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
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Biological Information

  • Product Name
    GCN2-IN-6
  • Note
    Research use only, not for human use.
  • Brief 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).?
  • 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.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    nitric oxide
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2183470-09-7
  • Formula Weight
    485.3
  • Molecular Formula
    C19H12Cl2F2N4O3S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    Nc1ncc(cn1)C#Cc1c(F)ccc(NS(=O)(=O)c2cc(Cl)cc(CO)c2Cl)c1F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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.
molnova catalog
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