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A 83-01 sodium

CAS No. :

MCE 国际站：A 83-01 sodium

产品活性：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。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

In Vitro: 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 M) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 M. A 83-01 (1-10 M) inhibits TGF-β-induced Smad activation in HaCaT cells. A 83-01 (1 M) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation.

In Vivo: 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.

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