GCN2iB

GCN2iB is an inhibitor of general control nonderepressible 2 kinase (GCN2, IC50 = 2.4 nM). It is selective for GCN2 over a panel of 465 kinases but does inhibit MAP2K5, eukaryotic translation initiation factor 2alpha 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.Formal Name: N-[3-[2-(2-amino-5-pyrimidinyl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxy-3-pyridinesulfonamide. CAS Number: 2183470-12-2. Molecular Formula: C18H12ClF2N5O3S. Formula Weight: 451.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: O=S(NC1=CC=C(C(C#CC2=CN=C(N)N=C2)=C1F)F)(C3=CC(Cl)=CN=C3OC)=O. InChi Code: InChI=1S/C18H12ClF2N5O3S/c1-29-17-15(6-11(19)9-23-17)30(27,28)26-14-5-4-13(20)12(16(14)21)3-2-10-7-24-18(22)25-8-10/h4-9,26H,1H3,(H2,22,24,25). InChi Key: JGHVXJKGYJYWOP-UHFFFAOYSA-N.