TABLE 1. Pharmacological Potencies, Toxicities and In Vitro Therapeutic Indices of Nrf2 Inducers in H4IIE-ARE8L Cells.
CDa (μM) | LC50b (μM) | Therapeutic indexc | |
---|---|---|---|
TP-225 | 0.0005 ± 0.0001 | 1.6 ± 0.2 | 3448.3 ± 698.2 |
BARD | 0.001 ± 0.0001 | 2.1 ± 0.5 | 1818.1 ± 356.3 |
TP-162 | 0.02 ± 0.009 | 18.4 ± 4.6 | 1397.7 ± 415.1 |
TP-151 | 0.01 ± 0.004 | 16.3 ± 3.7 | 1373.3 ± 201.5 |
TP-319 | 0.005 ± 0.001 | 1.9 ± 0.2 | 417.7 ± 72.1 |
SUL | 0.4 ± 0.1 | 51.9 ± 2.6 | 140.6 ± 38.4 |
TP-222 | 0.2 ± 0.02 | 7.2 ± 0.3 | 33.5 ± 2.1 |
DMF | 20.5 ± 8.7 | 184.4 ± 4.8 | 10.0 ± 3.7 |
TP-198 | 1.6 ± 0.6 | 8.1 ± 1.4 | 5.5 ± 1.4 |
TP-233 | 4.6 ± 2.1 | 10.4 ± 2.6 | 2.6 ± 1.4 |
TP-72 | 29.1 ± 2.7 | N.D.d | N.D.d |
aConcentration that provokes a twofold increase in ARE8L reporter transgene activity.
bConcentration that provokes a twofold decrease in cellular ATP content.
cRatio of LC50 divided by CD.
dNot determined, due to lack of ATP depletion at the highest possible concentration (100μM).