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PP 2

Catalog #: 1407
51 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1407/10
PP 2 | CAS No. 172889-27-9 | Src Family Kinase Inhibitors
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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%

Product Details
Citations (51)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Other Product-Specific Information:

Background References

  1. A novel and essential role for FcgammaRIIa in cancer cell-induced platelet activation.
    Mitrugno A, Williams D, Kerrigan S, Moran N
    Blood, 2013;123(2):249-60.
  2. Loss-of-function mutations in ATP6AP1 and ATP6AP2 in granular cell tumors
    F Pareja, AH Brandes, T Basili, P Selenica, FC Geyer, D Fan, A Da Cruz Pa, R Kumar, DN Brown, R Gularte-Mé, B Alemar, R Bi, RS Lim, I de Bruijn, S Fujisawa, R Gardner, E Feng, A Li, EM da Silva, JR Lozada, P Blecua, L Cohen-Goul, AA Jungbluth, EA Rakha, IO Ellis, MIA Edelweiss, J Palazzo, L Norton, T Hollmann, M Edelweiss, BP Rubin, B Weigelt, JS Reis-Filho
    Nat Commun, 2018;9(1):3533.
  3. GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes.
    Lee E, Sidoryk-Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, Aschner M
    J Biol Chem, 2012;287(32):26817-28.
  4. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
    Bayliss A, Evans P
    PLoS ONE, 2013;8(11):e80833.
  5. A switch role of Src in the biphasic EGF signaling of ER-negative breast cancer cells.
    Zhang, XinTian, Meng, Jun, Wang, Zhao-Yi
    PLoS ONE, 2012;7(8):e41613.
  6. Intrinsic Photosensitivity Enhances Motility of T Lymphocytes

    Sci Rep, 2016;6(0):39479.
  7. Role of focal adhesion tyrosine kinases in GPVI-dependent platelet activation and reactive oxygen species formation.
    Carrim N, Walsh T, Consonni A, Torti M, Berndt M, Metharom P
    PLoS ONE, 2014;9(11):e113679.
  8. CXCL9 causes heterologous desensitization of CXCL12-mediated memory T lymphocyte activation.
    Giegold O, Ogrissek N, Richter C, Schroder M, Herrero San Juan M, Pfeilschifter J, Radeke H
    J Immunol, 2013;190(7):3696-705.
  9. The specificities of protein kinase inhibitors: an update.
    Bain et al.
    Biochem.J., 2003;371:199
  10. Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor.
    Hanke et al.
    J.Biol.Chem., 1996;271:695
  11. Protein kinase inhibitors: the tyrosine-specific protein kinases.
    Lawrence and Niu
    Pharmacol.Ther., 1998;77:81
  12. A role for Src kinase in spontaneous epileptiform activity in the CA3 region of the hippocampus.
    Sanna et al.
    Proc.Natl.Acad.Sci.U.S.A., 2000;97:8653

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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

  1. 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
  2. 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
  3. 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
  4. Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression.
    Authors: Li Et al.
    Theranostics  2017;7:4671
  5. Increased NRG1-ErbB4 signaling in human symptomatic epilepsy.
    Authors: Zhu
    Sci Rep  2017;7(1):141
  6. Mathematical model of early Reelin-induced Src family kinase-mediated signaling.
    Authors: Hass Et al.
    PLoS One  2017;12:e0186927
  7. Estrogen and Progesterone Integration in an in vitro Model of RP3V Kisspeptin Neurons.
    Authors: Mittelman-Smith Et al.
    Neuroendocrinology  2017;106:101
  8. 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
  9. Sonic hedgehog stimulates neurite outgrowth in a mechanical stretch model of reactive-astrogliosis.
    Authors: Berretta Et al.
    Sci Rep  2016;6:21896
  10. 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
  11. 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
  12. Progesterone receptor membrane component-1 regulates hepcidin biosynthesis.
    Authors: Li Et al.
    J Clin Invest  2016;126:389
  13. The prion protein constitutively controls neuronal store-operated Ca(2+) entry through Fyn kinase.
    Authors: Mario Et al.
    Psychoneuroendocrinology  2015;9:416
  14. Extracellular galectin-3 programs multidrug resistance through Na+/K+-ATPase and P-glycoprotein signaling.
    Authors: Harazono Et al.
    PLoS One  2015;6:19592
  15. Anoikis resistance is a critical feature of highly aggressive ovarian cancer cells.
    Authors: Cai Et al.
    J Cell Sci  2015;34:3315
  16. Tyrosine phosphorylation of WIP releases bound WASP and impairs podosome assembly in macrophages.
    Authors: Vijayakumar Et al.
    Front Cell Neurosci  2015;128:251
  17. 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
  18. 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
  19. A role for intracellular zinc in glioma alteration of neuronal chloride equilibrium.
    Authors: Angelantonio Et al.
    Cell Death Dis  2014;5:e1501
  20. Palmitate induces reactive oxygen species production and β-cell dysfunction by activating nicotinamide adenine dinucleotide phosphate oxidase through Src signaling.
    Authors: Sato Et al.
    Carcinogenesis  2014;5:19
  21. 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
  22. BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals.
    Authors: Chen Et al.
    Eur J Neurosci  2014;39:1439
  23. The ShcD signaling adaptor facilitates ligand-independent phosphorylation of the EGF receptor.
    Authors: Wills Et al.
    Mol Biol Cell  2014;25:739
  24. Functional kinomics identifies candidate therapeutic targets in head and neck cancer.
    Authors: Moser Et al.
    Clin Cancer Res  2014;20:4274
  25. Reelin signaling specifies the molecular identity of the pyramidal neuron distal dendritic compartment.
    Authors: Kupferman Et al.
    Neuron  2014;158:1335
  26. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood  2014;123:249
  27. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor.
    Authors: Bayliss and Evans
    PLoS One  2013;8:e80833
  28. Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells.
    Authors: Soltoff and Lannon
    PLoS One  2013;8:e72881
  29. SPIN90 phosphorylation modulates spine structure and synaptic function.
    Authors: Cho Et al.
    Mol Immunol  2013;8:e54276
  30. 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
  31. Src kinase is a direct target of apigenin against UVB-induced skin inflammation.
    Authors: Byun Et al.
    Neuroscience  2013;34:397
  32. 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
  33. Annexin A1, formyl peptide receptor, and NOX1 orchestrate epithelial repair.
    Authors: Leoni Et al.
    J Clin Invest  2013;123:443
  34. Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells.
    Authors: Pham Et al.
    Pancreas  2012;41:1306
  35. β-OE unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus.
    Authors: Nebieridze Et al.
    Oncotarget  2012;37:1845
  36. 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
  37. Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth.
    Authors: Zhou and Too
    Neural Regen Res  2011;6:e21680
  38. 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
  39. 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
  40. 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
  41. 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
  42. Regulation of human cardiac KCNQ1/KCNE1 channel by epidermal growth factor receptor kinase.
    Authors: Dong Et al.
    Biochim Biophys Acta  2010;1798:995
  43. FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation.
    Authors: Grodzki Et al.
    Cell  2009;46:2539
  44. 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
  45. 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
  46. D1/5 receptor-mediated enhancement of LTP requires PKA, Src family kinases, and NR2B-containing NMDARs.
    Authors: Stramiello
    Neuropharmacology  2008;55:871
  47. 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
  48. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors.
    Authors: Melis Et al.
    J Neurosci  2008;28:13985
  49. 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
  50. 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.
    Endocrinology  2005;146:5397
  51. 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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