LDN-193189

Cell lines

C2C12 myofibroblast cells; bronchial epithelial (Beas2B) cells

Preparation method

This compound is limited soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.005-5 μM. 30-60 min

Applications

LDN-193189 inhibited both BMP induced Smad1/5/8 phosphorylation and BMP-mediated induction of the p38 MAPK, Erk1/2 and Akt pathway in C2C12 cells. LDN-193189 dose-dependently inhibited the activation of Smad1/5/8, p38 and Akt. LDN-193189 induced a strong increase in phosphorylated p38 MAPK levels and a slight increase in p-Akt in C2C12 cells. LDN (10 μM, 60 min) induced p38 and Akt phosphorylation. LDN (0.5 μM, 30 min) inhibited BMP-mediated Smad1/5/8, p38, ATF2 and CREB phosphorylation.

Animal models

C57BL/6 mice

Dosage form

Intraperitoneal injection; 3 mg/kg every 12 h

Application

In Ad.Cre-injected, caALK2-expressing mice, treatment with LDN-193189 prevented radiographic lesions at P15. LDN-193189–treated mice appeared to preserve knee and ankle joints at P30 and P60. LDN-193189-treated mice showed no ectopic bone at P15 but did show enhanced cartilage formation in surrounding soft tissues. LDN-193189–treated mice showed mildly impaired range of motion even in the absence of radiographically visible disease at P30.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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]. 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.