GCN2-IN-1 (A-92) (Synonyms: A-92, GCN2 Inhibitor 1, General Control Nonderepressible 2 Kinase Inhibitor 1) |
| Catalog No.GC32771 |
GCN2-IN-1 (A-92) (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
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Cas No.: 1448693-69-3
Sample solution is provided at 25 µL, 10mM.
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)
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