Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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). GCN2-IN-6 is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 27,000 |
5 mg | 在庫あり | ¥ 66,500 |
10 mg | 在庫あり | ¥ 104,500 |
25 mg | 在庫あり | ¥ 204,000 |
50 mg | 約6-8 週間 | ¥ 312,500 |
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 73,000 |
ターゲット&IC50 | GCN2:1.8 nM (IC50, in-house enzymatic), GCN2:9.3 nM (IC50, cellular assays), PERK:0.26 nM (IC50, in-house enzymatic), PERK:230 nM (cellular assays) |
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. |
分子量 | 485.29 |
分子式 | C19H12Cl2F2N4O3S |
CAS No. | 2183470-09-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (515.16 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GCN2-IN-6 2183470-09-7 Apoptosis Others PERK Eukaryotic Initiation Factor (eIF) GCN2 IN 6 GCN2IN6 Inhibitor inhibit GCN-2-IN-6 inhibitor