Catalog Number: 4423
Chemical Name: 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile
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.
Technical Data
  • M.Wt:
    465.34
  • Formula:
    C22H18Cl2N8
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    252917-06-9
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.
Background References
  1. Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2.
    Li et al.
    Stem Cells, 2009;27:2992
  2. AKT kinase activity is required for lithium to modulate mood-related behaviors in mice.
    Pan et al.
    Neuropsychopharmacology, 2011;36:1397
  3. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
    Ring et al.
    Diabetes, 2003;52:588
  4. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embyronic stem cells from refractory mouse strains.
    Ye et al.
    PLoS One, 2012;7:e35892
  5. Derivation of pluripotent stem cells with in vivo embryonic and extraembryonic potency.
    Yang et al.
    Cell., 2017;169:243
Citations:

The citations listed below are publications that use Tocris products. Selected citations for CHIR 99021 include:

36 Citations: Showing 1 - 10
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  1. Mutual reinforcement between telomere capping and canonical Wnt signalling in the intestinalstem cell niche.
    Authors: Yang
    Nat Commun 2017;8:14766
  2. Differentiation of human pluripotent stem cells into functional lung alveolar epithelial cells.
    Authors: Kotton Et al.
    Cell Stem Cell. 2017;21:472
  3. A modular platform for differentiation of human PSCs into all major ectodermal lineages.
    Authors: Tchieu Et al.
    Cell Stem Cell. 2017;21:399
  4. In Vivo Human Somitogenesis Guides Somite Development from hPSCs.
    Authors: Xi
    Cell Rep. 2017;18(6):1573
  5. Derivation of pluripotent stem cells with in vivo embryonic and extraembryonic potency.
    Authors: Yang Et al.
    Cell. 2017;169:243
  6. Integrin signalling regulates the expansion of neuroepithelial progenitors and neurogenesis via Wnt7a and Decorin.
    Authors: Long Et al.
    Nat Biotechnol 2016;7:10354
  7. Generating trunk neural crest from human pluripotent stem cells.
    Authors: Huang Et al.
    PLoS One 2016;6:19727
  8. Generation of serotonin neurons from human pluripotent stem cells.
    Authors: Lu Et al.
    Nat Biotechnol 2016;34:89
  9. Enhancing a Wnt-Telomere Feedback Loop Restores Intestinal Stem Cell Function in a Human Organotypic Model of Dyskeratosis Congenita
    Authors: Woo Et al.
    Cell Stem Cell 2016;19:397
  10. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell 2016;19:217
  11. Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation.
    Authors: Zhang Et al.
    Cell Stem Cell 2016;18:653
  12. Human Enteroids as a Model of Upper Small Intestinal Ion Transport Physiology and Pathophysiology.
    Authors: Foulke-Abel Et al.
    Nat Commun 2016;150:638
  13. Generation of human muscle fibers and satellite-like cells from human pluripotent stem cells in vitro.
    Authors: Chal Et al.
    Nat.Protoc. 2016;11:1833
  14. Generation of kidney organoids from human pluripotent stem cells.
    Authors: Takasato Et al.
    Nature Protocols 2016;11:1681
  15. Human pluripotent stem cell derived midbrain PITX3(eGFP/w) neurons: a versatile tool for pharmacological screening and neurodegenerative modeling.
    Authors: Watmuff Et al.
    Front Cell Neurosci 2015;9:104
  16. Enolase 1 (ENO1) and protein disulfide-isomerase associated 3 (PDIA3) regulate Wnt/β-catenin-driven trans-differentiation of murine alveolar epithelial cells.
    Authors: Mutze Et al.
    Cell Rep 2015;8:877
  17. Plasticity of Hopx(+) type I alveolar cells to regenerate type II cells in the lung.
    Authors: Jain Et al.
    Nat Commun 2015;6:6727
  18. Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells.
    Authors: Du Et al.
    Nat.Commun. 2015;6:6626
  19. Inhibition of Excessive Monoamine Oxidase A/B Activity Protects Against Stress-induced Neuronal Death in Huntington Disease.
    Authors: Ooi Et al.
    Nat Chem Biol 2015;52:1850
  20. Efficient generation of NKX6-1+ pancreatic progenitors from multiple human pluripotent stem cell lines.
    Authors: Nostro Et al.
    Eur J Immunol 2015;4:591
  21. The lymph node as a new site for kidney organogenesis.
    Authors: Francipane and Lagasse
    Stem Cells Transl Med 2015;4:295
  22. Glycogen synthase kinase-3 controls IL-10 expression in CD4(+) effector T-cell subsets through epigenetic modification of the IL-10 promoter.
    Authors: Hill Et al.
    Mol Neurobiol 2015;45:1103
  23. Nephron organoids derived from human pluripotent stem cells model kidney development and injury.
    Authors: Morizane Et al.
    Stem Cell Reports 2015;33:1193
  24. Phosphorylation and SCF-mediated degradation regulate CREB-H transcription of metabolic targets.
    Authors: Barbosa Et al.
    Stem Cell Reports 2015;26:2939
  25. Automated Video-Based Analysis of Contractility and Calcium Flux in Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes Cultured over Different Spatial Scales.
    Authors: Huebsch Et al.
    Tissue Eng Part C Methods 2015;21:467
  26. GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis.
    Authors: Zhang Et al.
    PLoS Biol 2015;13:e1002129
  27. Functional annotation of native enhancers with a Cas9-histone demethylase fusion.
    Authors: Kearns Et al.
    Nat Methods 2015;12:401
  28. Genomic DISC1 Disruption in hiPSCs Alters Wnt Signaling and Neural Cell Fate.
    Authors: Srikanth Et al.
    Sci Rep 2015;12:1414
  29. The bimodally expressed microRNA miR-142 gates exit from pluripotency.
    Authors: Sladitschek and Neveu
    J Biol Chem 2015;11:850
  30. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
    Authors: Thorne Et al.
    Mol Biol Cell 2015;11:58
  31. Manganese Superoxide Dismutase Gene Expression Is Induced by Nanog and Oct4, Essential Pluripotent Stem Cells' Transcription Factors.
    Authors: Solari Et al.
    Mol Syst Biol 2015;10:e0144336
  32. Mouse liver repopulation with hepatocytes generated from human fibroblasts.
    Authors: Zhu Et al.
    Nature 2014;508:93
  33. Derivation and expansion of PAX7-positive muscle progenitors from human and mouse embryonic stem cells.
    Authors: Shelton Et al.
    Dis Model Mech 2014;3:516
  34. A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence.
    Authors: Muthusamy Et al.
    Stem Cell Reports 2014;3:169
  35. A novel suppressive effect of alcohol dehydrogenase 5 in neuronal differentiation.
    Authors: Wu Et al.
    Stem Cell Res 2014;289:20193
  36. SIRPA, VCAM1 and CD34 identify discrete lineages during early human cardiovascular development.
    Authors: Skelton Et al.
    J Cachexia Sarcopenia Muscle 2014;13:172
Expand to show all 36 Citations
Average Rating: 4 (Based on 1 review)

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