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说明： p300/CBP inhibitor
化学名： 4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]benzoic acid
纯度： ≥98% (HPLC)
生物活性 for C 646
C 646 is a p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM). Suppresses histone H3 and H4 acetylation in mouse fibroblast cell lines. Also represses pluripotency markers in mouse embryonic stem cells. Newer p300 probes are also available: iP300w (Cat. No. 7270) and A 485 (Cat. No. 6387).
This compound is a mixture of Z:E isomers (~ 80:20).
技术数据 for C 646
| 分子量 | 445.42 |
| 公式 | C24H19N3O6 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 328968-36-1 |
| PubChem ID | 1285941 |
| InChI Key | HEKJYZZSCQBJGB-UNOMPAQXSA-N |
| Smiles | CC/2=NN(C(C2=C/C3=CC=C(C4=CC(C)=C(C)C=C4[N+]([O-])=O)O3)=O)C1=CC=C(C(O)=O)C=C1 |
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.
产品说明书 for C 646
参考文献 for C 646
参考文献是支持产品生物活性的出版物。
Bowers et al (2010) Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem.Biol. 17 471 PMID: 20534345
Mali et al (2010) Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes. Stem Cells 28 713 PMID: 20201064
Ott and Verdi (2010) HAT trick: p300, small molecule, inhibitor. Chem.Biol. 17 417 PMID: 20534339
Crump et al (2011) Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proc.Natl.Acad.Sci. USA 108 7814
Dan et al (2015) Roles for histone acetylation in regulation of telomere elongation and two-cell state in mouse ES cells. J.Cell.Physiol. 230 2337 PMID: 25752831
Dahlin et al (2017) Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors. Nat.Commun. 8 1527 PMID: 29142305
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关键词: C 646, C 646 supplier, C646, p300, CREB-binding, proteins, CBP, inhibitors, inhibits, histone, acetyltransferase, hat, kat, posttranslational, modifications, epigenetics, Post-translational, Modifications, Histone, Acetyltransferases, Other, Differentiation, Products, 4200, Tocris Bioscience
2 篇 C 646 的引用文献
引用文献是使用了 Tocris 产品的出版物。 C 646 的部分引用包括：
Yi et al (2021) Neuronal activity-induced BRG1 phosphorylation regulates enhancer activation. Cell Rep 36 109357 PMID: 34260936
Dong-Ming et al (2022) Accumulation of pTreg cells is detrimental in late-onset (aged) mouse model of multiple sclerosis. Aging Cell 21 e13630 PMID: 35615905
C 646 的评论
平均评分: 5 (Based on 1 Review.)
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C 646 In vitro concentration.
By
Anonymous on 01/08/2018
分析类型： In Vitro
种属： Human
细胞系/组织： Intestinal subepithelial myofibroblasts, smooth muscle cells,
It is dissolved well in DMSO. I diluted it with serum free medium (final concentration of 10 micromolar) and treated the cells for different time points to detect its inhibitory effect of p300 at protein level.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.