化合物EB-3D T7955

Product Introduction
Bioactivity


英文名: EB-3D

描述: 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。

细胞实验: 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

体外活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (77.59 mM)


关键字: lipid | inhibit | lymphoblastic | AMP-activated protein kinase | EB3D | acute | tumorigenesis | Apoptosis | homeostasis | dephosphorylation | AMPK | Inhibitor | EB 3D | leukemia | HepG2 | EB-3D

相关产品: Polygalacin D | 18α-Glycyrrhetinic acid | Novobiocin | Oxypalmatine | Nafamostat mesylate | Alexidine dihydrochloride | FD2157 | CP-724714 | AEE788 | Fludarabine Phosphate

相关库: Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Oxidation-Reduction Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Glycolysis Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途