Description
KD 5170 is a mercaptoketone-based inhibitor of class I and II histone deacetylases (HDACs; IC
50s = 20, 2,060, 75, 26, 950, 14, 85, 2,500, 150, and 18 nM for HDAC1-10, respectively). It exhibits broad spectrum antitumor activity
in vitro and
in vivo. KD 5170 increases the acetylation of histones and activates caspases 3, 8, and 9, leading to apoptosis in primary myeloma cells.
References
[1]. hassig ca, symons kt, guo x, et al. kd5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo. mol cancer ther, 2008, 7(5): 1054-1065.
[2]. payne je, bonnefous c, hassig ca, et al. identification of kd5170: a novel mercaptoketone-based histone deacetylase inhibitor. bioorg med chem lett, 2008, 18(23): 6093-6096.
[3]. feng r, ma h, hassig ca, et al. kd5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by dna damage and mitochondrial signaling. mol cancer ther, 2008, 7(6): 1494-1505.
