Enpp-1-IN-1
(Synonyms: N-4-(7-Methoxyquinolin-4-yl)benzylsulfamide, MV 658, UUN28589) 目录号 : GC38775
Enpp-1-IN-1是一种有效的选择性Ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1)抑制剂。
Cas No.:2289728-58-9
Sample solution is provided at 25 µL, 10mM.
Enpp-1-IN-1 is a potent and selective ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor[1-2]. Enpp-1-IN-1 is primarily employed in research to explore tumor immunotherapy[3].
In vitro, treatment of various RAS-mutant cancer cell lines (such as A549, H460, and H2030) with Enpp-1-IN-1 (11 or 33μM) for 72–96 hours significantly inhibits cell viability and proliferation[4]. Treating peripheral blood mononuclear cells (PBMCs) derived from small cell lung cancer (SCLC) patients with Enpp-1-IN-1 (2μM) for 72 hours significantly upregulates the mRNA expression levels of STING, MAVS, and IFI16[6].
References:
[1] Ji H, Jiang W, Zhang J, et al. ENPP1 governs the metabolic regulation of effector T cells in autoimmunity by detecting cytosolic mitochondrial DNA. Cell Rep. 2025 Jun 24;44(6):115851.
[2] Liu Q, Wang R, Hou S, et al. Chondrocyte-derived exosomes promote cartilage calcification in temporomandibular joint osteoarthritis. Arthritis Res Ther. 2022 Feb 14;24(1):44.
[3] Ng DYX, Li Z, Lee E, et al. Therapeutic and immunomodulatory potential of pazopanib in malignant phyllodes tumor. NPJ Breast Cancer. 2022 Apr 1;8(1):44.
[4] Xia RX, Zou PC, Xie JT, et al. Dependence of NPPS creates a targetable vulnerability in RAS-mutant cancers. Acta Pharmacol Sin. 2025 Mar;46(3):728-739. doi: 10.1038/s41401-024-01409-2.
[5] De Rosa C, Morgillo F, Amato L, et al. DNA-PK inhibition sustains the antitumor innate immune response in small cell lung cancer. iScience. 2025 Feb 1;28(3):111943.
Enpp-1-IN-1是一种有效的选择性Ectonucleotide pyrophosphatase-phosphodiesterase 1(enpp-1)抑制剂[1-2]。Enpp-1-IN-1主要被运用于探索肿瘤免疫治疗的相关研究[3]。
在体外,Enpp-1-IN-1(11–33μM)处理多种RAS突变癌细胞(如A549、H460、H2030等)72–96小时,可显著抑制细胞活力与增殖[4]。Enpp-1-IN-1(2μM)处理小细胞肺癌(SCLC)患者来源的外周血单个核细胞(PBMCs)72小时,Enpp-1-IN-1可显著上调STING、MAVS和IFI16的mRNA表达水平[5]。
| Cell experiment [1]: | |
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Cell lines |
A panel of human cancer cell lines (including A549, H460, HCT116, SW480, etc.) and normal lung epithelial cells (BEAS-2B) |
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Preparation Method |
Cells were propagated in respective media (DMEM, F-12K, McCoy’s 5a, or RPMI-1640) supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin at 37°C, 5% CO₂. Cells were treated with Enpp-1-IN-1 at 11μM or 33μM for 72–96 hours. |
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Reaction Conditions |
11μM or 33μM for 72–96h |
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Applications |
Enpp-1-IN-1 selectively suppressed viability and growth of RAS-mutant cancer cells while exhibiting minimal effects on normal cells (BEAS-2B) or RAS-wildtype cells (HCC827). Enpp-1-IN-1 impaired hexokinase activity by disrupting the NPPS-HK1 interaction, leading to reduced glycolysis and accumulation of glucose-6-phosphate. |
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References: |
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| Cas No. | 2289728-58-9 | SDF | |
| 别名 | N-4-(7-Methoxyquinolin-4-yl)benzylsulfamide, MV 658, UUN28589 | ||
| Canonical SMILES | O=S(N)(NCC1=CC=C(C2=CC=NC3=CC(OC)=CC=C23)C=C1)=O | ||
| 分子式 | C17H17N3O3S | 分子量 | 343.4 |
| 溶解度 | DMSO: 250 mg/mL (728.01 mM) | 储存条件 | Store at -20°C |
| 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 | 2.9121 mL | 14.5603 mL | 29.1206 mL |
| 5 mM | 582.4 μL | 2.9121 mL | 5.8241 mL |
| 10 mM | 291.2 μL | 1.456 mL | 2.9121 mL |
| 第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
| 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 | ||||||||||
计算结果:
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,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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