Table 1 Biochemical evaluation of covalent-allosteric Akt inhibitors with the Akt isoforms.
From: Cellular model system to dissect the isoform-selectivity of Akt inhibitors
| IC50 [nM] | ||||
|---|---|---|---|---|---|
# | R | Akt1 | Akt2 | Akt3 | |
Capivasertib | 1 ± 0.3 | 4 ± 1 | 8 ± 1 | ||
MK-2206 | 10 ± 2 | 54 ± 18 | 720 ± 121 | ||
Borussertib | 1 ± 0.2 | 14 ± 1 | 431 ± 31 | ||
1 |
| 53 ± 13 | 599 ± 63 | 6627 ± 1128 | |
2 |
| 22 ± 2 | 150 ± 5 | 7509 ± 1821 | |
3 |
| 186 ± 79 | 961 ± 174 | >20,000 | |
4 |
| 44 ± 18 | 248 ± 49 | 6446 ± 742 | |
5 |
| 35 ± 4 | 116 ± 2 | 3396 ± 406 | |
6 |
| 112 ± 21 | 108 ± 31 | 5752 ± 1547 | |
7 |
| 7087 ± 3437 | 479 ± 91 | >20,000 | |
8 |
| 4566 ± 197 | 2068 ± 147 | >20,000 | |
9 |
| 5930 ± 793 | 4214 ± 412 | 8374 ± 1784 | |
10 |
| 1716 ± 166 | 94 ± 4 | 1564 ± 75 | |
11 |
| 643 ± 95 | 76 ± 11 | 1890 ± 621 | |
12 |
| 1281 ± 18 | 251 ± 18 | 607 ± 95 | |
13 |
| 98 ± 15 | 53 ± 5 | 3543 ± 617 | |
14 |
| 527 ± 14 | 23 ± 4 | 356 ± 88 | |
15 |
| 604 ± 31 | 1400 ± 112 | 4356 ± 1077 | |
16 |
| 9484 ± 665 | 682 ± 83 | 5339 ± 2006 | |
17 |
| 2853 ± 758 | 133 ± 9 | 2108 ± 441 | |
18 |
| 91 ± 13 | 39 ± 6 | 5266 ± 1030 | |
19 |
| 1797 ± 105 | 511 ± 62 | 1509 ± 389 | |
20 |
| 1631 ± 148 | 175 ± 2 | 187 ± 40 | |
21 |
| 2111 ± 268 | 99 ± 6 | 272 ± 84 | |
22 |
| 209 ± 40 | 55 ± 5 | 3049 ± 646 | |
23 |
| 130 ± 11 | 151 ± 25 | 6303 ± 1923 | |
