EB-3D 是一种选择性胆碱激酶 α 抑制剂，对 ChoKα1 的IC50值为 1 μM。它影响 ChoKα 表达、AMPK激活、细胞凋亡、内质网应激和脂质代谢，具有抗癌活性。

EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor(IC50 : 1 μM).with anti-cancer activity.

EB-3D?exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines and primary cultures of pediatric patients.?Moreover, the drug strongly induces apoptosis and more importantly it enhanced T-leukemia cell sensitivity to chemotherapeutic agents, such as dexamethasone and l-asparaginase.?In addition, the compound induces an early activation of AMPK, the main regulator of cellular energy homeostasis, by its phosphorylation at residue T712 of catalytic subunit α, and thus repressing mTORC1 pathway, as shown by mTOR S2448 dephosphorylation.?The inhibition of mTOR in turn affects the activity of several known downstream targets, such as 4E-BP1, p70S6K, S6 Ribosomal Protein and GSK3 that ultimately may lead to a reduction of protein synthesis and cell death[1].

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

1839150-63-8

C30H36Br2N4O2

644.452

DMSO:50 mg/mL (77.59 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years