3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 CAS#: 909910-43-6

微信扫码

3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺价格(试剂级) 上下游产品信息

中文名称	3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺
中文同义词	3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺;化合物ALK5 INHIBITOR IV;83-01(DMSO溶液;3-(6-甲基吡啶-2-基)-N-苯基-4-(喹啉-4-基)-1H-吡唑-1-硫代甲酰胺;A 83-01,ALK4、5和7激酶抑制剂;3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)吡唑-1-硫代甲酰胺
英文名称	A-83-01
英文同义词	3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide;A 83-01;A83-01;TGF inhibitor A-83-01;3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide;TGF-β RI Kinase Inhibitor IV;A-83-01AB142092);ALK5 Inhibitor IV;A 83-01, >=98%
CAS号	909910-43-6
分子式	C25H19N5S
分子量	421.52
EINECS号
相关类别	小分子抑制剂;TGF-β抑制剂;抑制剂;小分子抑制剂，天然产物;Inhibitors;TGF-beta/Smad;Protein Kinase
Mol文件	909910-43-6.mol
结构式

3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 性质

3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 用途与合成方法

生物活性

A-83-01 是一种有效的 TGF-β type I receptor (ALK5-TD) 的抑制剂，其IC50值为12 nM。A-83-01 还抑制由 activin/nodal type I receptor (ALK4-TD) 和 nodal type I receptor (ALK7-TD) 诱导的转录，对应的IC50值分别为45 nM和7.5 nM。现配现用。

靶点

体外研究

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC     ₅₀    of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC     ₅₀    s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells. A 83-01 (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation.

体内研究

A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells.

安全信息

MSDS信息

3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 价格(试剂级)

3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 上下游产品信息