| Bioactivity | 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]. |
| Invitro | 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. 0 --> A 83-01 (Standard) 相关抗体: |
| In Vivo | 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. |
| CAS | 909910-43-6 |
| Formula | C25H19N5S |
| Molar Mass | 421.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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]. 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. |
A 83-01 (Standard)
CAS: 909910-43-6 F: C25H19N5S W: 421.52
A 83-01 (Standard) is the analytical standard of A 83-01 (HY-10432). This product is intended for research and analytica
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This product is for research use only, not for human use. We do not sell to patients.