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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-TEAD-IN-2
TEAD-IN-2

Chemical Structure : TEAD-IN-2

CAS No.: 2412761-57-8

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TEAD-IN-2 (TEAD antagonist 2)

货号: PC-38143Not For Human Use, Lab Use Only.

TEAD-IN-2 (TEAD antagonist 2) is a small molecule TEAD antagonist (TEAD2 IC50=603 nM FP assays, SPR Kd=229 nM) that binds the TEAD lipid pocket and disrupts TEAD S-palmitoylation.

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

    生物&药学活性

    TEAD-IN-2 (TEAD antagonist 2) is a small molecule TEAD antagonist (TEAD2 IC50=603 nM FP assays, SPR Kd=229 nM) that binds the TEAD lipid pocket and disrupts TEAD S-palmitoylation.
    TEAD-IN-2 showed similar IC50 against all TEAD paralogs TEAD1, TEAD3, and TEAD4 both in IP and SRP assays.
    TEAD-IN-2 disrupted Hippo signaling in a Detroit X1 562 cell reporter assay with IC50 of 31.8 nM, with no significant cytotoxicity indications in either primary human hepatocytes or human liver microtissues at 100 uM.
    The inhibition of TEAD activity via TEAD-IN-2 was not due to the inability of TEAD to form a complex with YAP in cells.
    TEAD-IN-2 functioned by acting as a TEAD S-palmitoylation mimic, binding and stabilizing newly translated TEAD proteins, TEAD-palmitoylation-deficient mutant K357A caused a stronger rescue of TEAD expression in HEK293T cells transfected TEAD2-K357A.
    Dysregulating TEAD S-palmitoylation via TEAD-IN-2 could effectively inhibit Hippo-dependent tumor growth in vivo.

    物理化学性质&存储条件

    分子量 346.393
    分子式 C15H20F2N2O3S
    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)-N-(5-(2-(4,4-difluorocyclohexyl)vinyl)-6-methoxypyridin-3-yl)methanesulfonamide

    参考文献

    1. Holden JK, et al. Cell Rep. 2020 Jun 23;31(12):107809.

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