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Submit ReviewRGFP 966 is a potent and selective HDAC3 inhibitor (IC50 = 80 nM); exhibits no effect on other HDAC (up to 15 μM). RGFP 966 reduces the frequency of striatal CAG repeat expansions in mouse models of Huntington's disease and reduces mHTT accumulation. RGFP 966 blocks the formation of reactive astrocytes and, in vivo, it is neuroprotective and enhances long-term object-location memory.
RGFP 966 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 362.4 |
公式 | C21H19FN4O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1357389-11-7 |
PubChem ID | 56650312 |
InChI Key | BLVQHYHDYFTPDV-VCABWLAWSA-N |
Smiles | NC1=C(C=CC(F)=C1)NC(/C=C/C2=CN(N=C2)C/C=C/C3=CC=CC=C3)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.24 | 100 |
以下数据基于产品分子量 362.4。 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 | 2.76 mL | 13.8 mL | 27.59 mL |
5 mM | 0.55 mL | 2.76 mL | 5.52 mL |
10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Malvaez et al (2013) HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc.Natl.Acad.Sci.USA. 110 2647 PMID: 23297220
Suelvez et al (2017) A selective inhibitor of histone deacetylase 3 prevents cognitive deficits and suppresses striatal CAG repeat expansions in Huntington's disease mice. Sci.Rep. 7 PMID: 28729730
Clayton et al (2024) A phenotypic screening platform for identifying chemical modulators of astrocyte reactivity. Nat.Neurosci. PMID: 38378993
If you know of a relevant reference for RGFP 966, please let us know.
关键词: RGFP 966, RGFP 966 supplier, RGFP966, potent, selective, HDAC, 3, inhibitors, inhibits, Class, I, HDACs, 6728, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RGFP 966 的部分引用包括:
Ting et al (2022) NF-κB-dependent repression of Sox18 transcription factor requires the epigenetic regulators histone deacetylases 1 and 2 in acute lung injury. Front Physiol 13 947537 PMID: 35991176
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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。
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.
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.