Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AKT inhibitor VIII (AKTi-1/2) is a highly specific Akt1/2 inhibitor (IC50: 58/210 nM). The selectivity for Akt1 is higher about 36-fold than Akt3.
説明 | AKT inhibitor VIII (AKTi-1/2) is a highly specific Akt1/2 inhibitor (IC50: 58/210 nM). The selectivity for Akt1 is higher about 36-fold than Akt3. |
ターゲット&IC50 | Akt1:58 nM, Akt2:210 nM |
In vitro | Akti-1/2 (50 mg/kg, i.p.) inhibits both basal and IGF-stimulated Akt1/2 phosphorylation in the lungs of mice. |
In vivo | In cell-based IPKA (C33A) assays, AKT inhibitor VIII suppresses Akt1/2 with IC50 values of 305 and 2086 nM, respectively. It significantly increases caspase-3 activity, inducing apoptosis in MCF7, HT29, and A2780 cells. In hepatocytes, it inhibits insulin's regulation of PEPCK and the expression of G6Pase and FOXO1 activity. Additionally, AKT inhibitor VIII enhances PAR-1-mediated platelet aggregation by blocking PKB. It inhibits cell growth in HCC827, NCI-H522, NCI-1651, and PC-9 cells with IC50 values of 4.7, 7.25, and 9.5 μM, respectively. When combined with gefitinib, the effects of suppressing cell growth and inducing apoptosis are enhanced. |
キナーゼ試験 | Kinase screen: Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol). |
細胞研究 | The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation.(Only for Reference) |
別名 | AKTi-1/2 |
分子量 | 551.64 |
分子式 | C34H29N7O |
CAS No. | 612847-09-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11 mg/mL (20 mM), Heating is recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
AKT inhibitor VIII 612847-09-3 Apoptosis Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt PKB Inhibitor AKTi-1/2 Protein kinase B inhibit inhibitor