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A 83-01

CAS号

909910-43-6

分子式

C25H19N5S

主要靶点

ALK|TGF-beta/Smad

仅限科研使用

Cat No : CM11075

Print datasheet

Synonyms

A 83 01|A 8301|A 83-01|ALK|ALK5|ALK5 Inhibitor IV|ALK4|ALK7|A8301|A83-01|inhibit|Transforming growth factor beta receptors|Smad|TGF-β/Smad|TGFβ|TGF-β Receptor|TGFbeta|TGF-beta|TGFbeta/Smad|TGF-b/Smad|TGFb|Inhibitor

验证数据展示

  • CAS No.: 909910-43-6

    A 83-01
    CAS#: 909910-43-6

产品信息

CAS号 909910-43-6
分子式 C25H19N5S
主要靶点 ALK|TGF-beta/Smad
主要通路 血管生成|蛋白酪氨酸激酶|干细胞
分子量 421.52
纯度 98.20%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature | Powder: -20°C for 3 years | Shipping with blue ice.
别名 A 83 01|A 8301|A 83-01|ALK|ALK5|ALK5 Inhibitor IV|ALK4|ALK7|A8301|A83-01|inhibit|Transforming growth factor beta receptors|Smad|TGF-β/Smad|TGFβ|TGF-β Receptor|TGFbeta|TGF-beta|TGFbeta/Smad|TGF-b/Smad|TGFb|Inhibitor

靶点活性

ALK4:45 nM|ALK7:7.5 nM|ALK5:12 nM

体内活性

方法：为检测体内抗肿瘤活性，将 A 83-01 (150 μg/只) 腹腔注射给 HM-1 癌症腹膜扩散的 B6C3F1 小鼠模型，每周三次，持续四周。 结果：A 83-01 治疗组的腹水形成往往较慢，A 83-01 显著提高了小鼠的存活率。[2] 方法：为研究在心肌损伤中的作用，将 A 83-01 (10 mg/kg) 腹腔注射给 Nkx2.5 enh-Cre/mTmG 小鼠，每天一次，持续七天。 结果：A 83-01 治疗在基线和心肌损伤后显著增加了 Nkx2.5+ 心肌成肌细胞的数量，导致新形成的心肌细胞增加。A 83-01 治疗显著改善了心室弹性和卒中功，从而改善了损伤后的收缩能力。[3]

体外活性

方法：野生型水貂肺上皮细胞 Mv1Lu 用 A 83-01 (0.03-10 μM) 和 TGF-β (1 ng/mL) 处理 48 h，使用 Coulter counter 检测细胞增殖。 结果：A 83-01 以剂量依赖的方式阻止 TGF-β 对 Mv1Lu 细胞生长的抑制。[1] 方法：小鼠卵巢癌细胞 HM-1 用 A 83-01 (1-10 μM) 处理 30 min，随后用 TGF-β (1-10 ng/mL) 处理 60 min，使用 Western Blot 方法检测靶点蛋白表达水平。 结果：添加 TGF-β1 增加了 pSmad3 的表达，A 83-01 抑制了 TGF-β 的上调。[2]

溶解度

DMSO:10 mg/mL (23.72 mM);

细胞实验

HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A-83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay following the manufacturer's instructions.

参考文献

1.Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800.
2.Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.
3.Chen WP, et al. Pharmacological inhibition of TGFβ receptor improves Nkx2.5 cardiomyoblast-mediated regeneration. Cardiovasc Res. 2015 Jan 1;105(1):44-54.
4.Wei-jian L I, Zhen-yu W, Tian-jie Y, et al. The study of immortalized hepatocyte-derived liver progenitor-like cells used in bioartificial liver therapy[J]. Chinese Hepatolgy. 24(8): 871.
5.Gong-Bo Fu, Wei-Jian Huang, Min Zeng, Xu Zhou, Hong-Ping Wu, Chang-Cheng Liu, Han Wu, Jun Weng, Hong-Dan Zhang, Yong-Chao Cai, Charles Ashton, Min Ding, Dan Tang, Bao-Hua Zhang, Yi Gao, Wei-Feng Yu, Bo Zhai, Zhi-Ying He, Hong-Yang Wang, and He-Xin Yan . Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens [J]. Cell Research. 2019 Jan;29(1):8-22.

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