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首页-小分子抑制剂&激动剂-Apoptosis-MDM2-p53-K-181
K-181

Chemical Structure : K-181

CAS No.: 1215171-87-1

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K-181 (K181)

货号: PC-49577Not For Human Use, Lab Use Only.

K-181 is a specific small-molecule Protein-Protein Interaction (PPI) inhibitor of Mdmx-p53 interaction, exhibits neuroprotective effects on ischemic stroke by disrupting Mdmx-p53 interaction and inhibiting HDAC6 activity.

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

    生物&药学活性

    K-181 is a specific small-molecule Protein-Protein Interaction (PPI) inhibitor of Mdmx-p53 interaction, exhibits neuroprotective effects on ischemic stroke by disrupting Mdmx-p53 interaction and inhibiting HDAC6 activity.
    K-181 preferentially inhibited Mdmx-p53 interaction over Mdm2-p53 interaction and suppressed the growth of cancer cells.
    K-181 could be hydrolyzed to its free thiol derivative (K-181SH) in cells, interfered with the p53-Mdmx interaction through disulfide-bond formation between the free thiol groups of K-181SH and Cys77 in Mdmx in the p53-binding domain.
    K-181 (50 mg/kg/day, oral) increased Mdmx expression in mice brain under physiological condition.
    K-181 attenuated acute ischemic stroke damage in mice, increased Mdmx expression under ischemic stroke in both in vivo and in vitro.
    K-181 exerted neuroprotective effects in response to hypoxia/reperfusion in neurons.
    K-181 selectively inhibited HDAC6 activity and enhanced tubulin acetylation.

    物理化学性质&存储条件

    分子量 299.39
    分子式 C17H17NO2S
    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

    S-2-benzamidophenyl 2-methylpropanethioate

    参考文献

    1. Yan H, et al. Sci Rep. 2022 Dec 6;12(1):21110.

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