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抑制剂/激活剂

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A 83-01

A-83-01 是一种有效的 TGF-β type I receptor (ALK5-TD) 的抑制剂，其IC50值为12 nM。A-83-01 还抑制由 activin/nodal type I receptor (ALK4-TD) 和 nodal type I receptor (ALK7-TD) 诱导的转录，对应的IC50值分别为45 nM和7.5 nM。在溶液中不稳定，请现配现用！

货号：
TK0429
规格：

1mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	909910-43-6
生物活性	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.
分子式	C25H19N5S
分子量	421.52
储存条件	-20°C, protect from light, stored under nitrogen *该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据	DMSO : 41.67 mg/mL (98.86 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
体内研究	A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells.
体外研究	A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and 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.

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