Table 2.
compd | R1 | R2 | R3 | IRE1β RNase IC50 (nM) | IRE1α RNase IC50 (nM) | IRE1β RNase Selectivity (Fold) |
---|---|---|---|---|---|---|
8 | 4.4 ± 0.7 | 22 ± 9 | 5.0 | |||
9 | 120 ± 40 | 120 ± 10 | 1.0 | |||
10 | 50 ± 2 | 6.0 ± 1.7 | 0.12 | |||
11 | 99 ± 56 | 57 ± 11 | 0.57 | |||
12 | 150 ± 30 | 130 ± 70 | 0.87 | |||
13 | 3.9 ± 1.1 | 240 ± 50 | 60 | |||
14 | 13 ± 2 | 110 ± 10 | 8.1 | |||
15 | 3.5 ± 1.4 | 390 ± 270 | 110 | |||
16 | 430 ± 70 | 2000 ± 100 | 4.5 | |||
17 | 74 ± 14 | 270 ± 70 | 3.6 | |||
18 | 17 ± 2 | 83 ± 8 | 5.8 |
RNase IC50 data are shown as mean ± SEM, n=3. RNase selectivity was determined by dividing the IRE1α RNase IC50 by the IRE1β RNase IC50 value for each inhibitor (individual IC50 curves provided in Supp. Figure 2).