PP 2

Cat. No. 1407

PP 2 C15H16ClN5 [172889-27-9]

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Chemical Name: 3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Biological Activity

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 PP 3 (Cat. No. 2794) also available.

Technical Data

M.Wt:
301.78
Formula:
C15H16ClN5
Solubility:
Soluble to 25 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
172889-27-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199. PMID: 12534346.

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.

Lawrence and Niu (1998) Protein kinase inhibitors: the tyrosine-specific protein kinases. Pharmacol.Ther. 77 81. PMID: 9578319.

Hanke et al (1996) Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. J.Biol.Chem. 271 695. PMID: 8557675.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PP 2 include:

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.

Cai et al (2015) Anoikis resistance is a critical feature of highly aggressive ovarian cancer cells. J Cell Sci 34 3315. PMID: 25132267.

Harazono et al (2015) Extracellular galectin-3 programs multidrug resistance through Na+/K+-ATPase and P-glycoprotein signaling. PLoS One 6 19592. PMID: 26158764.

Mario et al (2015) The prion protein constitutively controls neuronal store-operated Ca(2+) entry through Fyn kinase. Psychoneuroendocrinology 9 416. PMID: 26578881.

Vijayakumar et al (2015) Tyrosine phosphorylation of WIP releases bound WASP and impairs podosome assembly in macrophages. Front Cell Neurosci 128 251. PMID: 25413351.

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.

Kupferman et al (2014) Reelin signaling specifies the molecular identity of the pyramidal neuron distal dendritic compartment. Neuron 158 1335. PMID: 25201528.

Mitrugno et al (2014) A novel and essential role for FcγRIIa in cancer cell-induced platelet activation. Blood 123 249. PMID: 24258815.

Moser et al (2014) Functional kinomics identifies candidate therapeutic targets in head and neck cancer. Clin Cancer Res 20 4274. PMID: 25125259.

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.

Wills et al (2014) The ShcD signaling adaptor facilitates ligand-independent phosphorylation of the EGF receptor. Mol Biol Cell 25 739. PMID: 24430869.

Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor. PLoS One 8 e80833. PMID: 24265838.

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.

Leoni et al (2013) Annexin A1, formyl peptide receptor, and NOX1 orchestrate epithelial repair. J Clin Invest 123 443. PMID: 23241962.

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.

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.

Nebieridze et al (2012) β-Estradiol unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus. Oncotarget 37 1845. PMID: 22541715.

Pham et al (2012) Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells. Pancreas 41 1306. PMID: 22889981.

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.

Zhou and Too (2011) Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth. Neural Regen Res 6 e21680. PMID: 21738764.

Dong et al (2010) Regulation of human cardiac KCNQ1/KCNE1 channel by epidermal growth factor receptor kinase. Biochim Biophys Acta 1798 995. PMID: 20085748.

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.

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.

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.

Melis et al (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors. J Neurosci 28 13985. PMID: 19091987.

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.

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.

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Keywords: PP 2, supplier, Potent, selective, Src, inhibitors, inhibits, p56lck, and, p59fynT, Kinases, PP2, Tocris Bioscience, Src Kinase Inhibitor products

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