LDN193189 4HCl

LDN193189 tetrahydrochloride (CAS No.: 2310134-98-4) is the tetrahydrochloride form of LDN193189 (CAS No.: 1062368-24-4, Cat. No.: A8324). LDN193189 is a selective inhibitor of transcriptionally active bone morphogenetic protein (BMP) type I receptors, inhibiting activin receptor-like kinase-2 (ALK2) and ALK3, with IC50 values of 5 nM and 30 nM, respectively[1].

In C2C12 cells, LDN193189 inhibits BMP-induced phosphorylation of Smad signaling (Smad1/5/8) and non-Smad signaling, including p38 and Akt[2].

In bronchial epithelial (Beas2B) cells and C57BL/6 mice, pharmacological inhibition of BMP by LDN193189 prevents BMP2-induced downregulation of E-cadherin. LDN193189 also inhibits BMP-induced reduction of epithelial permeability at the cellular level[3].

References:

[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.