背景介绍 Romidepsin is a bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several heat shock protein 90 (Hsp90)-dependent oncoproteins. In vitro, romidepsin causes the accumulation of acetylated histones, and induces cell cycle arrest and apoptosis of some cancer cell lines with IC50 values in the nanomolar range. 产品介绍 Romidepsin, also known as FK228 or depsipeptide, is a potent and selective inhibitor of HDAC1 and HDAC2 , which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.