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 ActivityA 485 is a potent 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), which displays > 1000-fold selectivity over closely related HATs. A 485 suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro, and also inhibits tumor growth in a castration-resistant prostate cancer xenograft model. A 485 is orally bioavailable.
To request the negative control for A 485, please fill out the A 486 request form on the SGC website.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 485 is reviewed on the chemical probes website.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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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