Potent inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 10 mM in DMSO and to 10 mM in ethanol|
References are publications that support the biological activity of the product.
Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199 PMID: 12534346
Carlomagno et al (2002) The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes. Cancer Res. 62 1077 PMID: 11861385
Hanke et al (1996) Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor. J.Biol.Chem. 271 695 PMID: 8557675
Liu et al (1999) Structural basis for selective inhibition of Src family kinases by PP1. Chem.Biol. 6 671 PMID: 10467133
Tatton et al (2003) The src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases. J.Biol.Chem. 278 4847 PMID: 12475982
If you know of a relevant reference for PP 1, please let us know.
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Keywords: PP 1, PP 1 supplier, Potent, selective, Src, inhibitors, inhibits, Lyn, p56lck, p59fynT, Kinases, PP1, 1397, Tocris Bioscience
11 Citations for PP 1
Citations are publications that use Tocris products. Selected citations for PP 1 include:
Hildebrand et al (2009) Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines. J Neurosci 29 9668 PMID: 19657020
Mikelis et al (2009) Integrin alpha(v)beta(3) is a pleiotrophin receptor required for pleiotrophin-induced endothelial cell migration through receptor protein tyrosine phosphatase beta/zeta. FASEB J 23 1459 PMID: 19141530
Alonso-Magdalena et al Pancreatic insulin content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069 PMID: 18446233
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Zhang et al (2007) SRC-family kinases are activated in non-small cell lung cancer and promote the survival of epidermal growth factor receptor-dependent cell lines. Mol Cancer 170 366 PMID: 17200208
Lotz-Jenne et al (2016) A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor. Oncotarget 7 25983 PMID: 27036020
Pham et al (2012) Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells. Pancreas 41 1306 PMID: 22889981
Mace et al (2016) Human NK cell development requires CD56-mediated motility and formation of the developmental synapse. Nat Commun 7 12171 PMID: 27435370
Eum et al (2009) NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells. Toxicol Appl Pharmacol 240 299 PMID: 19632255
Koutsioumpa et al (2015) Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor. Front Syst Neurosci 14 19 PMID: 25644401
Lee et al (2007) Transforming growth factor-beta1 effects on endothelial monolayer permeability involve focal adhesion kinase/Src. Am J Respir Cell Mol Biol 37 485 PMID: 17585111
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Literature in this Area
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