Formulation: A solid
Formal Name: N-[3-[2-(2-amino-5-pyrimidinyl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxy-3-pyridinesulfonamide
Purity: ≥98%
Formula Markup: C18H12ClF2N5O3S
CAS Number: 2183470-12-2
Notes: 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.
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