产品描述:
ARQ 092 is an allosteric, orally bioavailable, pan-Akt inhibitor (IC50s = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively).{33792} It is selective for Akt isoforms over a panel of 303 other kinases.{33792} ARQ 092 binds inactive Akt and prevents membrane localization and full Akt activation.{33792,33790} It also directly inhibits the membrane-associated active form of Akt, preventing phosphorylation of downstream targets.{33792,33790} 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.{33792,33790,32947,33791}