GNE-493 is a low molecular weight, potent dual inhibitor of pan-PI3 kinases and mTOR. GNE-493 displays approximately equipotent inhibition of Class I PI3K isoforms, is submitted for screening in a 142 kinase panel provided by Invitrogen’s SelectScreen service. Of these kinases, only three are subject to greater than 50% inhibition by GNE-493, and none are inhibited greater than 80% when tested at 1 μM. Subsequently measured IC50s demonstrated that GNE-493 is more than 100-fold selective for PI3Kα over these three unrelated kinases (Aurora A IC50>10 μM, MLK1 IC50=591 nM and SYK IC50=371 nM)
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Alpelisib; Gedatolisib; AS-604850; CAY10505; AS-605240; Apitolisib; PIK-93; PIK-75 Hydrochloride; YM201636; ZSTK474; PI-103; PD98059; MTX-211; AKTIV; Duvelisib; TGX-221; LY294002