Apicidin is a cyclic peptide antibiotic with broad spectrum antiparasitic and antiprotozoan activity. Apicidin, a histone deacetylase inhibitor, is anti-angiogenic and induces apoptosis. A potent, cell permeable inhibitor of histone deacetylase (IC50 = 700 pM for parasitic histone deacetylase). Inhibits HeLa cell proliferation (IC50 = 50 – 100 nM) and induces the transcriptional activation of p21 (WAF1) in a reversible manner. Also prevents H-ras-induced invasive phenotype of MCF-10A cells possibly by down regulating MMP-2 in a reversible manner. Apicidin has antiproliferative activity on HeLa cells accompanied by cell arrest at the G1 phase. Apicidin induces selective changes in the expression of p21 and gelsolin.
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