Cyclic Tetrapeptide and Natural Product Inhibitors

Most show selectivity for Class I HDACs.

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A8851 Apicidin ≥98% (HPLC), from microbial Apicidin is a cyclic tetrapeptide that inhibits histone deacetylase. Apicidin has antiproliferative activity on various cancer cell lines and HeLa cells, accompanied by cell arrest at the G1 phase. It has been shown to induce selective changes in the expression of p21 and gelsolin, induce apoptosis in HL60 cells, and exhibit antiprotozoal, antiparasitic, and potential antimalarial properties.
 
T2580   Trapoxin A ≥98% (HPLC), from Helicoma ambiens Trapoxin A is a cyclotetrapeptide and a histone deacetylase (HDAC) inhibitor. It increases the level of chromatin acetylation associated with histone H3 at low nanomolar concentrations. Unlike the reversible HDAC inhibition induced by TCA, Trapoxin A irreversibly inhibites HDAC activity in crude cell lysates, and induces the accumulation of hyperacetylated core histones in a number of mammalian cell lines and tissues. Histone acetylation and methylation have been studied extensively for their anti-tumor activities in carcinogenesis and Trapoxin has been suggested as a potential anticancer agent for pre-clinical trials.