iP300w
Chemical Name: (1'S,3'R)-3'-Fluoro-N-[(4-fluorophenyl)methyl]-2',3'-dihydro-5'-[1-[2-(methylamino)-2-oxoethyl]-1H-pyrazol-4-yl]-2,5-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[imidazolidine-4,1'-[1H]indene]-1-acetamide
Purity: ≥98%
Biological Activity
iP300w is a potent p300/CBP inhibitor. iP300w inhibits p300-mediated H3K9 acetylation (IC50 = 33 nM). The cytotoxicity of DUX4 and overexpression of DUX4 target genes are inhibited by iP300w in vitro. In addition, the compound inhibits DUX4-mediated transcription in an animal model of facioscapulohumeral muscular dystrophy (FSHD). iP300w reduces viability and inhibits proliferation of CIC-DUX4 sarcoma (CDS) cells in vitro but not pancreatic or colorectal cancer cell lines. The compound suppresses tumor growth in a mouse CDS xenograft model.iP300w negative control iP300v (Cat. No. 7584) also available.Technical Data
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.
Background References
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A novel P300 inhibitor reverses DUX4-mediated global histone H3 hyperacetylation, target gene expression, and cell death.
Bosnakovski et al.
Sci.Adv., 2019;5
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