. 2014 Jul 7;5(8):905–910. doi: 10.1021/ml500170r

Table 1. Inhibition of Purified HDACs and Growth of HCT116 Cancer Cells by Largazole and Disulfide Analogues (IC₅₀ ± SD, nM).

IC₅₀ (nM)^a	2	4^b	5^b	FK228^b
HDAC1	0.4 ± 0.05	0.3 ± 0.01	0.4 ± 0.03	0.8 ± 0.03
HDAC2	0.9 ± 0.09	0.5 ± 0.09	0.9 ± 0.01	1 ± 0.1
HDAC3	0.7 ± 0.003	0.3 ± 0.02	0.6 ± 0.06	1.3 ± 0.1
HDAC4	NI^c	NI^c	NI^c	647 ± 20
HDAC5	NI^c	NI^c	NI^c	22%^d
HDAC6	35 ± 10	61 ± 8	135 ± 10	45%^d
HDAC7	NI^c	NI^c	NI^c	34%^d
HDAC8	102 ± 7	40%^d	35%^d	36%^d
HDAC9	NI^c	NI^c	NI^c	45%^d
HDAC10	0.5 ± 0.02	0.2 ± 0.004	0.5 ± 0.04	0.9 ± 0.1
HDAC11	3 ± 0.3	0.1 ± 0.0002	0.2 ± 0.03	0.3 ± 0.0003
HCT116 cells antiproliferative activity	5.9 ± 0.7	12 ± 2	13 ± 1	3.0 ± 0.2

IC₅₀ values for enzymatic assays are averages from duplicate experiments. IC₅₀ for HCT116 antiproliferative activity, n = 4.

Required pretreatment with DTT to reduce the disulfide bond.

NI denotes no significant inhibition if inhibition percent is <20% at the maximum tested concentration (1 μM for all compounds).

Percent inhibition at the highest concentration tested (1 μM).

Table 1. Inhibition of Purified HDACs and Growth of HCT116 Cancer Cells by Largazole and Disulfide Analogues (IC50 ± SD, nM).