gcn2

GCN2-IN-1 (A-92) is an effective GCN2 inhibitor and can be utilized in cancer research as a chemotherapeutic agent.

GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells). GCN2-IN-6  is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9

GCN2-IN-7 is an orally active, potent and selective inhibitor of the environmental sensing protein GCN2 with anti-tumor activity and can be used to study melanoma.

GCN2iB is an ATP-competitive inhibitor of serine threonine protein kinase, stress-responsive kinase (GCN2), with IC50 of 2.4 nM.

GCN2iB is a GCN2 inhibitor. GCN2iB may be useful 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.

AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) that induces autophagy. It also inhibits GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM), making it useful for cancer research.

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.

T-3861174 is a prolyl tRNA synthetase (PRS) inhibitor, exhibiting significant in vitro anti-tumor activity with GCN2-ATF4 pathway activation.

HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.

OPB-171775 is a molecular glue that forms a ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). This compound induces cell death mediated by SLFN12 RNase, activates the SLFN12 RNase-associated GCN2 signaling pathway, and demonstrates antitumor activity.