GCN2-IN-1 (A-92)

GCN2-IN-1 is an inhibitor of general control nonderepressible 2 kinase (GCN2; IC₅₀ = ~0.2 μM for autophosphorylation), a serine/threonine protein kinase involved in the integrated stress response.¹ It also inhibits integrase phosphorylation (IC₅₀ = ~0.2 μM for the HIV-1 enzyme). GCN2-IN-1 inhibits ELAV-like protein 1, also known as human antigen R (HuR), protein dimerization (IC₅₀ = 4.5 μM).² GCN2-IN-1 also decreases the viability of U251, XD456, U87, and LN-229 glioma cells (IC₅₀s = 4.7, 2.8, 3.2, and 2.7 μM, respectively).

References:
1.Torres, C., Garling, A., Taouji, S., et al.Targeting the integrated stress response kinase GCN2 to modulate retroviral integrationMolecules26(17)5423(2021)
2.Filippova, N., Yang, X., Ananthan, S., et al.Targeting the HuR oncogenic role with a new class of cytoplasmic dimerization inhibitorsCancer Res.81(8)2220-2233(2021)