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CHIR99021

2 mg

Cat. No.: 27-H76

Original price was: $219.00.Current price is: $89.00.

CHIR99021 is the most selective inhibitor of glycogen synthase kinase 3β (GSK3β). CHIR99021 does not show cross-reactivity against cyclin-dependent kinases (CDKs) with a 350 fold selectivity toward GSK3β compared to CDKs with a Kᵢ of <10nM in vitro. CHIR99021 has been shown in long term expansion of murine embryonic stem cells in conjunction with MEK/MAPK inhibitor PD184352 and fibroblast growth factor receptor (FGFR) inhibitor SU5402.

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TECHNICAL INFORMATION

Other Names: CT99021, 6-((2-((4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile

Chemical Formula: C22H18Cl2N8

CAS Number: 252917-06-09

Molecular Weight: 465.34

Purity: >98% by HPLC

IC50= 6.7nM

Appearance: Off White Solid

Solubility: DMSO (100mM)

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C.

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO (100mM). For a 10 mM solution, reconstitute by adding 430µl of DMSO to the entire contents of the vial. For most cells, the maximum tolerance to DMSO is <0.5%. Incubate in a 37°C water bath for 5 minutes  if a precipitate is observed.

When used in combination with PD0325901, CHIR99021 has been shown to sustain ES cell self-renewal.

References

Tighe A et al. (2007). GSK-3 inhibitors induce chromosome instability. BMC Cell Biol. 8:34.

Ring D et al. (2003). Selective Glycogen Synthase Kinase 3 Inhibitors Potentiate Insulin Activation of Glucose Transport and Utilization In Vitro and In Vivo. Diabetes. 52: 3 | 588-595.

Finley D et al. (2004). Glycogen Synthase Kinase-3 regulates IGFBP-1 gene transcription through the Thymine-rich Insulin Response Element. BMC Mol. Biol. 5:15

Ying Q. et al. (2008) The ground state of embryonic stem cell self renewal. Nature. 453: 519-523.

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