A-83-01
货号：C909910
规格：50mg
品牌：OrganRegen
产品介绍
DESCRIPTION
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M. W t |
421.52 |
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Formula |
C97H124N20O31S |
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CAS No |
10047-33-3 |
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Storage |
Powder |
-20°C 3 years |
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Solubility |
DMSO |
41.67 mg/mL(98.86 mM; Need ultrasonic) |
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H2O |
< 0.1 mg/mL(insoluble) |
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技术参数
BIOLOGICAL ALTIVITY
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[1]. 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[2].
In Vivo
A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3].
REFERENCES