A 83-01
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A 83-01是一种激活素受体样激酶（ALK）-5的小分子抑制剂，IC50值为12 nM[1]。
在转染荧光素酶报告基因和组成型活性ALK-5的Mv1LuR4-2细胞中，A 83-01在浓度为1 μM时可抑制68%的由ALK-5诱导的转录激活。在只转染荧光素酶报告基因的细胞中，用A 83-01处理，可抑制由TGF-β诱导（IC50值为12 nM）而不是BMP诱导的ALK-5的活性。在R4-2细胞中，A 83-01也显示出对ALK-4和ALK-7的抑制活性，IC50值分别为45 nM和7.5 nM。对于其他ALK受体，比如ALK-1、2、3和6，A 83-01显示微弱的抑制作用。除此之外，A 83-01被证明可减弱细胞的生长抑制作用[1]。
参考文献：
[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.
- 1. XiangRong Luo, JianTao She, et al. "Establishment and characterization of organoids from a patient with adenomyoepithelioma of the breast." Bioengineered. 2021 Dec;12(2):11578-11585. PMID: 34874791
- 2. Changchun Shao, Xue Yang, et al. "The stemness of hepatocytes is maintained by high levels of lipopolysaccharide via YAP1 activation." Stem Cell Res Ther. 2021 Jun 10;12(1):342. PMID: 34112239
- 3. Kathryn E. Worley, Erin E. Edwards, et al. "The importance of cell-subtype selection in creation of a 3D liver fibrosis model." Lonza Pharma&Biotech.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 421.52 |
| Cas No. | 909910-43-6 |
| Formula | C25H19N5S |
| Synonyms | A83-01;A-83-01 |
| Solubility | ≥21.1 mg/mL in DMSO; insoluble in H2O; ≥9.82 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
Mv1Lu和C2C12细胞 |
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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。 |
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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。 |
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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. |
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| 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 | |||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
