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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-(R)-STU104
(R)-STU104

Chemical Structure : (R)-STU104

CAS No.: 1983136-72-6

(R)-STU104 (TAK1-MKK3 inhibitor)

货号: PC-38495Not For Human Use, Lab Use Only.

(R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.

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

    生物&药学活性

    (R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.
    (R)-STU104 exhibited the potent inhibitory activity on TNF-α production on RAW264.7 cells with IC50 of 0.58 uM, suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways.
    (R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse ulcerative colitis (UC) models.
    (R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d.

    物理化学性质&存储条件

    分子量 298.338
    分子式 C18H18O4
    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

    (R)-4,6-dimethoxy-3-(4-methoxyphenyl)-2,3-dihydro-1H-inden-1-one

    参考文献

    1. Mei-Lin Tang, et al. J Med Chem. 2022 Apr 20. doi: 10.1021/acs.jmedchem.1c02198.

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