POM 1
(Synonyms: 聚钨酸钠,Sodium polyoxotungstate; POM-1) 目录号 : GC17027
POM 1是一种核苷三磷酸二磷酸水解酶（NTPDase）抑制剂，对NTPDase1（CD39）、NTPDase3和NTPDase2的Ki值分别为2.58μM、3.26μM和28.8μM。
Cas No.:12141-67-2
Sample solution is provided at 25 µL, 10mM.
POM 1 is a nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor with Ki values of 2.58μM, 3.26μM and 28.8μM for NTPDase1 (CD39), NTPDase3 and NTPDase2, respectively[1]. POM 1 can inhibit ATP decomposition, but also blocks central synaptic transmission, an effect that is independent of NTPDase inhibition[2]. POM 1 is an inorganic compound that can be used to make heavy liquids and is widely used for density separation[3].
In vitro, POM 1 (100μM) treatment of macrophages for 24h inhibited intracellular ectonucleotidase activity, inhibited the increase in intracellular free Ca2+ caused by nucleotides, inhibited ATP-induced P2X7-related cell pyroptosis, and inhibited LPS-induced NO production[4]. POM 1 (5μM) treatment of H1299 and A549 cells for 24h significantly increased lipid peroxide levels and increased the expression of ferroptosis-related proteins[5].
In vivo, intraperitoneal injection of POM 1 (5mg/kg) in multiple myeloma (MM) model mice significantly reduced spleen weight and the number of tumor cells in the spleen[6]. Intraperitoneal injection of POM 1 (250μg) in CD39-deficient and wild-type mice significantly increased the number of natural killer (NK) cells and enhanced effector function[7].
References:
[1] Müller C E, Iqbal J, Baqi Y, et al. Polyoxometalates—a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors[J]. Bioorganic & medicinal chemistry letters, 2006, 16(23): 5943-5947.
[2] Wall M J, Wigmore G, Lopatář J, et al. The novel NTPDase inhibitor sodium polyoxotungstate (POM-1) inhibits ATP breakdown but also blocks central synaptic transmission, an action independent of NTPDase inhibition[J]. Neuropharmacology, 2008, 55(7): 1251-1258.
[3] Savage N M. The use of sodium polytungstate for conodont separations[J]. Journal of Micropalaeontology, 1988, 7(1): 39-40.
[4] Pimenta-dos-Reis G, Torres E J L, Quintana P G, et al. POM-1 inhibits P2 receptors and exhibits anti-inflammatory effects in macrophages[J]. Purinergic Signalling, 2017, 13: 611-627.
[5] Lin J W, Zhou Y, Xiao H P, et al. Antitumor effects of a Sb-rich polyoxometalate on non-small-cell lung cancer by inducing ferroptosis and apoptosis[J]. Chemical Science, 2024, 15(37): 15367-15376.
[6] Yang R, Elsaadi S, Misund K, et al. Conversion of ATP to adenosine by CD39 and CD73 in multiple myeloma can be successfully targeted together with adenosine receptor A2A blockade[J]. Journal for immunotherapy of cancer, 2020, 8(1).
[7] Zhang H, Vijayan D, Li X Y, et al. The role of NK cells and CD39 in the immunological control of tumor metastases[J]. Oncoimmunology, 2019, 8(6): e1593809.
POM 1是一种核苷三磷酸二磷酸水解酶（NTPDase）抑制剂，对NTPDase1（CD39）、NTPDase3和NTPDase2的Ki值分别为2.58μM、3.26μM和28.8μM[1]。POM 1能够抑制ATP分解，但也会阻断中枢突触传递，这种作用与NTPDase抑制无关[2]。POM 1是一种无机化合物，能够用于制造重质液体，广泛用于密度分离[3]。
在体外，POM 1（100μM）处理巨噬细胞24h，抑制了细胞内的外核苷酸酶活性，抑制了核苷酸引起的细胞内的游离Ca2+增加，抑制了ATP诱导的P2X7相关细胞焦亡，抑制了LPS诱导的NO产生[4]。POM 1（5μM）处理H1299和A549细胞24h，显著升高了脂质过氧化物水平，增加了铁死亡相关蛋白的表达[5]。
在体内，POM 1（5mg/kg）通过腹腔注射处理多发性骨髓瘤（MM）模型小鼠，显著减轻了脾脏重量，减少了脾脏中的肿瘤细胞数量[6]。POM 1（250μg）通过腹腔注射治疗CD39缺陷型和野生型小鼠，显著增加了自然杀伤（NK）细胞数量，增强了效应功能[7]。
| Cell experiment [1]: | |
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Cell lines |
Macrophages |
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Preparation Method |
Macrophages (5×105/well plated in 96-well plates) were treated or not with LPS (at the concentrations indicated) for 24h, with or without of 100μM POM 1. After this time, the culture supernatants were collected for measurement of the amount of nitrite using the Griess colorimetric method. |
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Reaction Conditions |
100μM; 24h |
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Applications |
POM-1 inhibits LPS-induced NO production. |
| Animal experiment [2]: | |
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Animal models |
C57BL/KalwRij mice |
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Preparation Method |
Mice were injected intravenously on day 0 with 2×105 5T33 MM cells and treated intraperitoneally with 10mg/kg monoclonal anti-CD73 antibody on days 2, 4, 8, 11, 15, and 18. Of note, 5mg/kg of POM 1 was injected intraperitoneally once per day from 0 to day 4, day 7-11, and day 14-18. Number of tumor cells in the spleen was determined using FACS analysis. |
|
Dosage form |
5mg/kg; i.p. |
|
Applications |
Mice treated with the CD39 inhibitor POM 1 had significantly reduced spleen weight and fewer tumor cells in the spleen. |
|
References: |
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| Cas No. | 12141-67-2 | SDF | |
| 别名 | 聚钨酸钠,Sodium polyoxotungstate; POM-1 | ||
| Canonical SMILES | [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].O.[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O].[O-].[O-].[O-].[O-].[O-].[O-].[W].[W].[W].[W].[W].[W].[W].[W].[W].[W].[W].[W] | ||
| 分子式 | H2O40Na6W12 | 分子量 | 2986.01 |
| 溶解度 | ≥ 149.3mg/mL in DMSO with ultrasonic ≥50mg/mL in Water |
储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.3349 mL | 1.6745 mL | 3.349 mL |
| 5 mM | 0.067 mL | 0.3349 mL | 0.6698 mL |
| 10 mM | 0.0335 mL | 0.1674 mL | 0.3349 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Purity: >98.00%
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