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PFI-6

Chemical Structure : PFI-6

CAS No.: 2675452-91-0

PFI-6 (PFI6)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 391.43
    Formula C22H21N3O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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