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.
Chemical Formula: C34H29N7O
Exact Mass: 551.24336
Molecular Weight: 551.65
Elemental Analysis: C, 74.03; H, 5.30; N, 17.77; O, 2.90
AKT inhibitor VIII
InChi Code: InChI=1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
Morishita S, Tomita K, Ono T, Murakoshi M, Saito K, Sugiyama K, Nishino H, Kato H. Lactoferrin attenuates fatty acid-induced lipotoxicity via Akt signaling in hepatocarcinoma cells. Biochem Cell Biol. 2015 Jul 28:1-8. [Epub ahead of print] PubMed PMID: 26335364.
Myers AL, Lin L, Nancarrow DJ, Wang Z, Ferrer-Torres D, Thomas DG, Orringer MB, Lin J, Reddy RM, Beer DG, Chang AC. IGFBP2 modulates the chemoresistant phenotype in esophageal adenocarcinoma. Oncotarget. 2015 Jul 17. [Epub ahead of print] PubMed PMID: 26317790.
Xing W, Guo W, Zou CH, Fu TT, Li XY, Zhu M, Qi JH, Song J, Dong CH, Li Z, Xiao Y, Yuan PS, Huang H, Xu X. Acemannan accelerates cell proliferation and skin wound healing through AKT/mTOR signaling pathway. J Dermatol Sci. 2015 Aug;79(2):101-9. doi: 10.1016/j.jdermsci.2015.03.016. Epub 2015 Apr 1. PubMed PMID: 26049685.
Zheng S, Yang Y, Song R, Yang X, Liu H, Ma Q, Yang L, Meng R, Tao T, Wang S, He J. Ang-(1-7) promotes the migration and invasion of human renal cell carcinoma cells via Mas-mediated AKT signaling pathway. Biochem Biophys Res Commun. 2015 May 1;460(2):333-40. doi: 10.1016/j.bbrc.2015.03.035. Epub 2015 Mar 14. PubMed PMID: 25783053.
Halacli SO, Dogan AL. FOXP1 regulation via the PI3K/Akt/p70S6K signaling pathway in breast cancer cells. Oncol Lett. 2015 Mar;9(3):1482-1488. Epub 2015 Jan 16. PubMed PMID: 25663935; PubMed Central PMCID: PMC4315073.
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