GCN2-IN-6

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM) . GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells) [1]. GCN2-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[2183470-09-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Eukaryotic Initiation Factor (eIF)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gcn2-in-6.html

Purity

98.89

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=S(C1=CC(Cl)=CC(CO)=C1Cl)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O

Molecular Formula

C19H12Cl2F2N4O3S

Molecular Weight

485.29

Precautions

H302, H315, H319, H335

References & Citations

[1]Fujimoto J, et al. Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode. ACS Med Chem Lett. 2019 Sep 19;10 (10) :1498-1503.