PP 1

Cat. No. 1397

PP 1 C16H19N5 [172889-26-8]

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Chemical Name: 1-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Biological Activity

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.

Technical Data

M.Wt:
281.36
Formula:
C16H19N5
Solubility:
Soluble to 10 mM in DMSO and to 10 mM in ethanol
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
172889-26-8

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199. PMID: 12534346.

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.

Carlomagno et al (2002) The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes. Cancer Res. 62 1077. PMID: 11861385.

Liu et al (1999) Structural basis for selective inhibition of Src family kinases by PP1. Chem.Biol. 6 671. PMID: 10467133.

Hanke et al (1996) Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor. J.Biol.Chem. 271 695. PMID: 8557675.

If you know of a relevant reference for PP 1 please let us know.

Citations are publications that use Tocris products. Selected citations for PP 1 include:

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.

Pham et al (2012) Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells. Pancreas 41 1306. PMID: 22889981.

Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984. PMID: 21143600.

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.

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.

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.

Alonso-Magdalena et al Pancreatic insulin content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069. PMID: 18446233.

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Keywords: PP 1, supplier, Potent, selective, Src, inhibitors, inhibits, Lyn, p56lck, p59fynT, Kinases, PP1, Tocris Bioscience, Src Kinase Inhibitor products

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