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eEF-2K inhibitor 2C

Chemical Structure : eEF-2K inhibitor 2C

CAS No.: 2396779-33-0

eEF-2K inhibitor 2C (Compound 2C)

货号: PC-20825Not For Human Use, Lab Use Only.

eEF-2K inhibitor 2C (Compound 2C) is a small molecule inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K), binds to the ATP-binding site of eEF-2K.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    eEF-2K inhibitor 2C (Compound 2C) is a small molecule inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K), binds to the ATP-binding site of eEF-2K.
    eEF-2K inhibitor 2C (Compound 2C) (−7.691 kcal/mol) has better docking scores than some of the published eEF-2K inhibitors such as nonpotent inhibitor A484954 (−5.621 kcal/mol), NH125 (−4.503 kcal/mol), and TX-1918 (−5.533 kcal/mol), except for nonspecific eEF-2K inhibitor Rottlerin (−8.263 kcal/mol).
    eEF-2K inhibitor 2C (Compound 2C) (<1 uM) inhibits proliferation and colony formation in breast cancer cells, including highly aggressive and invasive TNBC cells such as MDA-MB-231 (p53- and Kras-mutated), BT-20 (PI3K- and p53-mutated), and MDA-MB-436 (p53- and BRCA1-mutated) and noninvasive MCF-7 (ER+) cells.
    eEF-2K inhibitor 2C (Compound 2C) inhibits activity of eEF-2K as indicated by reduced phosphorylation of its downstream target EF2, induces apoptosis in TNBC cells.
    Treatment with single-lipid nanoparticle incorporating eEF-2K inhibitor 2C (Compound 2C) (20 mg/kg) significantly inhibited tumor growth, led to significant reduction in eEF-2K activity as indicated by reduced levels of p-EF2 (Thr56) in MDA-MB-231 tumor xenographs in highly aggressive TNBC tumor models.

    物理化学性质&存储条件

    分子量 344.29
    分子式 C19H11F3O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (E)-3-(3-(3-(trifluoromethyl)phenyl)acryloyl)-2H-chromen-2-one

    参考文献

    1. Ferah Comert Onder, et al. ACS Pharmacol Transl Sci. 2021 Mar 30;4(2):926-940.

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