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. Author manuscript; available in PMC: 2016 Apr 1.
Published in final edited form as: Cancer Chemother Pharmacol. 2015 Jan 24;75(4):671–682. doi: 10.1007/s00280-015-2675-1
A. Calculated IC50 (nM) of Largazole and Largazole Analogs in Select Cell Lines
Compound HTC-116 HT-29 SW620 A549 MiaPaCa
Largazole 3.5 16.2 26.5 3.8 206.4
Largazole Peptide Isostere 103.3 81.0 224.8 281.2 842.7
Pyridyl Analog Depsipeptide 0.7 0.3 8.2 0.18 91.8
Pyridyl Analog Peptide Isostere 82.9 31.5 81.0 542.7 3536
Pyridyl Analog Pyridyl Disulfide ND ND ND 719.4 3290
B. Calculated Inhibitory IC50 (nM) of Largazole and Largazole Analogs Verses HDAC 1,2,3,6*
Compound HDAC 1 HDAC 2 HDAC 3 HDAC 6
Largazole Thiol 3.4 10.5 10.4 203.6
Largazole Peptide Isostere Thiol 5.8 10.0 12.0 2045
Pyridyl Analog Depsipeptide Thiol 3.9 16.5 17.9 654.5
Pyridyl Analog Peptide Isostere Thiol 38.7 76.4 82.8 33710
Pyridyl Analog Pyridyl Disulfide ND ND ND ND
Vorinostat (SAHA) 136.7 211.5 206.9 143.4
*

ND = not determined

*

All compounds tested were the unmasked thiol forms.