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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: ≥98% (HPLC)
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 | ≥98% (HPLC) |
| CAS Number | 172889-26-8 |
| PubChem ID | 1400 |
| InChI Key | ZVPDNRVYHLRXLX-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10 | ||
| 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.
| 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
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:
Kurz et al (2019) Role of ceramide synthase 2 in G-CSF signaling and G-CSF-R translocation into detergent-resistant membranes. Sci Rep 9 747 PMID: 30679689
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Ferland et al (2017) Chemerin-induced arterial contraction is Gi- and calcium-dependent. Vascul Pharmacol 88 30 PMID: 27890480
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
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
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
Pham et al (2012) Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells. Pancreas 41 1306 PMID: 22889981
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
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
Alonso-Magdalena et al Pancreatic Ins content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069 PMID: 18446233
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