An inhibitor of GCN2
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GCN2-IN-1

Item No. 36027

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1448693-69-3
Synonyms
  • A-92
  • GCN2 Inhibitor 1
  • General Control Nonderepressible 2 Kinase Inhibitor 1
Molecular Formula
C19H18N10O
Formula Weight
402.4
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
N1(C2=CC=C3C=NNC3=C2)N=NC4=CN=C(NC5=CN(C6CCOCC6)N=C5)N=C14
InChi Code
InChI=1S/C19H18N10O/c1-2-15(7-16-12(1)8-21-25-16)29-18-17(26-27-29)10-20-19(24-18)23-13-9-22-28(11-13)14-3-5-30-6-4-14/h1-2,7-11,14H,3-6H2,(H,21,25)(H,20,23,24)
InChi Key
CFNFLNGJQOHNPR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Torres, C., Garling, A., Taouji, S., et al. Targeting the integrated stress response kinase GCN2 to modulate retroviral integration. Molecules 26(17), 5423 (2021).

    2. Filippova, N., Yang, X., Ananthan, S., et al. Targeting the HuR oncogenic role with a new class of cytoplasmic dimerization inhibitors. Cancer Res. 81(8), 2220-2233 (2021).