ARQ 092

ARQ 092 is an allosteric, orally bioavailable, pan-Akt inhibitor (IC₅₀s = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively).¹ It is selective for Akt isoforms over a panel of 303 other kinases.¹ ARQ 092 binds inactive Akt and prevents membrane localization and full Akt activation.^1,2 It also directly inhibits the membrane-associated active form of Akt, preventing phosphorylation of downstream targets.^1,2 ARQ 092 inhibits the proliferation of a wide range of cancer cells in vitro, inhibits the mutated Akt form found in Proteus syndrome, and attenuates heterotypic cell-cell interactions in a mouse model of sickle cell disease.^1,2,3,4

WARNING This product is not for human or veterinary use.

1. Yu, Y., Savage, R.E., Eathiraj, S., et al. Targeting AKT1-E17K and the PI3K/AKT pathway with an allosteric AKT inhibitor, ARQ 092. PLoS One 10(10), e0140479 (2015).

2. Lapierre, J.-M., Eathiraj, S., Vensel, D., et al. 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), 6455-6469 (2016).

3. Kim, K., Li, J., Barazia, A., et al. ARQ 092, an orally-available, selective AKT inhibitor, attenuates neutrophil-platelet interactions in sickle cell disease. Haematologica 102(2), 246-259 (2016).

4. Lindhurst, M.J., Yourick, M.R., Yu, Y., et al. Repression of AKT signaling by ARQ 092 in cells and tissues from patients with Proteus syndrome. Sci. Rep. 5(17162), (2015).