Background:

LDN193189 is a selective transcriptional activity?morphogenetic protein (BMP) type I receptors inhibitor. It inhibits activin receptor-like kinase-2 (ALK2) and ALK3 with IC50 values of 5 nM and 30 nM, respectively [1].

LDN193189 has been showed to inhibit BMP induced phosphorylation of Smad signaling (Smad1/5/8) and non-Smad signaling including p38 and Akt in C2C12 cells [2].

Pharmacological inhibition of BMP by LDN193189 has shown to prevent down-regulation of E-cadherin in response to BMP2 both in bronchial epithelial (Beas2B) cells and in C57BL/6 mice. LDN193189 also inhibits the BMP-induced reduction of epithelial permeability at cellular level [3].

参考文献:
[1] Yu PB,?Deng DY,?Lai CS,?Hong CC,?Cuny GD,?Bouxsein ML,?Hong DW,?McManus PM,?Katagiri T,?Sachidanandan C,?Kamiya N,?Fukuda T,?Mishina Y,?Peterson RT,?Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med.?2008 Dec;14(12):1363-9.
[2] Boergermann JH1,?Kopf J,?Yu PB,?Knaus P. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol.?2010 Nov;42(11):1802-7.
[3] Helbing T1,?Herold EM,?Hornstein A,?Wintrich S,?Heinke J,?Grundmann S,?Patterson C,?Bode C,?Moser M. Inhibition of BMP activity protects epithelial barrier function in lung injury. J Pathol.?2013 Sep;231(1):105-16. doi: 10.1002/path.4215. Epub 2013 Jul 10.