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PFI-6

Chemical Structure : PFI-6

CAS No.: 2675452-91-0

PFI-6 (PFI6)

货号: PC-21341Not For Human Use, Lab Use Only.

PFI-6 is a selective small-molecule chemical probe inhibitor for the YEATS domain of MLLT1 and MLLT3 with IC50 of 140 nM and 160 nM, respectively.

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

    生物&药学活性

    PFI-6 is a selective small-molecule chemical probe inhibitor for the YEATS domain of MLLT1 ((ENL/YEATS1)) and MLLT3 (AF9/YEATS3) with IC50 of 140 nM and 160 nM, respectively.
    PFI-6 demonstrates good affinity and selectivity for MLLT1/3 over other human YD proteins (YEATS2/4, IC50>30 uM).
    PFI-6 exhibits MLLT3 cellular target engagement with IC50 of 0.76 uM in NanoLuciferase Bioluminescent Resonance Energy Transfer (NanoBRET) assays.
    PFI-6 exhibits high affinity for YEATS domain of MLLT1 and MLLT3 with Kd values of 82 and 76 nM in ITC assays respectively.

    物理化学性质&存储条件

    分子量 391.43
    分子式 C22H21N3O4
    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)-N-(2,3-dihydro-1H-inden-1-yl)-5-(4-(dimethylcarbamoyl)-3-hydroxyphenyl)isoxazole-3-carboxamide

    参考文献

    1. Brigitt Raux, et al. Bioorg Med Chem Lett. 2023 Nov 7:129546. doi: 10.1016/j.bmcl.2023.129546.

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