FK 228
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%
Biological Activity
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
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.
Background References
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Effects of FK228, a novel histone deacetylase inhibitor, on tumor growth and expression of p21 and c-myc genes in vivo.
Sasakawa et al.
Cancer Lett., 2003;195:161 -
FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases.
Furumai et al.
Cancer Res., 2002;62:4916 -
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
Matsubara et al.
J.Pharmacol.Exp.Ther., 2009;328:839
Product Datasheets
Citations for FK 228
The citations listed below are publications that use Tocris products. Selected citations for FK 228 include:
4 Citations: Showing 1 - 4
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NF-κB-dependent repression of Sox18 transcription factor requires the epigenetic regulators histone deacetylases 1 and 2 in acute lung injury.
Authors: Ting Et al.
Front Physiol 2022;13:947537
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INF2-mediated actin filament reorganization confers intrinsic resilience to neuronal ischemic injury.
Authors: Steven L Et al.
Nat Commun 2022;13:6037
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Preclinical characterization of tyrosine kinase inhibitor-based targeted therapies for neuroendocrine thyroid cancer.
Authors: Pozo Et al.
Oncotarget 2018;9:37662
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Class I histone deacetylase inhibitors inhibit the retention of BRCA1 and 53BP1 at the site of DNA damage.
Authors: Fukuda Et al.
J Pharmacol Exp Ther 2015;106:1050
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