| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87653-5mg促销 |
99.40% | ￥200.00 ￥160.00 |
8 | - | - | - | - |
|
S87653-10mg促销 |
99.40% | ￥280.00 ￥224.00 |
5 | - | - | - | - |
|
S87653-25mg |
99.40% | ￥350.00 |
4 | - | - | - | - |
|
S87653-100mg |
≥98% | ￥1280.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | 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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| 靶点： | IC50: 1 μM; Kd: 0.7 μM;Apoptosis; AMPK; AChR | ||||||||||||||||||||
| 体外研究： | 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. EB-3D (1.25-5μM; 24 hours) induced apoptosis in leukemia cell lines. EB-3D (0.5-1 μM; 24 hours) induces a G0/G1 arrest that lead to apoptosis. 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. EB-3D (1-40 μM; 48 hours) inhibits cell growth in HepG2 cells with a GI50 of 14.55 μM. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. Cell Proliferation Assay Cell Line: JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Time: 72 hours 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. Apoptosis Analysis Cell Line: Jurkat, CCRF-CEM and HSB-2 cells Concentration: 1.25, 2.5, 5 μM Incubation Time: 24 hours Result: Induced apoptosis in leukemia cell lines. Cell Cycle Analysis Cell Line: Jurkat, CCRF-CEM and HSB-2 cells Concentration: 0.5, 1 μM Incubation Time: 24 hours Result: Induces cell cycle arrest in G0/G1 phase. Western Blot Analysis Cell Line: Jurkat cells Concentration: 0.3 μM Incubation Time: 48 hours Result: Showed a first spike of activation of AMPKα after 30 minutes of treatment and a l | ||||||||||||||||||||
| 体内研究： | EB-3D (1 mg/kg; i.p.; every other day) impairs mammary tumor growth in syngeneic orthotopic E0771-C57BL/6 mouse model. EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis. Animal Model: E0771-C57BL/6 mice Dosage: I.p.; every other day for 4 weeks Administration: 2.5 mg/kg Result: A reduction of the number of spontaneous lung macro- and micrometastasis. | ||||||||||||||||||||
| 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. 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. 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).Sci Rep. 2016 Mar 31;6:23793. 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. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、H2O | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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