Published TCIMAIL newest issue No.197
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Histon Deacetylase 8 (HDAC8) Selective Inhibitor
N-Hydroxy-3-[1-(phenylthio)methyl-1H-1,2,3-triazol-4-yl]benzamide (NCC-149), developed by Suzuki, Miyata et al., selectively inhibits histon deacetylase 8 (HDAC8). Histon deacetylase (HDAC) regulates gene expression, such as the tumor-suppressor gene, by catalyzing the deacetylation reaction of the acetylated lysine residue in histon. HDAC8, an isoform of histon deacetylase, has been reported to be implicated in T-cell lymphomas and neuroblastoma tumorigenesis. It is expected that NCC-149 will be used as an epigenetics research tool and an anticancer agent because of its selective inhibitory activity of HDAC8 and tumor cell growth.
References
- 1) T. Suzuki, Y. Ota, Y. Kasuya, M. Mutsuga, Y. Kawamura, H. Tsumoto, H. Nakagawa, M. G. Finn, N. Miyata, Angew. Chem. Int. Ed. 2010, 49, 6817.
- 2) T. Suzuki, Y. Ota, M. Ri , M. Bando, A. Gotoh, Y. Itoh, H. Tsumoto, P. R. Tatum, T. Mizukami, H. Nakagawa, S. Iida, R. Ueda, K. Shirahige, N. Miyata, J. Med. Chem. 2012, 55, 9562.