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Description: Potent, selective Src family kinase inhibitor
Chemical Name: 3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥99% (HPLC)
Biological Activity for PP 2
PP 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.
Compound Libraries for PP 2
PP 2 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for PP 2
| M. Wt | 301.78 |
| Formula | C15H16ClN5 |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 172889-27-9 |
| PubChem ID | 4878 |
| InChI Key | PBBRWFOVCUAONR-UHFFFAOYSA-N |
| Smiles | CC(C)(C)N1N=C(C2=C(N)N=CN=C12)C1=CC=C(Cl)C=C1 |
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 2
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25 with gentle warming | ||
| ethanol | 10 with gentle warming |
Preparing Stock Solutions for PP 2
The following data is based on the product molecular weight 301.78. 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 |
|---|---|---|---|
| 0.25 mM | 13.25 mL | 66.27 mL | 132.55 mL |
| 1.25 mM | 2.65 mL | 13.25 mL | 26.51 mL |
| 2.5 mM | 1.33 mL | 6.63 mL | 13.25 mL |
| 12.5 mM | 0.27 mL | 1.33 mL | 2.65 mL |
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Product Datasheets for PP 2
References for PP 2
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
Hanke et al (1996) Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. J.Biol.Chem. 271 695 PMID: 8557675
Lawrence and Niu (1998) Protein kinase inhibitors: the tyrosine-specific protein kinases. Pharmacol.Ther. 77 81 PMID: 9578319
Sanna et al (2000) A role for Src kinase in spontaneous epileptiform activity in the CA3 region of the hippocampus. Proc.Natl.Acad.Sci.U.S.A. 97 8653 PMID: 10890901
If you know of a relevant reference for PP 2, please let us know.
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Keywords: PP 2, PP 2 supplier, Potent, selective, Src, inhibitors, inhibits, p56lck, and, p59fynT, Kinases, PP2, 1407, Tocris Bioscience
51 Citations for PP 2
Citations are publications that use Tocris products. Selected citations for PP 2 include:
Poli et al (2018) Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors. J Enzyme Inhib Med Chem 33 956 PMID: 29747534
Mittelman-Smith et al (2017) Estrogen and Progesterone Integration in an in vitro Model of RP3V Kisspeptin Neurons. Neuroendocrinology 106 101 PMID: 28384629
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481
Moser et al (2014) Functional kinomics identifies candidate therapeutic targets in head and neck cancer. Clin Cancer Res 20 4274 PMID: 25125259
Wills et al (2014) The ShcD signaling adaptor facilitates ligand-independent phosphorylation of the EGF receptor. Mol Biol Cell 25 739 PMID: 24430869
Mitrugno et al (2014) A novel and essential role for FcγRIIa in cancer cell-induced platelet activation. Blood 123 249 PMID: 24258815
Byun et al (2013) Src kinase is a direct target of apigenin against UVB-induced skin inflammation. Neuroscience 34 397 PMID: 23161610
Cho et al (2013) SPIN90 phosphorylation modulates spine structure and synaptic function. Mol Immunol 8 e54276 PMID: 23342115
Ivanova et al (2011) Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites. FASEB J 25 1402 PMID: 21233487
Zhang et al (2011) Genistein and tyrphostin AG556 inhibit inwardly-rectifying Kir2.1 channels expressed in HEK 293 cells via protein tyrosine kinase inhibition. Biochim Biophys Acta 1808 1993 PMID: 21570948
Zhang et al (2011) Epidermal growth factor receptor tyrosine kinase regulates the human inward rectifier potassium K(IR)2.3 channel, stably expressed in HEK 293 cells. Br J Pharmacol 164 1469 PMID: 21486282
Kupferman et al (2014) Reelin signaling specifies the molecular identity of the pyramidal neuron distal dendritic compartment. Neuron 158 1335 PMID: 25201528
Rosas et al (2014) Long-term treatment with PP2 after spinal cord injury resulted in functional locomotor recovery and increased spared tissue. PLoS One 9 2164 PMID: 25657738
Sato et al (2014) Palmitate induces reactive oxygen species production and β-cell dysfunction by activating nicotinamide adenine dinucleotide phosphate oxidase through Src signaling. Carcinogenesis 5 19 PMID: 24843732
Vliet et al (2013) 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). J Biol Chem 288 27519 PMID: 23918927
Leoni et al (2013) Annexin A1, formyl peptide receptor, and NOX1 orchestrate epithelial repair. J Clin Invest 123 443 PMID: 23241962
Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor. PLoS One 8 e80833 PMID: 24265838
Mobasher et al (2013) Protein tyrosine phosphatase 1B modulates GSK3β/Nrf2 and IGFIR signaling pathways in acetaminophen-induced hepatotoxicity. Cell Death Dis 4 e626 PMID: 23661004
Soltoff and Lannon (2013) Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells. PLoS One 8 e72881 PMID: 24009711
Zhou and Too (2011) Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth. Neural Regen Res 6 e21680 PMID: 21738764
Grodzki et al (2009) FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation. Cell 46 2539 PMID: 19540596
Zhu (2017) Increased NRG1-ErbB4 signaling in human symptomatic epilepsy. Sci Rep 7 141 PMID: 28273943
Bigford et al (2012) 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization. J Biol Chem 287 11049 PMID: 22291020
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
Deuretzbacher et al (2009) Beta1 integrin-dependent engulfment of Yersinia enterocolitica by macrophages is coupled to the activation of autophagy and suppressed by type III protein secretion. J Immunol 183 5847 PMID: 19812190
Li et al (2017) Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression. Theranostics 7 4671 PMID: 29187895
Walko et al (2017) A genome-wide screen identifies YAP/WBP2 interplay conferring growth advantage on human epidermal stem cells. Nat Commun 8 14744 PMID: 28332498
Hass et al (2017) Mathematical model of early Reelin-induced Src family kinase-mediated signaling. PLoS One 12 e0186927 PMID: 29049379
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
Berretta et al (2016) Sonic hedgehog stimulates neurite outgrowth in a mechanical stretch model of reactive-astrogliosis. Sci Rep 6 21896 PMID: 26902390
Li et al (2016) Progesterone receptor membrane component-1 regulates hepcidin biosynthesis. J Clin Invest 126 389 PMID: 26657863
Töyli et al (2010) 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. Lab Invest 90 915 PMID: 20212454
Cai et al (2015) Anoikis resistance is a critical feature of highly aggressive ovarian cancer cells. J Cell Sci 34 3315 PMID: 25132267
Vijayakumar et al (2015) Tyrosine phosphorylation of WIP releases bound WASP and impairs podosome assembly in macrophages. Front Cell Neurosci 128 251 PMID: 25413351
Mario et al (2015) The prion protein constitutively controls neuronal store-operated Ca(2+) entry through Fyn kinase. Psychoneuroendocrinology 9 416 PMID: 26578881
Harazono et al (2015) Extracellular galectin-3 programs multidrug resistance through Na+/K+-ATPase and P-glycoprotein signaling. PLoS One 6 19592 PMID: 26158764
Joshi et al (2014) Heat shock protein 90 inhibitors prevent LPS-induced endothelial barrier dysfunction by disrupting RhoA signaling. Am J Respir Cell Mol Biol 50 170 PMID: 23972231
Pham et al (2012) Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells. Pancreas 41 1306 PMID: 22889981
Dong et al (2010) Regulation of human cardiac KCNQ1/KCNE1 channel by epidermal growth factor receptor kinase. Biochim Biophys Acta 1798 995 PMID: 20085748
Dandoulaki et al (2018) Src activation by Chk1 promotes actin patch formation and prevents chromatin bridge breakage in cytokinesis. J Cell Biol 217 3071 PMID: 29954829
Chen et al (2014) BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals. Eur J Neurosci 39 1439 PMID: 24611998
Angelantonio et al (2014) A role for intracellular zinc in glioma alteration of neuronal chloride equilibrium. Cell Death Dis 5 e1501 PMID: 25356870
Delaney and Crane (2016) Presynaptic GABAB receptors reduce transmission at parabrachial synapses in the lateral central amygdala by inhibiting N-type calcium channels. Sci Rep 6 19255 PMID: 26755335
Wang et al (2016) Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2. Br J Pharmacol 173 3342 PMID: 27638545
Nebieridze et al (2012) β-OE unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus. Oncotarget 37 1845 PMID: 22541715
Belcher et al (2005) 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. Endocrinology 146 5397 PMID: 16123167
González-Maeso et al (2007) Hallucinogens recruit specific cortical 5-HT(2A) receptor-mediated signaling pathways to affect behavior. J Diabetes Investig 53 439 PMID: 17270739
Stramiello (2008) D1/5 receptor-mediated enhancement of LTP requires PKA, Src family kinases, and NR2B-containing NMDARs. Neuropharmacology 55 871 PMID: 18644393
Melis et al (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors. J Neurosci 28 13985 PMID: 19091987
Scheiderer et al (2008) 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. J Neurosci 28 5350 PMID: 18480291
Du et al (2004) Differential effects of tyrosine kinase inhibitors on volume-sensitive chloride current in human atrial myocytes: evidence for dual regulation by Src and EGFR kinases. J Gen Physiol 123 427 PMID: 15024039
Do you know of a great paper that uses PP 2 from Tocris? Please let us know.
Reviews for PP 2
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Good Src inhibitor.
By
Anonymous on 04/08/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: SW480
PP 2 decreased the viability of SW480 cells in a dose-dependent manner by MTS assay.
