Allosteric, selective, non-ATP competitive\xa0pan-Akt inhibitor (IC 50 = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively). Selective for Akt isoforms over a panel of 303 other kinases.
Storage Temp
Protected from light,Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR, INHIBITOR
Mechanism of action
Allosteric modulator of AKT serine/threonine kinase 1;Inhibitor of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Inhibitor of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3;Inhibit
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Shipped at 4°C. Store at -20°C. Store In the Dark. Store under desiccating conditions.
1.Lapierre JM, Eathiraj S, Vensel D, Liu Y, Bull CO, Cornell-Kennon S, Iimura S, Kelleher EW, Kizer DE, Koerner S et al.. (2016) Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.. J Med Chem, 59 (13):(6455-69). [PMID:27305487]
2.Yu Y, Savage RE, Eathiraj S, Meade J, Wick MJ, Hall T, Abbadessa G, Schwartz B. (2015) Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092.. PLoS ONE, 10 (10):(e0140479). [PMID:26469692]
3.Lindhurst MJ, Yourick MR, Yu Y, Savage RE, Ferrari D, Biesecker LG. (2015) Repression of AKT signaling by ARQ 092 in cells and tissues from patients with Proteus syndrome.. Sci Rep, 5 (3):(17162). [PMID:26657992]
4.Jiang Y et al.. (2022) Transcriptomic and ChIP-seq Integrative Analysis Identifies KDM5A-Target Genes in Cardiac Fibroblasts.. Front Cardiovasc Med, 9 (929030). [PMID:35845066]
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D2306314