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BT-O2C

Chemical Structure : BT-O2C

CAS No.: 3055107-34-8

BT-O2C (p300 degrader)

Catalog No.: PC-24242Not For Human Use, Lab Use Only.

BT-O2C is a potent, selective PROTAC degrader of p300, potently degrades p300 while sparing CBP, is cytotoxic in CIC::DUX4 sarcoma (CDS) cell lines (IC50=152-221 nM).

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    Biological Activity

    BT-O2C is a potent, selective PROTAC degrader of p300, potently degrades p300 while sparing CBP, is cytotoxic in CIC::DUX4 sarcoma (CDS) cell lines (IC50=152-221 nM).
    BT-O2C is mechanistically dependent on both neddylation to activate the CUL4CRBN and on proteasome activity.
    BT-O2C significantly reduces expression of CIC::DUX4 target genes ETV1, ETV4 and ETV5.

    Physicochemical Properties

    M.Wt 973.96
    Formula C48H48F5N9O8
    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

    2-((3'R,4S)-5'-(1-(2-((7-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)heptyl)amino)-2-oxoethyl)-1H-pyrazol-4-yl)-3'-fluoro-2,5-dioxo-2',3'-dihydrospiro[imidazolidine-4,1'-inden]-1-yl)-N-(4-fluorobenzyl)-N-((S)-1,1,1-trifluoropropan-2-yl)acetamide

    References

    1. Marsh GP, et al. RSC Med Chem. 2025 Mar 3. doi: 10.1039/d4md00969j.

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