FK 228

Name: FK 228
Brand: Tocris Bioscience
SKU: 3515

Tocris Bioscience a Bio-Techne Brand

Catalog # 3515

Citations (2)

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Key Product Details

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)
Molecular Weight:	540.7

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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

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 for FK 228

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	3.70 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	3.70 mL

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References for FK 228

References are publications that support the biological activity of the product.

Matsubara 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. 2009 PMID: 19073909
Sasakawa Effects of FK228, a novel histone deacetylase inhibitor, on tumor growth and expression of p21 and c-myc genes in vivo. Cancer Lett. 2003 PMID: 12767524
Furumai FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 PMID: 12208741

Citations for FK 228 (2)

Showing 1 - 2 of 2 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for FK 228 include:

Pozo et al. (2018) Preclinical characterization of tyrosine kinase inhibitor-based targeted therapies for neuroendocrine thyroid cancer. Oncotarget. 9:37662
PMID: 30701022
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

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