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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-JBI-097
JBI-097

Chemical Structure : JBI-097

CAS No.: 2738306-38-0

JBI-097 (JBI097)

货号: PC-24003Not For Human Use, Lab Use Only.

JBI-097 is a potent, dual LSD1/HDAC6 inhibitor with IC50 of 6/48 nM respectively, also inhibits HDAC8 (IC50=71 nM), does not inhibit other HDACs.

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

    生物&药学活性

    JBI-097 is a potent, dual LSD1/HDAC6 inhibitor with IC50 of 6/48 nM respectively, also inhibits HDAC8 (IC50=71 nM), does not inhibit other HDACs.
    JBI-097 inhibited the proliferation of haematological cancers like acute myeloid leukaemia (AML), chronic myeloid leukaemia (CML), erythroleukaemia, and multiple myeloma with stronger potency with EC50 of 0.002-1.5 uM (MM1.S, EC50=2 nM).
    JBI-097 also showed strong modulation of HDAC6 and LSD1 specific biomarkers, alpha-tubulin, CD86, CD11b, and GFi1b.
    JBI-097 showed a stronger effect in erythroleukemia, multiple myeloma xenograft models, and in CT-26 syngeneic model.
    JBI-097 also showed efficacy as monotherapy and additive or synergistic efficacy in combination with the standard of care or with immune checkpoint inhibitors.

    物理化学性质&存储条件

    分子量 407.56
    分子式 C25H33N3O2
    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

    N-hydroxy-4-(3-(4-((((1S,2R)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)propyl)benzamide

    参考文献

    1. Gajendran C, et al. PLoS One. 2023 Jan 3;18(1):e0279063.

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