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UNC7700

Chemical Structure : UNC7700

CAS No.: 2918813-30-4

UNC7700 (UNC-7700)

Catalog No.: PC-20148Not For Human Use, Lab Use Only.

UNC7700 (UNC-7700) is a potent EED-targeted PRC2 degrader, contains a unique cis-cyclobutane linker and potently degrades all PRC2 components EED (DC50=111 nM; Dmax=84%), EZH2WT/EZH2Y641N (DC50=275 nM; Dmax=86%) and SUZ12 (Dmax=44%) in DLBCL cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    UNC7700 (UNC-7700) is a potent EED-targeted PRC2 degrader, contains a unique cis-cyclobutane linker and potently degrades all PRC2 components EED (DC50=111 nM; Dmax=84%), EZH2WT/EZH2Y641N (DC50=275 nM; Dmax=86%) and SUZ12 (Dmax=44%) in DLBCL cells.
    UNC7700 is more potently reduces H3K27me3 levels and demonstrates a more robust anti-proliferative effect than UNC6852.
    UNC7700 degrades EED approximately 15-fold more potently than UNC6852 in DB cells and can effectively degrade the core PRC2 components in DLBCL cells after 24 h (EED, DC50 = 111 nM and Dmax = 84%; EZH2WT/EZH2Y641N, DC50 = 275 nM and Dmax = 86%; and SUZ12, Dmax = 44%).
    UNC7700-mediated PRC2 degradation is VHL- and proteasome-dependent.
    UNC7700 decreases H3K27me3 levels and is anti-proliferative in DB cells, potently degrades all core PRC2 components.

    Physicochemical Properties

    M.Wt 844.99
    Formula C44H48N10O6S
    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

    (2S,4R)-1-((S)-2-((1s,3R)-3-(4-(5-((furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)benzamido)cyclobutane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

    References

    1. Frances M Bashore, et al. ACS Chem Biol. 2023 Mar 6. doi: 10.1021/acschembio.2c00804.

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