product name Akti-1/2
Description: Akti-1/2 is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. AKTi-1/2, also known as AKT inhibitor VIII, is a potent, selective and ell permeable, allosteric inhibitor of Akt 1 and 2, which efficiently inhibits CaMKIα activity and aryl hydrocarbon receptor pathway. Akti-1/2 suppresses hyperthermia-induced Ndrg2 phosphorylation in gastric cancer cells. Akti-1/2 displays good selectivity against a panel of 70 other kinases with micromolar inhibition against some kinases, for example, calcium/calmodulin-dependent protein kinase 1 and smooth muscle myosin light-chain kinase.
References: Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4; Diabetes. 2007 Sep;56(9):2218-27.
551.64
Formula
C34H29N7O
CAS No.
612847-09-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (39.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonym
Akt Inhibitor VIII
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394499
| In Vitro |
Kinase Assay: 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). Cell Assay: 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. Cell lines: HCC827, NCI-H522, NCI-1651, and PC-9 cells In a cell-based IPKA (C33A) assay, Akti-1/2 inhibits Akt1 and Akt2 with IC50 of 305 nM and 2086 nM, respectively. In HT29, MCF7, and A2780 cells, Akti-1/2 induces cell apoptosis by dramatically increasing caspase-3 activity. In liver cells, Akti-1/2 blocks insulin regulation of PEPCK, G6Pase expression, and FOXO1 activity. Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. In HCC827, NCI-H522, NCI-1651, and PC-9 cells, Akti-1/2 inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination with gefitinib, Akti-1/2 causes enhanced inhibition of cell growth and apoptosis. |
|---|---|
| In Vivo | In mice, Akti-1/2 (50 mg/kg, i.p.) inhibits basal and IGF-stimulated Akt1 and Akt2 phosphorylation in lung. |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4; Diabetes. 2007 Sep;56(9):2218-27. |
Related Posts
product name Akti-1/2
Description: Akti-1/2 is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. AKTi-1/2, also known as AKT inhibitor VIII, is a potent, selective and ell permeable, allosteric inhibitor of Akt 1 and 2, which efficiently inhibits CaMKIα activity and aryl hydrocarbon receptor pathway. Akti-1/2 suppresses hyperthermia-induced Ndrg2 phosphorylation in gastric cancer cells. Akti-1/2 displays good selectivity against a panel of 70 other kinases with micromolar inhibition against some kinases, for example, calcium/calmodulin-dependent protein kinase 1 and smooth muscle myosin light-chain kinase.
References: Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4; Diabetes. 2007 Sep;56(9):2218-27.
551.64
Formula
C34H29N7O
CAS No.
612847-09-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (39.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonym
Akt Inhibitor VIII
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394499
| In Vitro |
Kinase Assay: 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). Cell Assay: 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. Cell lines: HCC827, NCI-H522, NCI-1651, and PC-9 cells In a cell-based IPKA (C33A) assay, Akti-1/2 inhibits Akt1 and Akt2 with IC50 of 305 nM and 2086 nM, respectively. In HT29, MCF7, and A2780 cells, Akti-1/2 induces cell apoptosis by dramatically increasing caspase-3 activity. In liver cells, Akti-1/2 blocks insulin regulation of PEPCK, G6Pase expression, and FOXO1 activity. Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. In HCC827, NCI-H522, NCI-1651, and PC-9 cells, Akti-1/2 inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination with gefitinib, Akti-1/2 causes enhanced inhibition of cell growth and apoptosis. |
|---|---|
| In Vivo | In mice, Akti-1/2 (50 mg/kg, i.p.) inhibits basal and IGF-stimulated Akt1 and Akt2 phosphorylation in lung. |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4; Diabetes. 2007 Sep;56(9):2218-27. |