A 83-01 (Standard) 

A 83-01 (Standard) is the analytical standard of A 83-01 (HY-10432). This product is intended for research and analytical applications. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC₅₀s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively^[1].

A 83-01 是 TGF-β I 型受体 ALK5 激酶、ALK4 和 ALK7 的有效抑制剂，在 Mv1Lu 细胞中降低 ALK-5 诱导的转录水平，IC₅₀ 为 12 nM，还阻断 ALK4-TD 和 ALK7-TD 诱导的转录，在 R4-2 细胞中的 IC₅₀ 分别为 45 nM 和 7.5 nM，并弱抑制由组成型活性 ALK-6、ALK-2 诱导的转录、ALK-3 和 ALK-1。A 83-01 (0.03-10 μM) 有效阻止 TGF-β 的生长抑制作用，并在 3 μM 时完全抑制该作用。A 83-01 (1-10 μM) 抑制 HaCaT 细胞中 TGF-β 诱导的 Smad 激活^[1]。A 83-01 (1 μM) 降低 HM-1 细胞中由 TGF-β1 增加的细胞运动性、粘附和侵袭，但不改变细胞增殖^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

A 83-01 (50、150 和 500 μg/只，腹腔注射) 显著提高无体重或神经行为表现小鼠的存活率^[2]。
A 83-01 (0.5 mg/kg, 腹腔注射) 对 M109 细胞小鼠有显著的抗肿瘤作用^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

421.52

C₂₅H₁₉N₅S

909910-43-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal Adriamycin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.  [Content Brief]