| Name | GCN2-IN-6 |
| Description | GCN2-IN-6 is a potent and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50: 1.8 nM) and cellular assays (IC50: 9.3 nM). GCN2-IN-6 is also an eIF2α kinase PERK inhibitor with IC50s of 0.26 nM in enzymatic assay and 230 nM in cells respectively. |
| In vitro | 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. 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 asparagine depleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. |
| In vivo | GCN2-IN-6 ( 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.3 mM), Sonication is recommended.
DMSO : 250 mg/mL (515.16 mM), Sonication is recommended.
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| Keywords | PERK, in-house enzymatic | PERK, cellular assays | PERK | Inhibitor | inhibit | GCN2-IN-6 | GCN-2-IN-6 | GCN2IN6 | GCN2, in-house enzymatic | GCN2, cellular assays | GCN2 IN 6 | GCN2 | Eukaryotic Initiation Factor (eIF) |
| Inhibitors Related | MSU-42011 | BTdCPU | GP 1a | GSK2606414 | GCN2-IN-7 | DNL343 | Azoramide | SHP099 | PERK-IN-4 | ATPγS tetralithium salt | CCT020312 | 4EGI-1 |
| Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Kinase Inhibitor Library | Inhibitor Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library |
United States
