AKT-IN-VIII, also known as AKTi-1/2, is a potent, selective and ell permeable, allosteric inhibitor of Akt 1 and 2, which efficiently inhibits CaMKIα activity and aryl hydrocarbon receptor pathway. AKT-IN-VIII suppresses hyperthermia-induced Ndrg2 phosphorylation in gastric cancer cells. AKT-IN-VIII 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.
CAS Number: 612847-09-3
Molecular Weight: 551.64
Chemical Name: 3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
When LnCaP cells are pretreated with AKT-IN-VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT-IN-VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by AKT-IN-VIII pretreatment. The AKT-IN-VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions. AKT-IN-VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1).
Mice are dosed with AKT-IN-VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation.
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