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 | – |
Mean IC50 value and standard error of at least three independent trials are shown (Figures S142-S148 and Tables S3-S9).
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.
“–” represents not determined.