Chemical Name: 1-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Biological ActivityPP 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The specificities of protein kinase inhibitors: an update.
Bain et al.
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.
Structural basis for selective inhibition of Src family kinases by PP1.
Liu et al.
The src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases.
Tatton et al.
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
Pancreatic Ins content regulation by the estrogen receptor ER alpha.
Authors: Alonso-Magdalena Et al.
PLoS One ;3:e2069
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
Chemerin-induced arterial contraction is Gi- and calcium-dependent.
Authors: Ferland Et al.
Vascul Pharmacol 2017;88:30
A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor.
Authors: Lotz-Jenne Et al.
Human NK cell development requires CD56-mediated motility and formation of the developmental synapse.
Authors: Mace Et al.
Nat Commun 2016;7:12171
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
Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells.
Authors: Pham Et al.
β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
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
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
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
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
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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