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
Biological ActivityFK 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.
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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.
Citations for FK 228
The citations listed below are publications that use Tocris products. Selected citations for FK 228 include:
2 Citations: Showing 1 - 2
Preclinical characterization of tyrosine kinase inhibitor-based targeted therapies for neuroendocrine thyroid cancer.
Authors: Pozo Et al.
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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