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Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8. Droxinostat shows comparable inhibition of HDAC6 and HDAC8 (IC50 = 2.47 and 1.46 μmol/L, respectively).
Droxinostat has shown a potent action against HDAC3, HDAC6, and HDAC8 which are pyrimidyl-hydroxamic acid-dependent histone deacetylases. Chemically Droxinostat stands for 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide. It contains a hydroxamic acid moiety. Caspase 8 is an effective stimulator of apoptosis and its action is inhibited by the protein FLIP. Hence FLIP inhibits apoptosis and Droxinostat targets FLIP induced inhibition of apoptosis.
Droxinostat shows a significant action on gene transcription hence controlling tumor progression. The cells resistant to the caspase mediated apoptotic pathway get sensitized by Droxinostat, hence proving an active agent of introducing death in cancerous cells. (source: http://www.hdacblog.com/2011/10/droxinostat-active-inhibitor-of-hdac3.html).
1: Bijangi-Vishehsaraei K, Saadatzadeh MR, Huang S,
Murphy MP, Safa AR. 4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide
(CMH) targets mRNA of the c-FLIP variants and induces apoptosis in MCF-7
human breast cancer cells. Mol Cell Biochem. 2010 Sep;342(1-2):133-42.
Epub 2010 May 6. PubMed PMID: 20446019.
(Keyword; CAS#; MedKoo code#)
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