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Description: Potent p300/CBP inhibitor
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% (HPLC)
Biological Activity for iP300w
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 for iP300w
| M. Wt | 618.55 |
| Formula | C29H27F5N6O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1889284-33-6 |
| PubChem ID | 134327298 |
| InChI Key | SWXCHCQCWFXILM-NPPGMGHMSA-N |
| Smiles | O=C(NC)CN(N=C1)C=C1C(C=C2)=CC3=C2[C@@](N4)(C[C@H]3F)C(N(CC(N(CC5=CC=C(F)C=C5)[C@@H](C)C(F)(F)F)=O)C4=O)=O |
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.
Solubility Data for iP300w
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 61.85 | 100 |
Preparing Stock Solutions for iP300w
The following data is based on the product molecular weight 618.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.62 mL | 8.08 mL | 16.17 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.23 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets for iP300w
References for iP300w
References are publications that support the biological activity of the product.
Bosnakovski et al (2019) A novel P300 inhibitor reverses DUX4-mediated global histone H3 hyperacetylation, target gene expression, and cell death. Sci.Adv. 5 eaaw7781 PMID: 31535023
Bosnakovski et al (2021) Inactivation of the CIC-DUX4 oncogene through P300/CBP inhibition, a therapeutic approach for CIC-DUX4 sarcoma. Oncogenesis 10 68
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Keywords: iP300w, iP300w supplier, HAT, inhibitors, inhibits, Histone, Acetyltransferases, KAT, Lysine, Aceyltransferases, p300, CBP, 7270, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.