MPI-5a is an effective and selective inhibitor of HDAC6 with IC50 value of 36nM.
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Histone deacetylases (HDACs) are epigenetic regulators that regulate the histone tail, chromatin conformation, protein-DNA interaction, and even transcription. HDACs are also post-transcriptional modifiers that regulate the protein acetylation implicated in several pathophysiologic states[1]. HDAC modulates cell proliferation and angiogenesis and plays an essential role in cell growth. Research shows that up-regulated HDACs are present in many cancer types and synthetic or natural HDAC inhibitors have been used to silence overregulated HDACs. Inhibiting HDACs may cause arrest of cell proliferation, angiogenesis reduction and cell apoptosis[2].In plasma from animals exposed to [HDAC inhibitor + anti-PD-1], but not [HDAC inhibitor + anti-CTLA4], the levels of CCL2, CCL5, CXCL9 and CXCL2 were increased. The cytokine data from HDAC inhibitor plus anti-PD-1 exposed tumors correlated with increased activated T cell, M1 macrophage, neutrophil and NK cell infiltration[3].Treatment with HDAC inhibitors results in the hyperacetylation of chaperones including heat shock protein (hsp)90, hsp70, hsp40, and the ER-resident hsp70 homolog, glucose-regulated protein 78 (GRP78), which affects their function. HDAC inhibitor-mediated deregulation of chaperone function, in turn, deregulates protein homeostasis and induces protein misfolding and proteotoxic stress. In the context of tumors which are particularly dependent on functional chaperones for maintaining protein homeostasis, HDAC inhibitors tip the balance toward lethal proteotoxic and ER stress[4].HDAC6 Inhibitor(MPI_5a) is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM)[5].
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