iP300w

Cat. No. 7270 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent p300/CBP inhibitor

化学名： (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

纯度： ≥98% (HPLC)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

技术数据 for iP300w

分子量	618.55
公式	C₂₉H₂₇F₅N₆O₄
储存	Store at -20°C
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for iP300w

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	61.85	100

制备储备液 for iP300w

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for iP300w

分析证书/产品说明书

化学品安全技术说明书

参考文献 for iP300w

参考文献是支持产品生物活性的出版物。

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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关键词: iP300w, iP300w supplier, HAT, inhibitors, inhibits, Histone, Acetyltransferases, KAT, Lysine, Aceyltransferases, p300, CBP, 7270, Tocris Bioscience

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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.