Description
Potent p300/CBP inhibitor. Inhibits p300-mediated H3K9 acetylation (IC50 = 33 nM). Inhibits cytotoxicity of DUX4 and overexpression of DUX4 target genes in vitro. Also impairs DUX4-mediated transcription in an animal model of facioscapulohumeral muscular dystrophy
Product information
Molecular Weight: 618.55
Formula: C29H27F5N6O4
Chemical Name: 2-(3'-fluoro-5'-{1-[(methylcarbamoyl)methyl]-1H-pyrazol-4-yl}-2, 5-dioxo-2', 3'-dihydrospiro[imidazolidine-4, 1'-inden]-1-yl)-N-[(4-fluorophenyl)methyl]-N-(1, 1, 1-trifluoropropan-2-yl)acetamide
Smiles: CC(N(CC1=CC=C(F)C=C1)C(=O)CN1C(=O)C2(CC(F)C3=CC(=CC=C23)C2=CN(CC(=O)NC)N=C2)NC1=O)C(F)(F)F
InChiKey: SWXCHCQCWFXILM-UHFFFAOYSA-N
InChi: InChI=1S/C29H27F5N6O4/c1-16(29(32,33)34)39(12-17-3-6-20(30)7-4-17)25(42)15-40-26(43)28(37-27(40)44)10-23(31)21-9-18(5-8-22(21)28)19-11-36-38(13-19)14-24(41)35-2/h3-9,11,13,16,23H,10,12,14-15H2,1-2H3,(H,35,41)(H,37,44)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Bosnakovski D, da Silva MT, Sunny ST, et al. A novel P300 inhibitor reverses DUX4-mediated global histone H3 hyperacetylation, target gene expression, and cell death. Sci Adv. 2019;5(9):eaaw7781. Published 2019 Sep 11. doi:10.1126/sciadv.aaw7781
Products are for research use only. Not for human use.
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