PP 1
Chemical Name: 1-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥99%
Biological Activity
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
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.
Background References
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The specificities of protein kinase inhibitors: an update.
Bain et al.
Biochem.J., 2003;371:199 -
The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes.
Carlomagno et al.
Cancer Res., 2002;62:1077 -
Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor.
Hanke et al.
J.Biol.Chem., 1996;271:695 -
Structural basis for selective inhibition of Src family kinases by PP1.
Liu et al.
Chem.Biol., 1999;6:671 -
The src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases.
Tatton et al.
J.Biol.Chem., 2003;278:4847
Product Datasheets
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Citations for PP 1
The citations listed below are publications that use Tocris products. Selected citations for PP 1 include:
13 Citations: Showing 1 - 10
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Pancreatic Ins content regulation by the estrogen receptor ER alpha.
Authors: Alonso-Magdalena Et al.
PLoS One ;3:e2069
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Role of ceramide synthase 2 in G-CSF signaling and G-CSF-R translocation into detergent-resistant membranes.
Authors: Kurz Et al.
Sci Rep 2019;9:747
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Chemerin-induced arterial contraction is Gi- and calcium-dependent.
Authors: Ferland Et al.
Vascul Pharmacol 2017;88:30
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A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor.
Authors: Lotz-Jenne Et al.
Oncotarget 2016;7:25983
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Human NK cell development requires CD56-mediated motility and formation of the developmental synapse.
Authors: Mace Et al.
Nat Commun 2016;7:12171
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Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor.
Authors: Koutsioumpa Et al.
Front Syst Neurosci 2015;14:19
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Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells.
Authors: Pham Et al.
Pancreas 2012;41:1306
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β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
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Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines.
Authors: Hildebrand Et al.
J Neurosci 2009;29:9668
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NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells.
Authors: Eum Et al.
Toxicol Appl Pharmacol 2009;240:299
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Integrin alpha(v)beta(3) is a pleiotrophin receptor required for pleiotrophin-induced endothelial cell migration through receptor protein tyrosine phosphatase beta/zeta.
Authors: Mikelis Et al.
FASEB J 2009;23:1459
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Transforming growth factor-beta1 effects on endothelial monolayer permeability involve focal adhesion kinase/Src.
Authors: Lee Et al.
Am J Respir Cell Mol Biol 2007;37:485
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SRC-family kinases are activated in non-small cell lung cancer and promote the survival of epidermal growth factor receptor-dependent cell lines.
Authors: Zhang Et al.
Mol Cancer 2007;170:366
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