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GCN2-IN-1 (A-92)

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.

GCN2-IN-1 (A-92) Chemical Structure

Size Price Stock Qty
10mM (in 1mL DMSO)
$212.00
In stock
5mg
$193.00
In stock
10mg
$304.00
In stock
25mg
$607.00
In stock
50mg
$1,011.00
In stock
100mg
$1,747.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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)

Chemical Properties

Cas No. 1448693-69-3 SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES C1(NC2=CN(C3CCOCC3)N=C2)=NC=C(N=NN4C5=CC6=C(C=C5)C=NN6)C4=N1
Formula C19H18N10O M.Wt 402.41
Solubility DMSO : 60 mg/mL (149.10 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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