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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-NSC682769
NSC682769

Chemical Structure : NSC682769

CAS No.: 205048-79-9

NSC682769 (NSC 682769)

货号: PC-20408Not For Human Use, Lab Use Only.

NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM.

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

    生物&药学活性

    NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM.
    NSC682769 blocks in vitro YAP-TEAD binding in a GST pull-down assay.
    NSC682769 potently inhibits YAP expression in LN299 and GBM39 cells with IC50 of 11.8 and 5.1 nM, respectively.
    NSC682769 inhibits the binding of all four TEAD members (TEAD1-4) to YAP, without appreciable effects on SMAD7, p73, FOS or TBX5 association.
    NSC682769 (50 nM, 6 h) markedly reduced YAP-TEAD transcriptional activity in LN229 or GBM39 cells, resulted in a reduction of nuclear YAP and a concomitant accumulation of cytoplasmic YAP consistent.
    NSC682769 inhibits proliferation, anchorage-independent growth, motility, invasive potential and induced apoptosis in glioblastoma multiforme (GBM).
    NSC682769 (5 and 20 mg/kg/day) inhibited GBM tumor growth in SCID mice implanted with subcutaneous LN229 xenografts.
    NSC682769 is blood-brain barrier (BBB) penetrant , twice-weekly 5 or 20 mg/kg NSC682769 increases survival of a glioma GEMM.

    物理化学性质&存储条件

    分子量 422.48
    分子式 C27H22N2O3
    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-(3,4-dimethoxyphenyl)-2-phenyl-5,7-dihydro-6H-benzo[b]pyrido[2,3-d]azepin-6-one

    参考文献

    1. Jacquelyn T Saunders, et al. J Neurooncol. 2021 Apr;152(2):217-231.

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