GSK-3 Inhibitor

　CHIR 99021 (1) is a cell-permeable and highly selective GSK-3 inhibitor¹⁾ and inhibits GSK3α (IC₅₀=10 nM) and GSK3β (6.7 nM).²⁾ 1 is also used as a key component for mouse embryonic stem cell self-renewal.³⁾ Under cytokine-free conditions, the combination of 1 and the mTOR inhibitor, rapamycin, maintains mouse and human hematopoietic stem cells.⁴⁾ In the presence of 1, OCT4-transduced human blood CD34⁺ cells are converted into induced mesenchymal stem cells (iMSCs).⁵⁾

The product is for research purposes only.

References

• 1) The selectivity of protein kinase inhibitors: further update
  • J. Bain, L. Plater, M. Elliott, N. Shpiro, C. J. Hastie, H. McLauchlan, I. Klevernic, J. S. C. Arthur, D. R. Alessi, P. Cohen, Biochem. J. 2007, 408, 297.
• 2) Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo
  • D. B. Ring, K. W. Johnson, E. J. Henriksen, J. M. Nuss, D. Goff, T. R. Kinnick, S. T. Ma, J. W. Reeder, I. Samuels, T. Slabiak, A. S. Wagman, M.-E. W. Hammond, S. D. Harrison, Diabetes 2003, 52, 588.
• 3) Modulation of β-catenin function maintains mouse epiblast stem cell and human embryonic stem cell self-renewal
  • H. Kim, J. Wu, S. Ye, C.-I. Tai, X. Zhou, H. Yan, P. Li, M. Pera, Q.-L. Ying, Nat. Commun. 2013, 4, 2403.
• 4) Maintenance of hematopoietic stem cells through regulation of Wnt and mTOR pathways
  • J. Huang, M. Nguyen-McCarty, E. O. Hexner, G. Danet-Desnoyers, P. S. Klein, Nat. Med. 2012, 18, 1778.
• 5) Rapid and efficient reprogramming of human fetal and adult blood CD34⁺ cells into mesenchymal stem cells with a single factor
  • X. Meng, R.-J. Su, D. J. Baylink, A. Neises, J. B. Kiriyan, W. Y.-W. Lee, K. J. Payne, D. S. Gridley, J. Wang, K.-H. W. Lau, G. Li, X.-B. Zhang, Cell Res. 2013, 23, 658.

Related Compounds

R0097

Rapamycin

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