Chemical Name: 3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Biological ActivityPP 2 is a selective inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 4 and 5 nM respectively). Displays > 10000-fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC50 = 0.73 μM).
Negative Control also available.
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.
The specificities of protein kinase inhibitors: an update.
Bain et al.
Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor.
Hanke et al.
Protein kinase inhibitors: the tyrosine-specific protein kinases.
Lawrence and Niu
A role for Src kinase in spontaneous epileptiform activity in the CA3 region of the hippocampus.
Sanna et al.
Citations for PP 2
The citations listed below are publications that use Tocris products. Selected citations for PP 2 include:
51 Citations: Showing 1 - 10
Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors.
Authors: Poli Et al.
J Enzyme Inhib Med Chem 2018;33:956
Src activation by Chk1 promotes actin patch formation and prevents chromatin bridge breakage in cytokinesis.
Authors: Dandoulaki Et al.
J Cell Biol 2018;217:3071
A genome-wide screen identifies YAP/WBP2 interplay conferring growth advantage on human epidermal stem cells.
Authors: Walko Et al.
Nat Commun 2017;8:14744
Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression.
Authors: Li Et al.
Increased NRG1-ErbB4 signaling in human symptomatic epilepsy.
Sci Rep 2017;7(1):141
Mathematical model of early Reelin-induced Src family kinase-mediated signaling.
Authors: Hass Et al.
PLoS One 2017;12:e0186927
Estrogen and Progesterone Integration in an in vitro Model of RP3V Kisspeptin Neurons.
Authors: Mittelman-Smith Et al.
A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor.
Authors: Lotz-Jenne Et al.
Sonic hedgehog stimulates neurite outgrowth in a mechanical stretch model of reactive-astrogliosis.
Authors: Berretta Et al.
Sci Rep 2016;6:21896
Presynaptic GABAB receptors reduce transmission at parabrachial synapses in the lateral central amygdala by inhibiting N-type calcium channels.
Authors: Delaney and Crane
Sci Rep 2016;6:19255
Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2.
Authors: Wang Et al.
Br J Pharmacol 2016;173:3342
Progesterone receptor membrane component-1 regulates hepcidin biosynthesis.
Authors: Li Et al.
J Clin Invest 2016;126:389
The prion protein constitutively controls neuronal store-operated Ca(2+) entry through Fyn kinase.
Authors: Mario Et al.
Extracellular galectin-3 programs multidrug resistance through Na+/K+-ATPase and P-glycoprotein signaling.
Authors: Harazono Et al.
PLoS One 2015;6:19592
Anoikis resistance is a critical feature of highly aggressive ovarian cancer cells.
Authors: Cai Et al.
J Cell Sci 2015;34:3315
Tyrosine phosphorylation of WIP releases bound WASP and impairs podosome assembly in macrophages.
Authors: Vijayakumar Et al.
Front Cell Neurosci 2015;128:251
mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
Authors: Kubota Et al.
PLoS One 2014;9:e106316
Long-term treatment with PP2 after spinal cord injury resulted in functional locomotor recovery and increased spared tissue.
Authors: Rosas Et al.
PLoS One 2014;9:2164
A role for intracellular zinc in glioma alteration of neuronal chloride equilibrium.
Authors: Angelantonio Et al.
Cell Death Dis 2014;5:e1501
Palmitate induces reactive oxygen species production and β-cell dysfunction by activating nicotinamide adenine dinucleotide phosphate oxidase through Src signaling.
Authors: Sato Et al.
Heat shock protein 90 inhibitors prevent LPS-induced endothelial barrier dysfunction by disrupting RhoA signaling.
Authors: Joshi Et al.
Am J Respir Cell Mol Biol 2014;50:170
BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals.
Authors: Chen Et al.
Eur J Neurosci 2014;39:1439
The ShcD signaling adaptor facilitates ligand-independent phosphorylation of the EGF receptor.
Authors: Wills Et al.
Mol Biol Cell 2014;25:739
Functional kinomics identifies candidate therapeutic targets in head and neck cancer.
Authors: Moser Et al.
Clin Cancer Res 2014;20:4274
Reelin signaling specifies the molecular identity of the pyramidal neuron distal dendritic compartment.
Authors: Kupferman Et al.
A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
Authors: Mitrugno Et al.
Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor.
Authors: Bayliss and Evans
PLoS One 2013;8:e80833
Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells.
Authors: Soltoff and Lannon
PLoS One 2013;8:e72881
SPIN90 phosphorylation modulates spine structure and synaptic function.
Authors: Cho Et al.
Mol Immunol 2013;8:e54276
Protein tyrosine phosphatase 1B modulates GSK3β/Nrf2 and IGFIR signaling pathways in acetaminophen-induced hepatotoxicity.
Authors: Mobasher Et al.
Cell Death Dis 2013;4:e626
Src kinase is a direct target of apigenin against UVB-induced skin inflammation.
Authors: Byun Et al.
Human T cell activation results in extracellular signal-regulated kinase (ERK)-calcineurin-dependent exposure of Tn antigen on the cell surface and binding of the macrophage galactose-type lectin (MGL).
Authors: Vliet Et al.
J Biol Chem 2013;288:27519
Annexin A1, formyl peptide receptor, and NOX1 orchestrate epithelial repair.
Authors: Leoni Et al.
J Clin Invest 2013;123:443
Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells.
Authors: Pham Et al.
β-OE unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus.
Authors: Nebieridze Et al.
5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization.
Authors: Bigford Et al.
J Biol Chem 2012;287:11049
Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth.
Authors: Zhou and Too
Neural Regen Res 2011;6:e21680
Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites.
Authors: Ivanova Et al.
FASEB J 2011;25:1402
Genistein and tyrphostin AG556 inhibit inwardly-rectifying Kir2.1 channels expressed in HEK 293 cells via protein tyrosine kinase inhibition.
Authors: Zhang Et al.
Biochim Biophys Acta 2011;1808:1993
Epidermal growth factor receptor tyrosine kinase regulates the human inward rectifier potassium K(IR)2.3 channel, stably expressed in HEK 293 cells.
Authors: Zhang Et al.
Br J Pharmacol 2011;164:1469
Different responses in transformation of MDCK cells in 2D and 3D culture by v-Src as revealed by microarray techniques, RT-PCR and functional assays.
Authors: Töyli Et al.
Lab Invest 2010;90:915
Regulation of human cardiac KCNQ1/KCNE1 channel by epidermal growth factor receptor kinase.
Authors: Dong Et al.
Biochim Biophys Acta 2010;1798:995
FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation.
Authors: Grodzki Et al.
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
Beta1 integrin-dependent engulfment of Yersinia enterocolitica by macrophages is coupled to the activation of autophagy and suppressed by type III protein secretion.
Authors: Deuretzbacher Et al.
J Immunol 2009;183:5847
D1/5 receptor-mediated enhancement of LTP requires PKA, Src family kinases, and NR2B-containing NMDARs.
Coactivation of M(1) muscarinic and alpha1 adrenergic receptors stimulates extracellular signal-regulated protein kinase and induces long-term depression at CA3-CA1 synapses in rat hippocampus.
Authors: Scheiderer Et al.
J Neurosci 2008;28:5350
Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors.
Authors: Melis Et al.
J Neurosci 2008;28:13985
Hallucinogens recruit specific cortical 5-HT(2A) receptor-mediated signaling pathways to affect behavior.
Authors: González-Maeso Et al.
J Diabetes Investig 2007;53:439
Rapid estrogenic regulation of extracellular signal- regulated kinase 1/2 signaling in cerebellar granule cells involves a G protein- and protein kinase A-dependent mechanism and intracellular activation of protein phosphatase 2A.
Authors: Belcher Et al.
Differential effects of tyrosine kinase inhibitors on volume-sensitive chloride current in human atrial myocytes: evidence for dual regulation by Src and EGFR kinases.
Authors: Du Et al.
J Gen Physiol 2004;123:427
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