Description: GCN2iB acetate is a novel, potent and ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM. GCN2iB has the potential to be used for the treatment of cancer. The inhibition of GCN2 sensitizes cancer cells with low basal-level expression of asparagine synthetase (ASNS) to the antileukemic agent L-asparaginase (ASNase) in vitro and in vivo.
References: 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.
Related CAS #: 2183470-12-2 (free base) 2183470-13-3 (acetate)