Network Version
A 83-01 Data Sheet
| Product Name: | A 83-01 |
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|---|---|---|
| CAS No.: | 909910-43-6 | |
| Cat. No.: | HY-10432 | |
| MWt: | 421.52 | |
| Formula: | C25H19N5S | |
| Purity : | >98% | |
| Solubility: | DMSO : 25 mg/mL (59.31 mM; ultrasonic and warming and heat to 60°C); H2O : < 0.1 mg/mL (insoluble) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| 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]. IC50 & Target: IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)[1] In Vitro: 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]. | ||
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