EB-3D
Based on 2 publication(s) in Google Scholar
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
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- 純度: 99.64%
- CAS 番号: 1839150-63-8
- 分子式: C30H36Br2N4O2
- 分子量:644.44
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
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PI3K/Akt/mTOR Compound Library
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Anti-Cancer Compound Library
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Oxygen Sensing Compound Library
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Endoplasmic Reticulum Stress Compound Library
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MedChemExpress（MCE）の使用を引用している文献 EB-3D
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生物活性
IC50: 1 μM; Kd: 0.7 μM[3]
EB-3D displays (0-100 μM; 72 hours) excellent antiproliferative activity against a wide cohort of T-leukemic cell lines, with GI GI50s 13 values in the nanomolar range[1].
EB-3D (1.25-5μM; 24 hours) induced apoptosis in leukemia cell lines[1].
EB-3D (0.5-1 μM; 24 hours) induces a G0/G1 arrest that lead to apoptosis[1].
EB-3D (0.3 μM; 48 hours) shows a first spike of activation of AMPKα after 30 minutes and a later increase in the phosphorylation of T172[1].
EB-3D (1-40 μM; 48 hours) inhibits cell growth in HepG2 cells with a GI50 of 14.55 μM[2].
EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells
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Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:72 hours
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Result:Inhibited JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, and ALL-SIL cells growth with GI50s of 136.2, 478.8, 17.7, 0.9, 60.6, 200, 265, and 132 nM, respectively.
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Cell Line:Jurkat, CCRF-CEM and HSB-2 cells
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:24 hours
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Result:Induced apoptosis in leukemia cell lines.
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Cell Line:Jurkat, CCRF-CEM and HSB-2 cells
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Concentration:0.5, 1 μM
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Incubation Time:24 hours
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Result:Induces cell cycle arrest in G0/G1 phase.
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Cell Line:Jurkat cells
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Concentration:0.3 μM
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Incubation Time:48 hours
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Result:Showed a first spike of activation of AMPKα after 30 minutes of treatment and a later increase in the phosphorylation of T172. The increase in S79 phosphorylation of its main target ACC (acetyl-coenzyme A (CoA) carboxylase), followed the same pattern. This rapid activation of AMPK, in turn induced a consequent reduction in mTOR phosphorylation that is visible already at 30’ and that becomes amplified at longer time probably due to the interruption of feedback loops that are characteristic of mTOR connecting pathways.
EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:E0771-C57BL/6 mice[4]
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Dosage:I.p.; every other day for 4 weeks
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Administration:2.5 mg/kg
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Result:A reduction of the number of spontaneous lung macro- and micrometastasis.
化学情報
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CAS 番号 1839150-63-8
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性状 Solid
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分子量 644.44
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分子式 C30H36Br2N4O2
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Color White to off-white
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SMILES
CN(C1=CC=[N+](CC2=CC=C(OCCOC3=CC=C(C[N+]4=CC=C(N(C)C)C=C4)C=C3)C=C2)C=C1)C.[Br-].[Br-]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 50 mg/mL (77.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 9.09 mg/mL (14.11 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Mariotto E, et al. EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. Biochem Pharmacol. 2018 Sep;155:213-223. [Content Brief]
[2]. Sola-Leyva A, et al. Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells. Sci Rep. 2019 Mar 25;9(1):5109. [Content Brief]
[3]. Schiaffino-Ortega S, et al. Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human Choline Kinase α1 (ChoKα1). [Content Brief]
[4]. Mariotto E, et al. Choline Kinase Alpha Inhibition by EB-3D Triggers Cellular Senescence, Reduces Tumor Growth and Metastatic Dissemination in Breast Cancer. Cancers (Basel). 2018;10(10):391. Published 2018 Oct 22. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.5517 mL | 7.7587 mL | 15.5173 mL | 38.7934 mL |
| 5 mM | 0.3103 mL | 1.5517 mL | 3.1035 mL | 7.7587 mL | |
| 10 mM | 0.1552 mL | 0.7759 mL | 1.5517 mL | 3.8793 mL | |
| DMSO | 15 mM | 0.1034 mL | 0.5172 mL | 1.0345 mL | 2.5862 mL |
| 20 mM | 0.0776 mL | 0.3879 mL | 0.7759 mL | 1.9397 mL | |
| 25 mM | 0.0621 mL | 0.3103 mL | 0.6207 mL | 1.5517 mL | |
| 30 mM | 0.0517 mL | 0.2586 mL | 0.5172 mL | 1.2931 mL | |
| 40 mM | 0.0388 mL | 0.1940 mL | 0.3879 mL | 0.9698 mL | |
| 50 mM | 0.0310 mL | 0.1552 mL | 0.3103 mL | 0.7759 mL | |
| 60 mM | 0.0259 mL | 0.1293 mL | 0.2586 mL | 0.6466 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
EB-3D 関連分類
HY-115463 関連分類
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