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Submit ReviewPOM 1 is an inhibitor of Ecto-NTPDases that displays minor selectivity for NTPDases 1 and 2 over NTPDase 3 and P2Y12 (Ki values are 2.58, 3.26, > 10 and 28.8 μM for NTPDase 1, NTPDase 3, P2Y12 and NTPDase 2 respectively). Abolishes renal protection induced by ischemic preconditioning. Inhibits synaptic transmission at hippocampal CA1 pyramidal synapses and at the cerebellar parallel fiber-Purkinje cell (PF) synapse.
分子量 | 2986.01 |
公式 | H2O40Na6W12 |
储存 | Store at RT |
CAS Number | 12141-67-2 |
PubChem ID | 71311259 |
InChI Key | YVQUUPJGDSQKML-UHFFFAOYSA-N |
Smiles | O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.O=[W](=O)=O.[O-][W]([O-])(=O)=O.[O-][W]([O-])(=O)=O.[O-][W]([O-])(=O)=O |
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 | |||
water | 298.6 | 100 |
以下数据基于产品分子量 2986.01。 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 |
---|---|---|---|
1 mM | 0.33 mL | 1.67 mL | 3.35 mL |
5 mM | 0.07 mL | 0.33 mL | 0.67 mL |
10 mM | 0.03 mL | 0.17 mL | 0.33 mL |
50 mM | 0.01 mL | 0.03 mL | 0.07 mL |
参考文献是支持产品生物活性的出版物。
Muller et al (2006) Polyoxometalates - a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors. Bioorg.Med.Chem.Lett. 16 5943 PMID: 16997558
Grenz et al (2007) Contribution of E-NTPDase1 (CD39) to renal protection from ischemia-reperfusion injury. FASEB J. 21 2863 PMID: 17442731
Wall et al (2008) The novel NTPDase inhibitor sodium polyoxotungstate (POM-1) inhibits ATP breakdown but also blocks central synaptic transmission, an action independent of NTPDase inhibition. 55 1251 PMID: 18768144
If you know of a relevant reference for POM 1, please let us know.
关键词: POM 1, POM 1 supplier, inhibitors, inhibits, E-NTPDases, ATPases, POM1, Sodium, polyoxotungstate, NTPDase, 2689, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 POM 1 的部分引用包括:
Aho et al (2016) Extracellular ATP protects endothelial cells against DNA damage. Purinergic Signal 12 575 PMID: 27030122
Yegutkin et al (2012) Metabolism of circulating ADP in the bloodstream is mediated via integrated actions of soluble adenylate kinase-1 and NTPDase1/CD39 activities. FASEB J 26 3875 PMID: 22637533
Hirata et al (2018) CD150high Bone Marrow Tregs Maintain Hematopoietic Stem Cell Quiescence and Immune Privilege via Adenosine. Cell Stem Cell 22 445 PMID: 29456159
Sassi et al (2014) Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation. J Clin Invest 124 5385 PMID: 25401477
Ohradanova-Repic et al (2018) Extracellular purine metabolism is the switchboard of immunosuppressive macrophages and a novel target to treat diseases with macrophage imbalances. Front Immunol 9 852 PMID: 29780382
Crittenden et al (2018) Purine metabolism controls innate lymphoid cell function and protects against intestinal injury. Immunol Cell Biol 96 1049 PMID: 29758102
Del Papa et al (2016) The NOTCH1/CD39 axis: a Treg trip-switch for GvHD. Leukemia 30 1931 PMID: 27125307
Fang et al (2016) Expression of CD39 on activated T cells impairs their survival in older individuals. Cell Rep. 14 1218 PMID: 26832412
Rao et al (2014) A dual role for autophagy in a murine model of lung cancer. Cancer Biol Ther 5 3056 PMID: 24445999
Alvarez-Sanchez et al (2019) Peripheral CD39-expressing T regulatory cells are increased and associated with relapsing-remitting multiple sclerosis in relapsing patients. Sci Rep 9 2302 PMID: 30783191
Burr and Parekkadan (2019) Kinetics of MSC-based enzyme therapy for immunoregulation. J Transl Med 17 263 PMID: 31409424
Pinheiro et al (2013) Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation. Cell Commun Signal 11 70 PMID: 24047499
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Human PBMCs were incubated with 10 μM POM-1 for 30 minutes to inhibit CD39 ATPase activity. POM-1 caused a 80% inhibition of PBMCs ATPase activity.
PBMCs were isolated from healthy subjects and from multiple sclerosis patients and CD39 activity was measured by the Malachite Green Phosphate Assay. Cells were washed in phosphate-free buffer and incubated with ATP (250 μM) for 30 minutes at 37ºC. To selectively assess CD39 ATPase activity, POM-1 (10 μM) was added while cells were incubated with ATP.