PP 2

Pricing Availability   Qty
Cat.No. 1407 - PP 2 | C15H16ClN5 | CAS No. 172889-27-9
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)
Datasheet
Citations (51)
Reviews (1)
Literature (3)

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 also available.

Compound Libraries

PP 2 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25 with gentle warming
ethanol 10 with gentle warming

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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:

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

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

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

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

Stramiello (2008) D1/5 receptor-mediated enhancement of LTP requires PKA, Src family kinases, and NR2B-containing NMDARs. Neuropharmacology 55 871 PMID: 18644393

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

Zhu (2017) Increased NRG1-ErbB4 signaling in human symptomatic epilepsy. Sci Rep 7 141 PMID: 28273943

Li et al (2016) Progesterone receptor membrane component-1 regulates hepcidin biosynthesis. J Clin Invest 126 389 PMID: 26657863

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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.

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