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说明： Potent, selective Src family kinase inhibitor
化学名： 3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
纯度： ≥99% (HPLC)
生物活性 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.
化合物库 for PP 2
PP 2 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PP 2
| 分子量 | 301.78 |
| 公式 | C15H16ClN5 |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PP 2
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 25 温和加热 | ||
| ethanol | 10 温和加热 |
制备储备液 for PP 2
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for PP 2
参考文献 for PP 2
参考文献是支持产品生物活性的出版物。
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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关键词: PP 2, PP 2 supplier, Potent, selective, Src, inhibitors, inhibits, p56lck, and, p59fynT, Kinases, PP2, 1407, Tocris Bioscience
51 篇 PP 2 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PP 2 的部分引用包括：
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
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
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
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
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
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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Good Src inhibitor.
By
Anonymous on 04/08/2020
分析类型： In Vitro
种属： Human
细胞系/组织： SW480
PP 2 decreased the viability of SW480 cells in a dose-dependent manner by MTS assay.
