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)
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 |
|
1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameGCN2-IN-6
-
NoteResearch use only, not for human use.
-
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).?
-
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.
-
Synonyms——
-
PathwayOthers
-
TargetOther Targets
-
Recptornitric oxide
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number2183470-09-7
-
Formula Weight485.3
-
Molecular FormulaC19H12Cl2F2N4O3S
-
Purity>98% (HPLC)
-
Solubility——
-
SMILESNc1ncc(cn1)C#Cc1c(F)ccc(NS(=O)(=O)c2cc(Cl)cc(CO)c2Cl)c1F
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
-
Alisol B
Alisol B may be a potential novel therapeutic molecule for bone disorders through targeting the differentiation of osteoclasts as well as their functions.
-
Maltotriose
Maltotriose is a common oligosaccharide metabolite found in human urine after maltose ingestion or infusion. Maltotriose is increased in Glycogen storage disease II due to a mutation of the enzyme alpha-14-glucosidase.
-
Pyrimidine
Pyrimidines are heterocyclic six-membered nitrogen-containing carbon ring structures with uracil cytosine and thymine being the basal structures of ribose-containing nucleosides (uridine cytidine and thymidine respectively) or deoxyribose-containing deoxynucleosides and their corresponding ribonucleotides or deoxyribonucleotides.