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UNC4976

Chemical Structure : UNC4976

CAS No.: 2920299-34-7

UNC4976 (UNC-4976)

Catalog No.: PC-38261Not For Human Use, Lab Use Only.

UNC4976 (UNC-4976) is a potent cellular active positive allosteric modulator of CBX7, binds to CBX7 competitively with H3K27me3 peptides (IC50=20 nM), while increasing affinity for oligonucleotides.

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    Biological Activity

    UNC4976 (UNC-4976) is a potent cellular active positive allosteric modulator of CBX7, binds to CBX7 competitively with H3K27me3 peptides (IC50=20 nM), while increasing affinity for oligonucleotides.
    UNC4976 displays >40-fold selectivity over CBX8 (IC50=890 nM).
    The PAM activity of UNC4976 resulted in enhanced efficacy across three orthogonal cellular assays by simultaneously antagonizing H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
    UNC4976 reequilibrates PRC1 away from H3K27me3 target regions.

    Physicochemical Properties

    M.Wt 847.111
    Formula C47H70N6O8
    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

    methyl N6-(bicyclo[2.2.1]heptan-2-yl)-N2-(4-(tert-butyl)benzoyl)-L-phenylalanyl-L-alanyl-L-leucyl-N6-methyl-L-lysyl-L-serinate

    References

    1. Kelsey N Lamb, et al. Cell Chem Biol. 2019 Oct 17;26(10):1365-1379.e22.

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