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EB-3D

CAS No. : 1839150-63-8

MCE 站：EB-3D

产品活性：EB-3D 是有效的选择性胆碱激酶 α (ChoKα) 抑制剂，对 ChoKα1 的 IC₅₀ 值为 1 μM。EB-3D 对 ChoKα 表达、AMPK 激活、细胞凋亡 (apoptosis)、内质网应激和脂质代谢有影响。EB-3D 在一组T-白血病细胞系中显示出强大的抗增殖活性。具有抗癌活性。

研究领域：PI3K/Akt/mTOR  |  Epigenetics  |  Apoptosis

作用靶点：AMPK  |  Apoptosis

In Vitro: 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.

In Vivo: 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.

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