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Submit ReviewMS 275 is a class I HDAC inhibitor (IC50 values are 0.18, 0.74, 44.9 and >100 μM for HDAC1, 3, 8 and 6, respectively). Exhibits antiproliferative effects and induces apoptosis in a range of tumor cell lines in vitro and in vivo. Increases estrogen receptor α- and aromatase expression in breast cancer cells. Inhibits PCB-induced neuronal cell death by preventing HDAC3 binding and histone deacetylation within the synapsin-1 promoter.
MS 275 is also offered as part of the Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 376.41 |
公式 | C21H20N4O3 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 209783-80-2 |
PubChem ID | 4261 |
InChI Key | INVTYAOGFAGBOE-UHFFFAOYSA-N |
Smiles | O=C(C1=CC=C(C=C1)CNC(OCC2=CN=CC=C2)=O)NC3=CC=CC=C3N |
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 | 37.64 | 100 |
以下数据基于产品分子量 376.41。 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 | 2.66 mL | 13.28 mL | 26.57 mL |
5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Saito et al (1999) A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc.Natl.Acad.Sci. 96 4592 PMID: 10200307
Beckers et al (2007) Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. Int.J.Cancer 121 1138 PMID: 17455259
Formisano et al (2015) MS-275 inhibits aroclor 1254-induced SH-SY5Y neuronal cell toxicity by preventing the formation of the HDAC3/REST complex on the synapsin-1 promoter. J.Pharmacol.Exp.Ther. 352 236 PMID: 25467131
Sabnis et al (2011) Functional activation of the estrogen receptor-α and aromatase by the HDAC inhibitor entinostat sensitizes ER-negative tumors to letr. Cancer Res. 71 1893 PMID: 21245100
If you know of a relevant reference for MS 275, please let us know.
关键词: MS 275, MS 275 supplier, MS275, HDAC1, HDAC3, inhibits, inhibitors, class, I, histone, deacetylases, SNDX275, entinostat, SNDX, 275, Class, HDACs, 6208, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 MS 275 的部分引用包括:
Kim (2018) Suppression of TGFβ-mediated conversion of endothelial cells and fibroblasts into cancer associated (myo)fibroblasts via HDAC inhibition. Br J Cancer 118 1359 PMID: 29695769
Verónica et al (2020) Differential effects of HDAC inhibitors on PPN oscillatory activity in vivo. Neuropharmacology 165 107922 PMID: 31923766
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TGF beta high responder treated with 1.5 μM MS 275 (HDAC 3 inhibitor) for 48 h. Cell lysates were analysed by western blot.
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.
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