Thiols and Related HDAC Inhibitors

Number R HDAC NE IC50 ivM) NCI-H460 cells ICsoffiM) Number n HDAC NE IC50 (fiM) 

HDAC1 IC5o = 1210nM HDAC4 IC5o = 1030 nM HDAC6 IC50 = 29 nM 

300 nM, respectively. Unfortunately, these compounds proved to have antiproliferation activities only in the range of tens of micromoles. However, more recently it was demonstrated that these compounds are in fact potent and selective HDAC 

6 inhibitors [93], where 81a inhibits HDAC 6 with IC5o = 95 nM and the other HDAC isoforms only in the micromolar range. 

and Jones, P.A. (2006) Epigenetic therapy of cancer past, present and future. Nature Reviews Drug Discovery, 5, 37—50. 

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