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Akt Inhibitor VIII does not exhibit any inhibitory effect against pleckstrin homology (PH) domain-lacking Akts, AGC family kinases, PKA, PKC or SGK. Akt Inhibitor VIII prevails over Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and has been shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 in cultured cells and in mice.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
| Molecular Weight | 551.64 |
| Formula | C34H29N7O |
| CAS Number | 612847-09-3 |
| Purity | >99% |
| Solubility | 10 mM in DMSO |
| Storage | at -20°C |
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GSK2141795 is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively (Clinical phase 1). |
| GDC-0068 (dihydrochloride)
GDC-0068(RG 7440) 2Hcl 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. |
| Afuresertib
Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2. |
| SC79
SC79 is an inhibitor of Akt-PH domain translocation and a specific Akt activator used to enhance Akt activity in various conditions. |
| AT-13148
AT-13148 is an oral, ATP-competitive inhibitor of multi-AGC kinases with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. |
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