产品
编 号：F276231
分子式：C19H12Cl2F2N4O3S
分子量：485.29
分子式：C19H12Cl2F2N4O3S
分子量：485.29
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2183470-09-7
产品详情
生物活性：
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). 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 click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
经天冬酰胺酶预处理后，GCN2-IN-6 (Compound 6d；0.3-3 mg/kg；口服) 在 3 mg/kg 剂量下，抑制 GCN2 和下游效应物 ATF4 的自磷酸化至基础水平。Animal Model:Mice bearing CCRF-CEM cells xenografts
Dosage:0.3 mg/kg, 1 mg/kg, and 3 mg/kg
Administration:Oral administration; for 8 hours
Result:Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.
体外研究：
为了检查 GCN2 抑制对癌细胞增殖的影响，在存在天冬酰胺消耗剂天冬酰胺酶的情况下，用 GCN2-IN-6 (化合物 6d) 处理急性淋巴细胞白血病 (ALL) CCRFCEM 细胞。用 GCN2-IN-6 处理可大大提高 CCRF-CEM 细胞对天冬酰胺酶的敏感性。在 GCN2 野生型 (WT) 小鼠胚胎成纤维细胞 (MEF) 中观察到通过组合天冬酰胺酶和 GCN2-IN-6 处理实现的适度抗增殖作用，但在 GCN2 敲除 (KO) MEF 中没有观察到。GCN2-IN-6 可抑制天冬酰胺酶激活的 p-GCN2、p-eIF2α 和 ATF4。
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). 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 click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
经天冬酰胺酶预处理后，GCN2-IN-6 (Compound 6d；0.3-3 mg/kg；口服) 在 3 mg/kg 剂量下，抑制 GCN2 和下游效应物 ATF4 的自磷酸化至基础水平。Animal Model:Mice bearing CCRF-CEM cells xenografts
Dosage:0.3 mg/kg, 1 mg/kg, and 3 mg/kg
Administration:Oral administration; for 8 hours
Result:Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.
体外研究：
为了检查 GCN2 抑制对癌细胞增殖的影响，在存在天冬酰胺消耗剂天冬酰胺酶的情况下，用 GCN2-IN-6 (化合物 6d) 处理急性淋巴细胞白血病 (ALL) CCRFCEM 细胞。用 GCN2-IN-6 处理可大大提高 CCRF-CEM 细胞对天冬酰胺酶的敏感性。在 GCN2 野生型 (WT) 小鼠胚胎成纤维细胞 (MEF) 中观察到通过组合天冬酰胺酶和 GCN2-IN-6 处理实现的适度抗增殖作用，但在 GCN2 敲除 (KO) MEF 中没有观察到。GCN2-IN-6 可抑制天冬酰胺酶激活的 p-GCN2、p-eIF2α 和 ATF4。
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