2183470-13-3
Chemical Structure
GCN2iB acetate
- CAS No.: 2183470-13-3
- Formula:C20H16ClF2N5O5S
- Molecular Weight:511.89
IUPAC Name: N-(3-((2-aminopyrimidin-5-yl)ethynyl)-2,4-difluorophenyl)-5-chloro-2-methoxypyridine-3-sulfonamide acetate
InChIKey: QNHLMBSUYPVOLX-UHFFFAOYSA-N
SMILES: O=S(C1=CC(Cl)=CN=C1OC)(NC2=CC=C(C(C#CC3=CN=C(N=C3)N)=C2F)F)=O.CC(O)=O
Biological Activity: GCN2iB acetate is an ATP-competitive, selective GCN2 inhibitor with an IC50 of 2.4 nM. GCN2iB acetate inhibits the activation of the GCN2 pathway and upregulates GPX4. GCN2iB acetate enhances the anticancer effect of ASNase against acute lymphoblastic leukemia. GCN2iB acetate increases left ventricular ejection fraction, while reducing fasting blood glucose and myocardial fibrosis. GCN2iB acetate can be used in research related to acute lymphoblastic leukemia, acute myeloid leukemia and diabetic cardiomyopathy[1][2].
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GCN2iB acetate | GCN2iB acetate is an ATP-competitive, selective GCN2 inhibitor with an IC50 of 2.4 nM. GCN2iB acetate inhibits the activation of the GCN2 pathway and upregulates GPX4. GCN2iB acetate enhances the anticancer effect of ASNase against acute lymphoblastic leukemia. GCN2iB acetate increases left ventricular ejection fraction, while reducing fasting blood glucose and myocardial fibrosis. GCN2iB acetate can be used in research related to acute lymphoblastic leukemia, acute myeloid leukemia and diabetic cardiomyopathy. | |||||||||||||||||||||
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- [1]. Nakamura A, et al. Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response. Proc Natl Acad Sci U S A. 2018;115(33):E7776-E7785. [Content Brief]
- [2]. Yuan J, et al. Inhibition of GCN2 Alleviates Cardiomyopathy in Type 2 Diabetic Mice via Attenuating Lipotoxicity and Oxidative Stress. Antioxidants (Basel). 2022;11(7):1379. Published 2022 Jul 16. [Content Brief]
Keywords
