Protein Kinase Inhibitor PP2 (PKI PP2, 4-amino-5-(4-chlorophenyl)-7- (t-butyl)pyrazolo[3,4-d]pyrimidine)

PP2 is a potent and selective inhibitor of the Src family tyrosine kinases. PP2 is a useful tool for probing the involvement of Src family tyrosine kinases in cellular signaling. \n\nMolecular Weight: \n~301.8\n\nBiological Activity: \nLck: IC50 =4nM\nFyn: IC50 =5nM\nHck: IC50 =5nM\nEGFR: IC50 =480nM\n\nSolubility: \nDMSO (~25mg/ml)\n\nStorage and Stability:\nLyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with sterile dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.

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SPECIFICATIONS

Catalog Number

P9104-82

Size

1mg

Form

Supplied as a off white lyophilized powder. Reconstitute with sterile dH2O to 0.1-1mg/ml.

Purity

~98% (TLC)

References

1. Hanke, J.H., et al. (1996) Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J. Biol. Chem. 271:695-701. 2. Chen, J.K., et al. (2000) Overexpression of C-terminal Src kinase blocks 14, 15- epoxyeicosatrienoic acid-induced tyrosine phosphorylation and mitogenesis. J. Biol. Chem. 275(18):13789-13792. 3. Abu-Ghazaleh, R., et al. (2001) Src mediates stimulation by vascular endothelial growth factor of the phosphorylation of focal adhesion kinase at tyrosine 861, and migration and anti-apoptosis in endothelial cells. Biochem. J. 360(Pt 1):255-264 (cites the use of 44-624 and 44-626). 4. Shanley, T.P., et al. (2001) The serine/threonine phosphatase, PP2A: endogenous regulator of inflammatory cell signaling. J. Immunol. 166(2):966-972. 5. Wilson, M.B., et al. (2002) Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene 21(53):8075-8088. 6. Williamson, R., et al. (2002) Rapid tyrosine phosphorylation of neuronal proteins including tau and focal adhesion kinase in response to amyloid-beta peptide exposure: involvement of Src family protein kinases. J. Neurosci. 22(1):10-20.