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Inhibitor Libraries

Kinase Kit Resource

Inhibitor Resource
  PP2
Cat. No. 529573  
All Categories » Calbiochem » Inhibitors » Kinase and Phosphatase » Protein Tyrosine Kinase (PTK) » Non-Receptor

AG 1879
4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine

Off-white solid. PACKAGED UNDER INERT GAS. A potent and selective inhibitor of the Src family of protein tyrosine kinases. Inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM). Does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 > 50 µM), or ZAP-70 (IC50 >100 µM). Inhibits the activation of focal adhesion kinase and its phosphorylation at Tyr577. Also potently inhibits anti-CD3-stimulated tyrosine phosphorylation of human T cells (IC50 = 600 nM). Purity: ≥95% by HPLC. CAS 172889-27-9.

Ref.: Karni, R., et al. 2003. FEBS Lett. 537, 47. Salazar, E.P., and Rozengurt, E. 1999. J. Biol. Chem. 274, 28371. Hanke, J.H., et al. 1996. J. Biol. Chem. 271, 695.

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1 mgYN/A

SolubilityMolecular FormulaMol. Wt.
DMSO C15H16ClN5 301.8 


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Related Categories:
All Categories » Calbiochem » Inhibitors » Kinase and Phosphatase » Protein Tyrosine Kinase (PTK) » Non-Receptor

Selected Citations:
  1. Marie Dance, et al. (2006) The adaptor protein gab1 couples the stimulation of vascular endothelial growth factor receptor-2 to the activation of phosphoinositide 3-kinase. Journal of Biological Chemistry 281, 23285-23295.
  2. Satoshi Fukumoto, et al. (2006) Laminin 5 is required for dental epithelium growth and polarity and the development of tooth bud and shape. Journal of Biological Chemistry 281, 5008-5016.
  3. Elke Heiss, et al. (2006) Identification of Y589 and Y599 in the juxtamembrane domain of Flt3 as ligand-induced autophosphorylation sites involved in binding of Src family kinases and the protein tyrosine phosphatase SHP2. Blood in press,.
  4. Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.
  5. Ana Olivera, et al. (2006) IgE-dependent activation of sphingosine kinase 1 and 2 and secretion of sphingosine-1-phosphate requires Fyn kinase and contributes to mast cell responses. Journal of Biological Chemistry 281, 2515-2525.
  6. Suresh K. Rayala, et al. (2006) Hepatocyte growth factor-regulated tyrosine kinase substrate (HRS) interacts with PELP1 and activates MAPK. Journal of Biological Chemistry 281, 4395-4403.
  7. Ellen J. Tisdale and Cristina R. Artalejo. (2006) Src-dependent aPKC/ tyrosine phosphorylation is required for aPKC/ association with Rab2 and glyceraldehyde-3-phosphate dehydrogenase on Pre-golgi intermediates. Journal of Biological Chemistry 281, 8436-8442.
  8. Ellen J. Tisdale and Cristina R. Artalejo. (2006) Src-dependent a protein kinase C(aPKC) λ tyrosine phosphorylation is required for aPKCl/λ association with Rab2 and glyceraldehyde-3-phosphate dehydrogenase on pre-golgi intermediates. Journal of Biological Chemistry 281, 8436-8442.
  9. Malcolm A. Meyn, et al. (2005) Src family kinase activity is required for murine embryonic stem cell growth and differentiation. Molecular Pharmacology 68, 1320-1330.
  10. Justin M. Summy, et al. (2005) AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Molecular Cancer Therapeutics 4, 1900-1911.

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