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Submit ReviewFK 228
说明： Potent and selective class I histone deacetylase inhibitor; antitumor
别名： Depsipeptide,FR 901228,Romidepsin
化学名： Cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl], cyclic (3-5) disulfide
纯度： ≥98% (HPLC)
生物活性 for FK 228
FK 228 is a potent and selective inhibitor of class I histone deacetylases (HDACs) (IC50 values are 36, 47, 510 and 14,000 nM for HDAC1, HDAC2, HDAC4 and HDAC6 respectively). Exhibits cytotoxicity against various human tumor cell lines; also exhibits antitumor activity against human tumor xenografts.
External Portal Information for FK 228
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of Romidepsin is reviewed on the Chemical Probes website.
技术数据 for FK 228
| 分子量 | 540.7 |
| 公式 | C24H36N4O6S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 128517-07-7 |
| PubChem ID | 5352062 |
| InChI Key | OHRURASPPZQGQM-GCCNXGTGSA-N |
| Smiles | O=C([C@H]([C@H](C)C)NC(/C(NC([C@@H]2NC([C@@H]([C@H](C)C)N1)=O)=O)=C/C)=O)O[C@H](/C=C/CCSSC2)CC1=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 FK 228
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 5.41 | 10 |
制备储备液 for FK 228
以下数据基于产品分子量 540.7。 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 |
|---|---|---|---|
| 0.1 mM | 18.49 mL | 92.47 mL | 184.95 mL |
| 0.5 mM | 3.7 mL | 18.49 mL | 36.99 mL |
| 1 mM | 1.85 mL | 9.25 mL | 18.49 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.7 mL |
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产品说明书 for FK 228
参考文献 for FK 228
参考文献是支持产品生物活性的出版物。
Sasakawa et al (2003) Effects of FK228, a novel histone deacetylase inhibitor, on tumor growth and expression of p21 and c-myc genes in vivo. Cancer Lett. 195 161 PMID: 12767524
Matsubara et al (2009) Involvement of extracellular signal-regulated kinase activation in human osteosarcoma cell resistance to the histone deacetylase inhibitor FK228 [(1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-bis(propan-2-y J.Pharmacol.Exp.Ther. 328 839 PMID: 19073909
Furumai et al (2002) FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 62 4916 PMID: 12208741
If you know of a relevant reference for FK 228, please let us know.
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关键词: FK 228, FK 228 supplier, FK228, antitumour, antitumor, HDAC, histone, deacetylases, class, I, HDAC1, HDAC2, inhibitors, inhibits, anticancer, FR, 109228, FR109228, Depsipeptide, Romidepsin, 901228, Class, HDACs, 3515, Tocris Bioscience
4 篇 FK 228 的引用文献
引用文献是使用了 Tocris 产品的出版物。 FK 228 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
Steven L et al (2022) INF2-mediated actin filament reorganization confers intrinsic resilience to neuronal ischemic injury. Nat Commun 13 6037 PMID: 36229429
Fukuda et al (2015) Class I histone deacetylase inhibitors inhibit the retention of BRCA1 and 53BP1 at the site of DNA damage. J Pharmacol Exp Ther 106 1050 PMID: 26053117
Pozo et al (2018) Preclinical characterization of tyrosine kinase inhibitor-based targeted therapies for neuroendocrine thyroid cancer. Oncotarget 9 37662 PMID: 30701022
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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.
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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.
Epigenetics in Cancer Poster
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