产品描述:
GCN2iB is an inhibitor of general control nonderepressible 2 kinase (GCN2; IC50 = 2.4 nM).{65974} It is selective for GCN2 over a panel of 465 kinases but does inhibit MAP2K5, eukaryotic translation initiation factor 2α kinase 2 (EIF2AK2), and MAP3K20 at 1 µM. GCN2iB (1 µM), in combination with L-aspariginase, reduces the viability of mouse embryonic fibroblasts (MEFs). It decreases the levels of activating transcription factor 4 (ATF4) and phosphorylated GCN2 in combination with L-aspariginase in CCRF CEM leukemia cells when used at a concentration of 0.4 µM. In vivo, GCN2iB (10 mg/kg twice per day), in combination with L-aspariginase, reduces tumor volume in CCRF CEM and MV4-11 leukemia mouse xenograft models.