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PP1

Src kinase inhibitor
 
BML-EI275-0001 1 mg 111.00 USD
 
BML-EI275-0005 5 mg 459.00 USD
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Replaces Prod. #: ALX-270-177

A highly potent and selective inhibitor of Src family tyrosine kinases, IC50=5 nM for p56lck; p59fynT=6 nM; p60src=170 nM. Inhibition of Src family kinases by PP1 has been shown to: prevent a-thrombin-stimulated Akt phosphorylation, delay PAF-mediated STAT3 phosphorylation, block Zn2+-induced Ras activation, block adhesion-dependent tyrosine phosphorylation of p105HEF1 5, and inhibit HLA-DR-induced tyrosine phosphorylation without affecting the activation of ERK1/2.

Product Details

Formula:C16H19N5
 
MW:281.4
 
CAS:172889-26-8
 
Purity:≥98% (TLC)
 
Appearance:Tan solid.

 
Solubility:Soluble in DMSO (25mg/ml), slightly soluble in 100% ethanol.

 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
 
Regulatory Status:RUO - Research Use Only
 
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Product Literature References

Gαs proteins Activate p72 Syk and p60-c-Src Tyrosine Kinases to Mediate Sickle Red Blood Cell Adhesion to Endothelium via LW-αvβ3 and CD44-CD44 Interactions: E. Chiou, et al.; Int. J. Biochem. Cell. Biol. 65, 40 (2015), Application(s): Cell Culture, Abstract;
α6 integrin transactivates insulin-like growth factor receptor-1 (IGF-1R) to regulate caspase-3-mediated lens epithelial cell differentiation initiation: S. Basu, et al.; J. Biol. Chem. 289, 3842 (2014), Abstract;
The specificities of protein kinase inhibitors: an update: J. Bain et al.; Biochem. J. 371, 199 (2003), Abstract;
The Src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases: L. Tatton et al.; J. Biol. Chem. 278, 4847 (2003), Abstract;
The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes: F. Carlomagno et al.; Cancer Res. 62, 1077 (2002), Abstract;
Cytokine-driven proliferation and differentiation of human naive, central memory, and effector memory CD4(+) T cells: J. Geginat et al.; J. Exp. Med. 194, 1711 (2001), Abstract;
Reactive oxygen species activate p90 ribosomal S6 kinase via Fyn and Ras: J. Abe et al.; J. Biol. Chem. 275, 1739 (2000), Abstract;
Morphological differentiation of oligodendrocytes requires activation of Fyn tyrosine kinase: D.J. Osterhout et al.; J Cell Biol 145, 1209 (1999), Abstract;
Structural basis for selective inhibition of Src family kinases by PP1: Y. Liu et al.; Chem. Biol. 6, 671 (1999), Abstract;
The urokinase-type plasminogen activator receptor mediates tyrosine phosphorylation of focal adhesion proteins and activation of mitogen-activated protein kinase in cultured endothelial cells: H. Tang et al.; J. Biol. Chem. 273, 18268 (1998), Abstract;
Tyrosine kinases of the Src family participate in signaling to MAP kinase from both Gq and Gi-coupled receptors: T. Igishi & J.s. Gutkind et al.; Biochem. Biophys. Res. Commun. 244, 5 (1998), Abstract;
Src family-selective tyrosine kinase inhibitor, PP1, inhibits both Fc epsilonRI- and Thy-1-mediated activation of rat basophilic leukemia cells: M. Amoui et al.; Eur. J. Immunol. 27, 1881 (1997), Abstract;
Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation: J.H. Hanke et al.; J. Biol. Chem. 271, 695 (1996), Abstract;

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