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Stemgent Stemolecule CHIR99021

Code: 04-0004-base
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The aminopyrimidine CHIR99021 is the most selective inhibitor of glycogen synthase kinase 3 β (GSK-3β) reported to date1,2. Unlike other potent inhibitors of GSK-3, CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs3. Along with the elimination of differentiation-inducing signaling from mitogen-activated protein kinases, using CHIR99021 to block the activity of GSK-3β enables the self-renewal of embryonic stem cells4.

Also available as a convenient 10 mM solution in DMSO (Cat. No. 04-0004-02)

Product Name

Stemolecule CHIR99021

Catalog Number

04-0004

Size

2 mg (Cat. No. 04-0004)

10 mg (Cat. No. 04-0004-10)

2 mg in 10 mM DMSO solution (Cat. No. 04-0004-02)

AlternateName(s)

6-[[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2 pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile

Chemical Formula

C22H18Cl2N8

Molecular Weight

465.34

CAS Number

252917-06-9

Purity

Greater than 95% by HPLC analysis

Formulation

Off-white solid

Solubility

Reconstitute in DMSO to the desired concentration. For reconstitution instructions please reference product specifications sheet.

Storage and Stability

Store powder at 4 °C protected from light. Information about the stability of Stemolecules in solution is largely not available. As a general guideline, we recommend that stock solution be freshly made and stored in aliquots at −20 °C. The effect of storage of stock solutions should be verified for each application.

Quality Control

The purity of CHIR99021 was determined by HPLC analysis. The accurate mass was determined by mass spectrometry. Cellular toxicity of CHIR99021 was tested on mouse embryonic stem cells.

  1. Sato, N., Meijer, L., Skaltsounis, L., Greengard, P., and Brivanlou, A.H. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat Med 10: 55-63 (2004).
  2. Besser, D. (2004) Expression of nodal, lefty-a, and lefty-B in undifferentiated human embryonic stem cells requires activation of Smad 2/3. J Biol Chem 279: 45076-45084 (2004).
  3. Ying, Q.L., Wray, J., Nichols, J., Batlle-Morera, L., Doble, B., Woodgett, J., Cohen, P., and Smith, A. The ground state of embryonic stem cell self renewal. Nature 453: 519-523 (2008).
  4. Polychronopoulos, P., Magiatis, P., Skaltsounis, A.L., Myrianthopoulos, V., Mikros, E., Tarricone, A., Musacchio, A., Roe, S.M., Pearl, L., Leost, M., Greengard, P., and Meijer, L. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem 47: 935-946 (2004).

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