TP0427736 Chemical Properties

Boiling point:

634.7±65.0 °C(Predicted)

Density 

1.439±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: 67 mg/mL (200.09 mM);Ethanol: Insoluble

pka

9.70±0.10(Predicted)

Water Solubility 

Water: Insoluble

TP0427736 Usage And Synthesis

Uses

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].

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

References

[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

TP0427736(864374-00-5)Related Product Information

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