EB-3D
- CAS号:1839150-63-8
- 英文名:EB-3D
- 中文名:EB-3D
- CBNumber:CB44667867
- 分子式:C30H36BrN4O2+
- 分子量:564.55
- MOL File:1839150-63-8.mol
- 储存条件 :Inert atmosphere,Room Temperature
- 溶解度 :DMSO: 50 mg/mL (77.59 mM)
- 形态 :Solid
- 颜色 :White to off-white
EB-3D性质、用途与生产工艺
- 生物活性 EB-3D 是一种有效的 choline kinase α (ChoKα) 的选择性抑制剂,对ChoKα1的IC50值为1 μM。EB-3D 可在白血病T细胞中诱导 AMPK-mTOR 通路失调和凋亡。
-
靶点
Target Value ChoKα1
(Cell-free assay)1 μM -
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 GI 50 s 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 GI 50 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 GI 50 s 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 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. -
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.
- 更新日期:2024/04/30
- 产品编号:HY-115463
- 产品名称:EB-3D
- CAS编号:
- 包装:1 mg
- 价格:952元
- 更新日期:2024/04/30
- 产品编号:HY-115463
- 产品名称:EB-3D EB-3D
- CAS编号:1839150-63-8
- 包装:5mg
- 价格:1900元
- 公司名称:上海一飞生物科技有限公司
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