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

CAS: 2183470-09-7 Cat. No.: G655048 Formula: C₁₉H₁₂Cl₂F₂N₄O₃S Peso molecolare: 485.29 PubChem CID: 137347437

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

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

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

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Tipo di azione

INHIBITOR

Nomi e identificatori

PubChem CID

137347437

Peso molecolare

485.29