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A 83-01

现货
Catalog No.
A3133
ALK-5抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,200.00
现货
10mg
¥ 1,400.00
现货
50mg
¥ 4,050.00
Ship with 10-15 days

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Background

A 83-01 is a small-molecule inhibitor of activin receptorlike kinase (ALK)-5 with IC50 value of 12 nM [1].

A 83-01 inhibited 68% of the transcriptional activation induced by ALK-5 at concentration of 1 μM in Mv1LuR4-2 cells that transfected with luciferase reporter gene and constitutively active ALK-5. In cells transfected with luciferase reporter gene only, A 83-01 treatment inhibited the activity of ALK-5 induced by TGF-β (IC50 value was 12 nM) but not BMP. A 83-01 also showed inhibition on the activity of ALK-4 and ALK-7 in R4-2 cells with IC50 values of 45 and 7.5 nM, respectively. For other ALK receptors such as ALK-1, 2, 3 and 6, A 83-01 showed weak inhibition. Besides that, A 83-01 was proved to reduce the cell growth inhibition [1].

References:
1. Tojo M, Hamashima Y, Hanyu A, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer science, 2005, 96(11): 791-800.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt421.52
Cas No.909910-43-6
FormulaC25H19N5S
SynonymsA83-01;A-83-01
Solubility≥21.1 mg/mL in DMSO, ≥9.82 mg/mL in EtOH with ultrasonic and warming, <2.29 mg/mL in H2O
Chemical Name3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
SDFDownload SDF
Canonical SMILESCC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

Mv1Lu和C2C12细胞

制备方法

在DMSO中的溶解度大于21.1 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.01 ~ 10 μM;1小时

实验结果

在Mv1Lu细胞中,A-83-01呈浓度依赖性地降低TGF-β诱导的转录水平,其IC50值为25 nM。另一方面,在C2C12细胞中,1 μM A-83-01对BMP诱导的转录活性无影响。然而,当浓度超过3 μM时,A-83-01对BMP4诱导的转录活性显示出微弱的抑制作用。

References:

[1]. Tojo M, Hamashima Y, Hanyu A, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer science, 2005, 96(11): 791-800.

生物活性

Description A 83-01是一种TGF-β I型受体ALK5激酶\I型激活素/节点受体ALK4和I型节点受体ALK7的选择性抑制剂,IC50值分别为12 nM\45 nM和7.5 nM.
靶点 ALK5 ALK4 ALK7      
IC50 12 nM 45 nM 7.5 nM      

质量控制

质量控制和MSDS

批次:

化学结构

A 83-01