GCN2iB（Cat No.:I019877）is a potent and selective inhibitor of GCN2, a serine/threonine protein kinase that is involved in the regulation of cellular stress responses. GCN2iB acts as an ATP-competitive inhibitor of GCN2, with an IC50 value of 2.4 nM. GCN2iB has been shown to inhibit the activation of GCN2 by amino acid deprivation in cells and to block the phosphorylation of eukaryotic initiation factor 2 alpha (eIF2α), a downstream target of GCN2. The inhibition of GCN2 by GCN2iB may have potential therapeutic applications in the treatment of certain diseases.
| Catalog Number | I019877 |
| CAS Number | 2183470-12-2 |
| Molecular Formula | C₁₈H₁₂ClF₂N₅O₃S |
| Purity | ≥95% |
| Storage | Store at -20°C |
| IUPAC Name | N-[3-[2-(2-aminopyrimidin-5-yl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxypyridine-3-sulfonamide |
| InChI | 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) |
| InChIKey | JGHVXJKGYJYWOP-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C(C=N1)Cl)S(=O)(=O)NC2=C(C(=C(C=C2)F)C#CC3=CN=C(N=C3)N)F |
| Reference | [1]. Nakamura A, et al. Inhibition of GCN2 sensitizes ASNS-low cancer cells by disrupting the amino acid response. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7776-E7785. |
