PP 1

Pricing Availability   Qty
Description: Potent, selective Src family kinase inhibitor
Chemical Name: 1-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥99% (HPLC)
Citations (13)
Literature (1)

Biological Activity for PP 1

PP 1 is a 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 for PP 1

M. Wt 281.36
Formula C16H19N5
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 172889-26-8
PubChem ID 1400
Smiles CC1=CC=C(C=C1)C1=NN(C2=NC=NC(N)=C12)C(C)(C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PP 1

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 10

Preparing Stock Solutions for PP 1

The following data is based on the product molecular weight 281.36. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 35.54 mL 177.71 mL 355.42 mL
0.5 mM 7.11 mL 35.54 mL 71.08 mL
1 mM 3.55 mL 17.77 mL 35.54 mL
5 mM 0.71 mL 3.55 mL 7.11 mL

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Product Datasheets for PP 1

Certificate of Analysis / Product Datasheet
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References for PP 1

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

13 Citations for PP 1

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

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

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

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

Do you know of a great paper that uses PP 1 from Tocris? Please let us know.

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Literature in this Area

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