iP300w

Name: iP300w
Brand: Tocris Bioscience
SKU: 7270

Tocris Bioscience, part of Bio-Techne | Catalog # 7270

Citations (3)

COA / SDS

Potent p300/CBP inhibitor

Key Product Details

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)
Molecular Weight:	618.55

View Full Technical Details for iP300w

Technical Data
Citations

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 for iP300w

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for iP300w

References are publications that support the biological activity of the product.

Bosnakovski Inactivation of the CIC-DUX4 oncogene through P300/CBP inhibition, a therapeutic approach for CIC-DUX4 sarcoma. Oncogenesis
Bosnakovski A novel P300 inhibitor reverses DUX4-mediated global histone H3 hyperacetylation, target gene expression, and cell death. Sci.Adv. 2019 PMID: 31535023