Catalog Number: 1407
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:
  • Formula:
  • Solubility:
    Soluble to 25 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
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.
Additional Information
Other Product-Specific Information:
Background References
  1. The specificities of protein kinase inhibitors: an update.
    Bain et al.
    Biochem.J., 2003;371:199
  2. Protein kinase inhibitors: the tyrosine-specific protein kinases.
    Lawrence and Niu
    Pharmacol.Ther., 1998;77:81
  3. Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor.
    Hanke et al.
    J.Biol.Chem., 1996;271:695
  4. 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

The citations listed below are publications that use Tocris products. Selected citations for PP 2 include:

Showing Results 1 - 10 of 32

  1. 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
  2. The prion protein constitutively controls neuronal store-operated Ca(2+) entry through Fyn kinase.
    Authors: Mario Et al.
  3. Extracellular galectin-3 programs multidrug resistance through Na+/K+-ATPase and P-glycoprotein signaling.
    Authors: Harazono Et al.
    PLoS One
  4. Anoikis resistance is a critical feature of highly aggressive ovarian cancer cells.
    Authors: Cai Et al.
    J Cell Sci
  5. Tyrosine phosphorylation of WIP releases bound WASP and impairs podosome assembly in macrophages.
    Authors: Vijayakumar Et al.
    Front Cell Neurosci
  6. 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
  7. Long-term treatment with PP2 after spinal cord injury resulted in functional locomotor recovery and increased spared tissue.
    Authors: Rosas Et al.
    PLoS One
  8. Palmitate induces reactive oxygen species production and β-cell dysfunction by activating nicotinamide adenine dinucleotide phosphate oxidase through Src signaling.
    Authors: Sato Et al.
  9. The ShcD signaling adaptor facilitates ligand-independent phosphorylation of the EGF receptor.
    Authors: Wills Et al.
    Mol Biol Cell
  10. Functional kinomics identifies candidate therapeutic targets in head and neck cancer.
    Authors: Moser Et al.
    Clin Cancer Res
  11. Reelin signaling specifies the molecular identity of the pyramidal neuron distal dendritic compartment.
    Authors: Kupferman Et al.
  12. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
  13. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
    Authors: Bayliss and Evans
    PLoS One
  14. Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells.
    Authors: Soltoff and Lannon
    PLoS One
  15. SPIN90 phosphorylation modulates spine structure and synaptic function.
    Authors: Cho Et al.
    Mol Immunol
  16. Protein tyrosine phosphatase 1B modulates GSK3β/Nrf2 and IGFIR signaling pathways in acetaminophen-induced hepatotoxicity.
    Authors: Mobasher Et al.
    Cell Death Dis
  17. Src kinase is a direct target of apigenin against UVB-induced skin inflammation.
    Authors: Byun Et al.
  18. 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
  19. Annexin A1, formyl peptide receptor, and NOX1 orchestrate epithelial repair.
    Authors: Leoni Et al.
    J Clin Invest
  20. Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells.
    Authors: Pham Et al.
  21. β-Estradiol unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus.
    Authors: Nebieridze Et al.
  22. Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth.
    Authors: Zhou and Too
    Neural Regen Res
  23. 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.
  24. 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
  25. 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
  26. Regulation of human cardiac KCNQ1/KCNE1 channel by epidermal growth factor receptor kinase.
    Authors: Dong Et al.
    Biochim Biophys Acta
  27. FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation.
    Authors: Grodzki Et al.
  28. 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
  29. 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
  30. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors.
    Authors: Melis Et al.
    J Neurosci
  31. Hallucinogens recruit specific cortical 5-HT(2A) receptor-mediated signaling pathways to affect behavior.
    Authors: González-Maeso Et al.
    J Diabetes Investig
  32. 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.
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