GCN2-IN-6
CAS No. 2183470-09-7
GCN2-IN-6 ( —— )
Catalog No. M26228 CAS No. 2183470-09-7
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).?
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
5MG | 262 | Get Quote |
|
50MG | 1224 | Get Quote |
|
100MG | 2088 | Get Quote |
|
200MG | Get Quote | Get Quote |
|
500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameGCN2-IN-6
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NoteResearch use only, not for human use.
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Brief DescriptionGCN2-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).?
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DescriptionGCN2-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.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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Recptornitric oxide
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Research Area——
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Indication——
Chemical Information
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CAS Number2183470-09-7
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Formula Weight485.3
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Molecular FormulaC19H12Cl2F2N4O3S
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Purity>98% (HPLC)
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Solubility——
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SMILESNc1ncc(cn1)C#Cc1c(F)ccc(NS(=O)(=O)c2cc(Cl)cc(CO)c2Cl)c1F
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Güney HZ, G?rgün CZ, Tun?tan B, Uluda? O, Hodo?lugil U, Abacio?lu N, Zengil H. Circadian-rhythm-dependent effects of L-NG-nitroarginine methyl ester (L-NAME) on morphine-induced analgesia. Chronobiol Int. 1998 May;15(3):283-9.
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