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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)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for iP300w, please let us know.

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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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