FK 228

Pricing Availability Delivery Time Qty
Cat.No. 3515 - FK 228 | C24H36N4O6S2 | CAS No. 128517-07-7
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)
Datasheet
Citations (1)
Literature

Biological Activity

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

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.41 10

Preparing Stock Solutions

The following data is based on the product molecular weight 540.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.85 mL 9.25 mL 18.49 mL
5 mM 0.37 mL 1.85 mL 3.7 mL
10 mM 0.18 mL 0.92 mL 1.85 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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.

View Related Products by Target

View Related Products by Product Action

View all Histone Deacetylase Inhibitors

Keywords: FK 228, supplier, FK228, antitumour, antitumor, HDAC, histone, deacetylases, class, I, HDAC1, HDAC2, inhibitors, inhibits, anticancer, FR, 109228, FR109228, Depsipeptide, Romidepsin, Depsipeptide, FR, 901228, Romidepsin, Histone, Deacetylases, Histone, Deacetylases, Tocris Bioscience

1 Citation for FK 228

Citations are publications that use Tocris products. Selected citations for FK 228 include:

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


Do you know of a great paper that uses FK 228 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Epigenetics

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.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

Pathways for FK 228

Protocols

TODO: Add Protocols