A 83-01 sodium 是一种有效的 TGF-β I 型受体 ALK5，ALK4 和 ALK7 的抑制剂，能够抑制 ALK5，ALK4 和 ALK7 诱导的转录，IC₅₀ 值分别为 12 nM，45 nM 和 7.5 nM。

A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC 50 s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.

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ALK5 12 nM (IC50) ALK4 45 nM (IC50

A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation. has not independently confirmed the accuracy of the

A 83-01 (50, 150 and 500 μg/mouse, i.p.) sodium significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5 mg/kg, i.p.) sodium shows a significantly strong antitumor effect in mice bearing M109 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

In Vitro: DMSO : 50 mg/mL (112.48 mM; Need ultrasonic)配制储备液