Formulation: A crystalline solid
Formal Name: 3-(1H-indazol-6-yl)-N-[1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine
Purity: ≥90%
Formula Markup: C19H18N10O
Formula Weight: 402,4
Shelf life (days): 1460
CAS Number: 1448693-69-3
Notes: 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.{69158} 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).{69157} 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).