Akt1 Selective Inhibitors
| Catalog No. | Product Name | Information | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| S2670 | A-674563 | A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC. |
Selective | Akt1, Ki: 11 nM |
| S1113 | GSK690693 | GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1. |
Pan | Akt1, IC50: 2 nM |
| S8019 | AZD5363 | AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2. |
Pan | Akt1, IC50: 3 nM |
| S2808 | Ipatasertib (GDC-0068) | Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. Phase 2. |
Pan | Akt1, IC50: 5 nM |
| S1078 | MK-2206 2HCl | MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2. |
Pan | Akt1, IC50: 8 nM |
| S1558 | AT7867 | AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family. |
Pan | Akt1, IC50: 32 nM |
| S7563 | AT13148 | AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1. |
Pan | Akt1, IC50: 38 nM |
