Biological Activity
TP0427736 is a potent ALK5 kinase inhibitor with IC50 of 2.72 nM and IC50 of 836 nM for ALK3. It also inhibits TGF-β1-induced phosphorylation of Smad2/3 in A549 cells with IC50 of 8.68 nM.
in vitro
TP0427736 can inhibit Smad2/3 phosphorylation in a concentration-dependent manner with IC50 of 8.68 nM. In outer root sheath cells, it rescued the inhibition of cell proliferation by TGF-β1 and TGF-β2.
in vivo
TP0427736 reduces hair follicle length shortening during the transition from anagen to catagen.
target
| Target | Value |
ALK5
(Cell-free assay) | 2.72 nM |
