Effect of BISINDs on NBT-R activity in NB4 cells
| Compound | Chemical structure | Activity | Differentiation AC50 or IC50 (μM) | Differentiation Relative potency, (10 μM) | Cytotoxicity (μM) | Cell growth (10 μM) % T/C |
|---|---|---|---|---|---|---|
| ST1707 |  | potentiating | 2.7 ± 2.0 | +108 (±10) | >10 | 98 ± 6 |
| ST1346 |  | potentiating | 2.8 ± 1.6 | +95 (±11) | >50 | 81 ± 5 |
| ST1422 |  | potentiating | 8.2 ± 1.8 | +76 (±7) | >50 | 97 ± 16 |
| ST1860 |  | potentiating | 3.2 ± 0.6 | +76 (±6) | >10 | 88 ± 7 |
| ST1381 |  | potentiating | 0.3 ± 0.2 | +55 (±2) | >10 | 83 ± 3 |
| ST1730 |  | nil | ND | +18 (±7)* | >1 | ND |
| ST1350 |  | nil | 21.8 ± 0.1 | +3 (±1) | >50 | 98 ± 3 |
| ST1866 |  | nil | >50 | −2 (±1) | >50 | 122 ± 6 |
| ST1371 |  | nil | 27.7 ± 0.3 | −3 (±1) | >50 | 100 ± 4 |
| ST1385 |  | inhibitory | 0.5 ± 0.1 | −43 (±1) | >5 | ND |
| ST1345 |  | inhibitory | 0.7 ± 0.1 | −56 (±1) | >5 | ND |
| ST1750 |  | inhibitory | 3.2 ± 0.6 | −67 (±4) | >50 | 74 ± 1 |
| Compound | Chemical structure | Activity | Differentiation AC50 or IC50 (μM) | Differentiation Relative potency, (10 μM) | Cytotoxicity (μM) | Cell growth (10 μM) % T/C |
|---|---|---|---|---|---|---|
| ST1707 | | potentiating | 2.7 ± 2.0 | +108 (±10) | >10 | 98 ± 6 |
| ST1346 | | potentiating | 2.8 ± 1.6 | +95 (±11) | >50 | 81 ± 5 |
| ST1422 | | potentiating | 8.2 ± 1.8 | +76 (±7) | >50 | 97 ± 16 |
| ST1860 | | potentiating | 3.2 ± 0.6 | +76 (±6) | >10 | 88 ± 7 |
| ST1381 | | potentiating | 0.3 ± 0.2 | +55 (±2) | >10 | 83 ± 3 |
| ST1730 | | nil | ND | +18 (±7)* | >1 | ND |
| ST1350 | | nil | 21.8 ± 0.1 | +3 (±1) | >50 | 98 ± 3 |
| ST1866 | | nil | >50 | −2 (±1) | >50 | 122 ± 6 |
| ST1371 | | nil | 27.7 ± 0.3 | −3 (±1) | >50 | 100 ± 4 |
| ST1385 | | inhibitory | 0.5 ± 0.1 | −43 (±1) | >5 | ND |
| ST1345 | | inhibitory | 0.7 ± 0.1 | −56 (±1) | >5 | ND |
| ST1750 | | inhibitory | 3.2 ± 0.6 | −67 (±4) | >50 | 74 ± 1 |
NB4 cells were treated with increasing concentrations of the indicated BISIND in the presence or absence of ATRA (0.1 μM), and dose-response curves for NBT-reducing activity and cell growth similar to those reported in Figure 1 were constructed. Differentiation AC50 = the concentration of the compound giving 50% of the maximal induction of NBT-reducing activity in the presence of ATRA. Differentiation relative potency is the percent increase in NBT-reducing activity observed for a given combination of BISIND (at the concentration of 10 μM) and ATRA over that observed with ATRA alone. A “+” symbol indicates potentiation and a “−” symbol indicates inhibition. A value below 30% is considered negative, and the test compound is labeled as inactive (nil activity). In the case of ST1730, the value was calculated at the concentration of 1 μM. The value under the column labeled “Cytotoxicity” indicates the concentration of test compound above which we observed a decrease in cell viability of at least 40% following a standard treatment period of 3 days. The effect on cell growth was evaluated following 3 days of treatment with the test compound alone (10 μM). The value is expressed as the percentage of the total number of viable cells in treated (T) versus control (C) conditions. Each value is the mean ± SD of 3 separate culture dishes.