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Submit ReviewFK 228
Description: Potent and selective class I histone deacetylase inhibitor; antitumor
Alternative Names: Depsipeptide,FR 901228,Romidepsin
Chemical Name: Cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl], cyclic (3-5) disulfide
Purity: ≥98% (HPLC)
Biological Activity 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.
Technical Data for FK 228
| M. Wt | 540.7 |
| Formula | C24H36N4O6S2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FK 228
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.41 | 10 |
Preparing Stock Solutions for FK 228
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for FK 228
References for FK 228
References are publications that support the biological activity of the product.
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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Keywords: 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 Citations for FK 228
Citations are publications that use Tocris products. Selected citations for FK 228 include:
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
Do you know of a great paper that uses FK 228 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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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Epigenetics in Cancer Poster
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