A 83-01

909910-43-6

421.52

DMSO : 30 mg/mL (71.17 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Protein Tyrosine Kinase/RTK; TGF-beta/Smad

A 83-01 is a potent inhibitor of TGF-beta 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.
IC50 & Target: IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)
In Vitro: A 83-01 is a potent inhibitor of TGF-beta 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 uM) potently prevents the growth-inhibitory effects of TGF-beta, and completely inhibits the effect at 3 uM. A 83-01 (1-10 uM) inhibits TGF-beta-induced Smad activation in HaCaT cells. A 83-01 (1 uM) decreases cell motility, adhesion and invasion increased by TGF-beta1 in HM-1 cells, but does not change cell proliferation.
In Vivo: A 83-01 (50, 150 and 500 ug/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.