A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC 50 s of 12 nM, 45 nM and 7.5 nM against the ALK5, ALK4 and ALK7 induced transcription, respectively [1].

ALK4 (cell-based assay):45 nM , ALK7 (cell-based assay):7.5 nM , ALK5 (cell-based assay):12 nM

A 83-01 sodium salt is a powerful inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, significantly reducing ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells. It also inhibits ALK4-TD and ALK7-TD induced transcription in R4-2 cells with IC50 values of 45 nM and 7.5 nM, respectively, while only mildly suppressing transcription induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. At concentrations ranging from 0.03-10 μM, A 83-01 effectively counteracts the growth-inhibitory effects of TGF-β, completely negating this effect at 3 μM. Furthermore, A 83-01 at 1-10 μM prevents TGF-β-induced Smad activation in HaCaT cells, and at 1 μM, it decreases TGF-β1-enhanced cell motility, adhesion, and invasion in HM-1 cells without affecting cell proliferation.

A 83-01, administered intraperitoneally (i.p.) at doses of 50, 150, and 500 μg/mouse, significantly enhances survival rates in mice without affecting their body weight or neurobehavioral functions [2]. At a dosage of 0.5 mg/kg, A 83-01 exhibits a pronounced antitumor effect in mice with M109 cells [3].