GCN2-IN-6 - 10mM in DMSO , CAS No.2183470-09-7

CAS: 2183470-09-7 Cat. No.: G655048 Molecular Weight: 485.29 PubChem CID: 137347437

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic ( IC 50 of 1.8 nM) and cellular assays ( IC 50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC 50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells)

In Vitro

To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF.? GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral administration; for 8 hours; mice) treatment at 3 mg/kg suppresses both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice bearing CCRF-CEM cells xenografts Dosage: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg Administration: Oral administration; for 8 hours Result: Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.

IC50& Target:GCN2

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic ( IC 50 of 1.8 nM) and cellular assays ( IC 50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC 50 of 0.26 nM (in enzymatic assa

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• PubChem CID: 137347437
• Molecular Weight: 485.29