A 77-01

中文名称:

A 77-01

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

CAS号:

607737-87-1

分子式:

C18H14N4

分子量:

286.33

EINECS号:

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

Mol文件:

607737-87-1.mol

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。

靶点

IC50: 25 nM (ALK5)

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.

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 Line:

Mv1Lu cells

Concentration:

1 µM

Incubation Time:

24 hours, 48 hours, 72 hours

Result:

Efficiently prevented the growth-inhibitory effects of TGF-β.

Cell Line:

HaCaT cells

Concentration:

1 µM

Incubation Time:

30 minutes

Result:

Inhibited TGF-β-induced phosphorylation of Smad2.