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说明： Potent pan-HDAC inhibitor
化学名： (2E)-N-Hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-2-propenamide
纯度： ≥98% (HPLC)
生物活性 for Belinostat
Belinostat is a potent pan-HDAC inhibitor (IC50 = 28 nM). Dose-dependently reduces tumor volume in a rat model of glioblastoma and induces 70% and 28% apoptosis in LN-229 and LN-18 glioma cell lines (IC50 values are 210 nM and 300 nM respectively). In H358 cells, Belinostat dose-dependently reduces cell viability and upregulates amino acids and metabolites of the TCA and urea cycle. Also potently inhibits C4 release from stem cell-derived astrocytes and shows antidepressant activity. Belinostat is brain penetrant.
技术数据 for Belinostat
| 分子量 | 318.35 |
| 公式 | C15H14N2O4S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 866323-14-0 |
| PubChem ID | 6918638 |
| InChI Key | NCNRHFGMJRPRSK-MDZDMXLPSA-N |
| Smiles | S(NC1=CC=CC=C1)(=O)(=O)C2=CC(/C=C/C(NO)=O)=CC=C2 |
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 Belinostat
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.84 | 100 | |
| ethanol | 31.84 | 100 |
制备储备液 for Belinostat
以下数据基于产品分子量 318.35。 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 | 3.14 mL | 15.71 mL | 31.41 mL |
| 5 mM | 0.63 mL | 3.14 mL | 6.28 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.14 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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产品说明书 for Belinostat
参考文献 for Belinostat
参考文献是支持产品生物活性的出版物。
Finn et al (2005) Novel sulfonamide derivatives as inhibitors of histone deacetylase. Helv.Chim.Acta 88 1630
Kusaczuk et al (2016) Molecular and cellular effects of a novel hydroxamate-based HDAC inhibitor - belinostat - in glioblastoma cell lines: a preliminary report. Invest.New Drugs 34 552 PMID: 27468826
Peter et al (2022) Histone deacetylase inhibitor belinostat regulates metabolic reprogramming in killing KRAS-mutant human lung cancer cells. Mol.Carcinog. 62 1136 PMID: 37144836
Rapino et al (2023) Small-molecule screen reveals pathways that regulate C4 secretion in stem cell-derived astrocytes. Stem Cell Reports 18 237 PMID: 36563689
Gurbani et al (2019) Assessing treatment response of glioblastoma to an HDAC inhibitor using whole-brain spectroscopic MRI. Tomography 5 53 PMID: 30854442
If you know of a relevant reference for Belinostat, please let us know.
关键词: Belinostat, Belinostat supplier, pan, HDAC, inhibitor, inhibits, inhibitors, glioblastoma, glia, H358, cells, NSCLC, lung, cancer, Non-selective, HDACs, Other, Apoptosis, 7981, Tocris Bioscience
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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.
Rheumatoid Arthritis Poster
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.