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Submit ReviewPP 1 is a potent inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl.
分子量 | 281.36 |
公式 | C16H19N5 |
储存 | Desiccate at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 172889-26-8 |
PubChem ID | 1400 |
InChI Key | ZVPDNRVYHLRXLX-UHFFFAOYSA-N |
Smiles | CC1=CC=C(C=C1)C1=NN(C2=NC=NC(N)=C12)C(C)(C)C |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 10 | ||
ethanol | 10 |
以下数据基于产品分子量 281.36。 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 |
---|---|---|---|
0.1 mM | 35.54 mL | 177.71 mL | 355.42 mL |
0.5 mM | 7.11 mL | 35.54 mL | 71.08 mL |
1 mM | 3.55 mL | 17.77 mL | 35.54 mL |
5 mM | 0.71 mL | 3.55 mL | 7.11 mL |
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
Carlomagno et al (2002) The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes. Cancer Res. 62 1077 PMID: 11861385
Hanke et al (1996) Discovery of a novel, potent, and src family-selective tyrosine kinase inhibitor. J.Biol.Chem. 271 695 PMID: 8557675
Liu et al (1999) Structural basis for selective inhibition of Src family kinases by PP1. Chem.Biol. 6 671 PMID: 10467133
Tatton et al (2003) The src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases. J.Biol.Chem. 278 4847 PMID: 12475982
If you know of a relevant reference for PP 1, please let us know.
关键词: PP 1, PP 1 supplier, Potent, selective, Src, inhibitors, inhibits, Lyn, p56lck, p59fynT, Kinases, PP1, 1397, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PP 1 的部分引用包括:
Koutsioumpa et al (2015) Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor. Front Syst Neurosci 14 19 PMID: 25644401
Pham et al (2012) Apigenin inhibits NNK-induced focal adhesion kinase activation in pancreatic cancer cells. Pancreas 41 1306 PMID: 22889981
Kurz et al (2019) Role of ceramide synthase 2 in G-CSF signaling and G-CSF-R translocation into detergent-resistant membranes. Sci Rep 9 747 PMID: 30679689
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Ferland et al (2017) Chemerin-induced arterial contraction is Gi- and calcium-dependent. Vascul Pharmacol 88 30 PMID: 27890480
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
Mace et al (2016) Human NK cell development requires CD56-mediated motility and formation of the developmental synapse. Nat Commun 7 12171 PMID: 27435370
Eum et al (2009) NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells. Toxicol Appl Pharmacol 240 299 PMID: 19632255
Alonso-Magdalena et al Pancreatic Ins content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069 PMID: 18446233
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
Mikelis et al (2009) Integrin alpha(v)beta(3) is a pleiotrophin receptor required for pleiotrophin-induced endothelial cell migration through receptor protein tyrosine phosphatase beta/zeta. FASEB J 23 1459 PMID: 19141530
Zhang et al (2007) SRC-family kinases are activated in non-small cell lung cancer and promote the survival of epidermal growth factor receptor-dependent cell lines. Mol Cancer 170 366 PMID: 17200208
Lee et al (2007) Transforming growth factor-beta1 effects on endothelial monolayer permeability involve focal adhesion kinase/Src. Am J Respir Cell Mol Biol 37 485 PMID: 17585111
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