864374-00-5

TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells[1].

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.

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.

TP0427736 reduces hair follicle length shortening during the transition from anagen to catagen.

Target	Value
ALK5 (Cell-free assay)	2.72 nM

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[1] Naruse T, et al. Novel ALK5 inhibitor TP0427736 reduces TGF-βinduced growth inhibition in human outer root sheath cells and elongates anagen phase in mouse hair follicles. Pharmacol Rep. 2017 Jun;69(3):485-491. DOI:10.1016/j.pharep.2017.01.024