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PP2

Src kinase inhibitor
 
BML-EI297-0001 1 mg 113.00 USD
 
BML-EI297-0005 5 mg 459.00 USD
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Replaces Prod. #: ALX-270-233

A potent and selective inhibitor of the Src family tyrosine kinases. Inhibits Lck (IC50=4 nM), Fyn (IC50=5 nM), and Hck (IC50=5 nM). It displays weaker inhibition of EGFR (IC50=480 nM) and no inhibition of ZAP-70 (IC50 100 µM) and JAK2 (IC5050 µM). PP2 is a useful tool for probing the involvement of Src family tyrosine kinases in cellular signaling.

Product Details

Alternative Name:AG1879, 4-Amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
 
Formula:C15H16CIN5
 
MW:301.8
 
CAS:172889-27-9
 
Purity:≥98% (TLC)
 
Appearance:Off-white solid.
 
Solubility:Soluble in DMSO (25mg/ml).
 
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

CD24 associates with EGFR and supports EGF/EGFR signaling via RhoA in gastric cancer cells: W. Deng, et al.; J. Transl. Med. 14, 32 (2016), Application(s): Cell culture, Abstract; Full Text
Ras-related C3 Botulinum Toxin Substrate (Rac) and Src Family Kinases (SFK) are Proximal and Essential for Phosphatidylinositol-3 Kinase (PI3K) Activation in Natural Killer (NK) Cell-Mediated Direct Cytotoxicity Against C. neoformans: R.F. Xiang, et al.; J. Biol. Chem. 291, 6912 (2016), Application(s): Cell culture, Abstract; Full Text
Activation of phosphatidylinositol 3-kinase β by the platelet collagen receptors integrin α2β1 and GPVI: The role of Pyk2 and c-Cbl: D. Manganaro, et al.; Biochim. Biophys. Acta 1853, 1879 (2015), Application(s): Cell Culture, Abstract;
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;
Ligands Binding to Cell Surface Ganglioside GD2 Cause Src-Dependent Activation of N-Methyl-D-Aspartate Receptor Signaling and Changes in Cellular Morphology: W. Tong, et al. ; PLoS One 10, e0134255 (2015), Application(s): Pharmacological inhibition , Abstract; Full Text
Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2): F. Carlomagno et al.; J. Clin. Endocrinol. Metab. 88, 1897 (2003), Abstract;
Overexpression of C-terminal Src kinase blocks 14, 15-epoxyeicosatrienoic acid-induced tyrosine phosphorylation and mitogenesis: J.K. Chen et al.; J Biol Chem 275, 13789 (2000), Abstract;
Src and Cas mediate JNK activation but not ERK1/2 and p38 kinases by reactive oxygen species: M. Yoshizumi et al.; J. Biol. Chem. 275, 11706 (2000), 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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