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首页-小分子抑制剂&激动剂-Others-Other Targets-SMALS-329
SMALS-329

Chemical Structure : SMALS-329

CAS No.: 2684270-22-0

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SMALS-329 (SMALS329)

货号: PC-27800Not For Human Use, Lab Use Only.

SMALS-329 is a small-molecule activator of liver kinase B1 (LKB1, STK11) via pseudokinase STE20-related kinase adapter protein (STRAD) with EC50 of 8.5 uM (activation 541%), binds ATP pocket of STRADα to activate LKB1.

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

    生物&药学活性

    SMALS-329 is a small-molecule activator of liver kinase B1 (LKB1, STK11) via pseudokinase STE20-related kinase adapter protein (STRAD) with EC50 of 8.5 uM (activation 541%), binds ATP pocket of STRADα to activate LKB1.
    SMALS-329 activates LKB1 in tumor cell lines in a target- and dose-dependent manner.
    SMALS-329 not only increases the thermal stability of STRAD, as assessed by cellular thermal shift assay (CETSA), but also the stability of LKB1.
    SMALS-329 (8 uM) resulted in increased phosphorylation of the known LKB1 sites on the key LKB1 effectors AMPK1/2 and SIK1-3 in LKB1WT H358 lung cancer cell line.
    SMALS-329 inhibits the viability of H358 cells in a dose-dependent manner, and LKB1 knockdown by CRISPRi reduced this effect by 1.5-fold.
    SMALS-329 shows a growth inhibition 50% (GI50) ≤ 15 uM for 12 multiple cancer types.
    SMALS-329 enhances PI3K/AKT and KRAS inhibitor effects.

    物理化学性质&存储条件

    分子量 518.52
    分子式 C23H27N4O6PS
    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

    diethyl (((4-(3-amino-6-(p-tolyl)pyrazine-2-carboxamido)phenyl)sulfonyl)methyl)phosphonate

    参考文献

    1. Kretschmer LS, et al. Cell Chem Biol. 2026 Aug 18:S2451-9456(26)00286-2.

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