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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-TEAD inhibitor TM2
TEAD inhibitor TM2

Chemical Structure : TEAD inhibitor TM2

CAS No.: 1008768-41-9

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TEAD inhibitor TM2 (TEAD-IN-8)

货号: PC-49537Not For Human Use, Lab Use Only.

TEAD inhibitor TM2 is a potent pan-TEAD auto-palmitoylation inhibitor with IC50 of 156 and 38 nM for TEAD2 palmitoylation and TEAD4 auto-palmitoylation, respectively, disrupts TEAD-YAP association and specifically inhibits YAP transcriptional activities.

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

    生物&药学活性

    TEAD inhibitor TM2 is a potent pan-TEAD auto-palmitoylation inhibitor with IC50 of 156 and 38 nM for TEAD2 palmitoylation and TEAD4 auto-palmitoylation, respectively, disrupts TEAD-YAP association and specifically inhibits YAP transcriptional activities.
    TM2 dramatically suppresses Myc-TEAD1 palmitoylation in cells in a dose-dependent manner, also significantly inhibits endogenous TEAD1-4 palmitoylation using an antibody recognizing pan-TEADs at as low as 100 nM.
    TM2 adopts a novel binding mode compared to other known TEAD inhibitors (MGH-CP1, VT105 and K975).
    TM2 showed striking anti-proliferation efficacy as a single agent in human MPM, a type of tumor that is highly associated with YAP activation, also shows synergy effects in combination with a MEK inhibitor in YAP-dependent cancer cells

    物理化学性质&存储条件

    分子量 435.568
    分子式 C26H33N3O3
    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

    4-(3-(2-cyclohexylethoxy)benzoyl)-N-phenylpiperazine-1-carboxamide

    参考文献

    1. Lu Hu, et al. Elife. 2022 Nov 18;11:e80210.

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