparing Stock Solutions
for CHIR 99021
The following data is based on the product molecular weight 465.34
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 10.74 mL | 53.72 mL | 107.45 mL |
| 1 mM | 2.15 mL | 10.74 mL | 21.49 mL |
| 2 mM | 1.07 mL | 5.37 mL | 10.74 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.15 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Hoang Generation of spatial-patterned early-developing cardiac organoids using human pluripotent stem cells. Nat.Protoc. 2018 PMID: 29543795
- Lian Robust cardiomyocyte differentiation from human pluripotent stem cells via temporal modulation of canonical Wnt signaling. Proc.Natl.Acad.Sci.U.S.A. 2012 PMID: 22645348
- Wimmer Human blood vessel organoids as a model of diabetic vasculopathy. Nature 2019 PMID: 30651639
- Noor 3D Printing of Personalized Thick and Perfusable Cardiac Patches and Hearts. Adv.Sci.(Weinh) 2019 PMID: 31179230
- Dye In vitro generation of human pluripotent stem cell derived lung organoids. Elife 2015 PMID: 25803487
- Koehler 3D mouse embryonic stem cell culture for generating inner ear organoids. Nat.Protoc. 2014 PMID: 24784820
- Bartfeld In vitro expansion of human gastric epithelial stem cells and their responses to bacterial infection. Gastroenterology 2015 PMID: 25307862
- Ring Selective glycogen synthase kinase 3 inhibitors potentiate Ins activation of glucose transport and utilization in vitro and in vivo. Diabetes 2003 PMID: 12606497
- Sato SnapShot: Growing Organoids from Stem Cells. Cell 2015 PMID: 26091044
- Mahe Establishment of gastrointestinal epithelial organoids Curr.Protoc. Mouse Biol. 2014 PMID: 25105065
- Yang Derivation of pluripotent stem cells with in vivo embryonic and extraembryonic potency. Cell. 2017 PMID: 28388409
- Ye Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embyronic stem cells from refractory mouse strains. PLoS One 2012 PMID: 22540008
- Li Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells 2009 PMID: 19839055
- Schafer An in vivo neuroimmune organoid model to study human microglia phenotypes. Cell 2023 PMID: 37172564
- Xia The generation of kidney organoids by differentiation of human pluripotent cells to ureteric bud progenitor-like cells. Nat. Protoc. 2014 PMID: 25340442
- Ng Long-term engrafting multilineage hematopoietic cells differentiated from human induced pluripotent stem cells. Nat.Biotechnol. 2024 PMID: 39223325
- Pan AKT kinase activity is required for Li to modulate mood-related behaviors in mice. Neuropsychopharmacology 2011 PMID: 21389981
Product Specific Notices for CHIR 99021
For research use only
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