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. Author manuscript; available in PMC: 2019 Jan 1.
Published in final edited form as: Eur J Med Chem. 2017 Oct 31;143:1790–1806. doi: 10.1016/j.ejmech.2017.10.076

Table 2. IC50 values for SAHA, Tubastatin, SAHA analogs 1b-1f, (R)-1f, and (S)-1f against HDAC1, 2, 3, 6 and 8, and EC50 values with U937 cells.

Compound IC50 values (nM)a EC50 (μM)b,c
HDAC1 HDAC2 HDAC3 HDAC6 HDAC8 U937 cells
SAHAd 33 ± 1 96 ± 10 20 ± 1 33 ± 3 540 ± 10 0.88 ± 0.13
Tubastatind 2,700 ± 200 3,900 ± 400 2,900 ± 500 31 ± 4 330 ± 10 83 ± 8
PCI-34051 210 ± 30
1b (ethyl) 4,400 ± 300 4,900 ± 400 6,000 ± 1200 160 ± 10 130 ± 3
1c (n- butyl) 15,000 ± 1000 18,000 ± 2000 23,000 ± 3000 88 ± 7 74 ± 2 34 ± 2
1d (n-hexyl) 35,000 ± 1000 38,000 ± 3000 30,000 ± 3000 140 ± 10 79 ± 3 16 ± 3
1e (phenyl) 11,000 ± 1000 12,000 ± 1000 23,000 ± 2000 110 ± 10 290 ± 20
1f (benzyl) 29,000 ± 1000 32,000 ± 2000 42,000 ± 4000 140 ± 10 57 ± 2 28 ± 7
(R)-1f 25,000 ± 2000 36,000 ± 3000 27,000 ± 2000 48 ± 8 27 ± 2
(S)-1f 40,000 ± 1000 51,000 ± 1000 37,000 ± 2000 95 ± 9 150 ± 10
a

Mean IC50 value and standard error of at least three independent trials are shown (Figures S142-S148 and Tables S3-S9).

b

Mean EC50 value and standard error of at least three independent trials are shown. Data in table is associated with Figures S150 and Table S11.

c

“–” represents not determined.

d

Previously reported IC50 values using the same assay procedure [28, 42].