| Name | Afuresertib |
| Description | Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. |
| Cell Research | A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference) |
| Kinase Assay | Potency (Ki*) of afuresertib: The true potency (Ki*) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ33P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2). |
| In vitro | Overall 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibited the kinase activity of the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration-dependent effect on the phosphorylation levels of multiple AKT substrates, including GSK3b, PRAS40, FOXO and cystatin 9. |
| In vivo | Overall 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibited the kinase activity of the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration-dependent effect on the phosphorylation levels of multiple AKT substrates, including GSK3b, PRAS40, FOXO and cystatin 9. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 250 mg/mL (585.04 mM), Sonication is recommended.
Ethanol : 79 mg/mL (184.87 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.68 mM), Sonication is recommended.
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| Keywords | ROK | ROCK | Rho-kinase | Rho-associated protein kinase | Rho-associated kinase | Protein kinase C | Protein kinase B | PKC | PKB | Inhibitor | inhibit | GSK-2110183 | GSK 2110183 | Akt3 | Akt2 | Akt1 | Akt | Afuresertib |
| Inhibitors Related | Aceglutamide | Musk ketone | Stearamide | Bisphenol A | Creatine monohydrate | Hyaluronic acid | α-Vitamin E | Ethyl linoleate | Artemisinin | Methyl eugenol | Chloramphenicol | 2,3-Butanediol |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | TGF-beta/Smad Compound Library |
United States
