GCN2-IN-6
CAS No. 2183470-09-7
GCN2-IN-6 ( —— )
产品货号. 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).?
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥2357 | 有现货 |
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50MG | ¥11016 | 有现货 |
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100MG | ¥18792 | 有现货 |
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200MG | 获取报价 | 有现货 |
|
500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称GCN2-IN-6
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述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).?
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产品描述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.
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同义词——
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通路Others
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靶点Other Targets
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受体nitric oxide
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研究领域——
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适应症——
化学信息
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CAS Number2183470-09-7
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分子量485.3
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分子式C19H12Cl2F2N4O3S
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纯度>98% (HPLC)
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溶解度——
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SMILESNc1ncc(cn1)C#Cc1c(F)ccc(NS(=O)(=O)c2cc(Cl)cc(CO)c2Cl)c1F
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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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