Chemical Name: (1R)-N-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide
Biological ActivityPotent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC50 values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively). Displays > 1000-fold selectivity over closely related HATs. Suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro. Inhibits tumor growth in a castration-resistant prostate cancer xenograft model. Orally bioavailable.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Lasko et al.
Another one (of the "undruggable" targets) bites the dust: discovery of a potent and selective inhibitor of the histone acetyl transferase p300/CBP.
Kodadek et al.
Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome.
Weinert et al.
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