Acalisib (GS-9820)

Description: Acalisib (formerly known as GS-9820) is a novel, potent and highly selective inhibitor of p110deltathe beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with IC50 of 14 nM, it displays 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. Acalisib has potential immunomodulating and anticancer activities. PI3K-mediated signaling is often dysregulated in cancer cells.Acalisib inhibits the activity of PI3K, thereby preventing the production of the second messenger phosphatidylinositol-3, 4, 5-trisphosphate (PIP3), which decreases tumor cell proliferation and induces cell death.

References: J Biol Chem. 2013 Dec 6; 288(49):35346-57.