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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-MPK5 inhibitor 1
MPK5 inhibitor 1

Chemical Structure : MPK5 inhibitor 1

CAS No.: 882289-64-7

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MPK5 inhibitor 1 (MPK5-IN-1, MPK5 inhibitor compound 1)

货号: PC-72803Not For Human Use, Lab Use Only.

MPK5 inhibitor 1 (MPK5-IN-1, MPK5 inhibitor compound 1) is a potent, selective allosteric inhibitor of MAPK phosphatase MKP5 with Kd/IC50 of 1.0/3.9 uM.

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

    生物&药学活性

    MPK5 inhibitor 1 (MPK5-IN-1, MPK5 inhibitor compound 1) is a potent, selective allosteric inhibitor of MAPK phosphatase MKP5 with Kd/IC50 of 1.0/3.9 uM.
    MPK5 inhibitor 1 also inhibited the full-length MKP5 with similar potency to the catalytic domain, showed little to no inhibition on STEP-46, PTP-1B and other members of the MKP family, MKP1, MKP3, and MKP7 (IC50>100 uM).
    MPK5 inhibitor 1 also inhibited Y435W mutant with Kd/IC50 of 1.3/2.9 uM, but not for mutants Y435A/Y435S/T432D/M431L-T432D, suggesteTyr435 as essential for phosphatase activity of MPK5.
    MPK5 inhibitor 1 induces MAPK activity and stimulates myoblast differentiation, MKP5 is required for TGF-β1 signaling and MPK5 inhibitor 1 inhibits Smad2 activity.
    MKP5 targeting may serve as a therapeutic pathway for the treatment of dystrophic muscle disease.

    物理化学性质&存储条件

    分子量 364.54
    分子式 C17H20N2OS3
    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

    3,3-dimethyl-1-((9-(methylthio)-5,6-dihydrothieno[3,4-h]quinazolin-2-yl)thio)butan-2-one

    参考文献

    1. Zachary T K Gannam, et al. Sci Signal. 2020 Aug 25;13(646):eaba3043.

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