中文同义词:
4-[3-(6-甲基-2-吡啶基)-1H-吡唑-4-基]喹啉;TGF-Β I型受体家族ALK5抑制剂(A 77-01)
英文名称:
4-[3-(6-METHYL-2-PYRIDINYL)-1H-PYRAZOL-4-YL]-QUINOLINE
英文同义词:
4-[3-(6-METHYL-2-PYRIDINYL)-1H-PYRAZOL-4-YL]-QUINOLINE;A 77-01;A-77-01;A77-01;4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]quinoline A 77-01;4-[3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline;CS-1775;4-[5-(6-methylpyridin-2-yl)-1~{H}-pyrazol-4-yl]quinoline
相关类别:
细胞生物学试剂;小分子抑制剂，天然产物;小分子抑制剂;抑制剂;Inhibitors
生物活性
A 77-01 是一种有效的 TGF-β I 型受体家族 ALK5 抑制剂，IC50 值为 25 nM。
体外研究
A-77-01 (0.01-10 µM; 25 hours; Mv1Lu cells) treatment effectively inhibits TGF-β-induced transcriptional activation in concentration-dependent fashion.
A-77-01 (1 µM; 24-72 hours; Mv1Lu cells) treatment efficiently prevents the growth-inhibitory effects of TGF-β.
A-77-01 (1 µM; 30 minutes; HaCaT cells) treatment inhibits TGF-β-induced phosphorylation of Smad2.
RT-PCR
Cell Line: Mv1Lu cells
Concentration: 0.01 µM, 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, 10 µM
Incubation Time: 25 hours
Result: Inhibited the luciferase activity induced by TGF-β in concentration-dependent fashion.
Cell Viability Assay
Cell Line: Mv1Lu cells
Concentration: 1 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Efficiently prevented the growth-inhibitory effects of TGF-β.
Western Blot Analysis
Cell Line: HaCaT cells
Concentration: 1 µM
Incubation Time: 30 minutes
Result: Inhibited TGF-β-induced phosphorylation of Smad2.
Concentration:
0.01 µM, 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, 10 µM
Result:
Inhibited the luciferase activity induced by TGF-β in concentration-dependent fashion.
Incubation Time:
24 hours, 48 hours, 72 hours
Result:
Efficiently prevented the growth-inhibitory effects of TGF-β.
Incubation Time:
30 minutes
Result:
Inhibited TGF-β-induced phosphorylation of Smad2.
