LDN193189

LDN193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. BMPs induce Smad1/5/8 plus non-Smad pathways, such as MAPK and Akt. BMP signaling pathway is the key regulator of cell fate decisions during embryogenesis and tissue homeostasis. It inhibits the activation of p38, ERK1/2 and Akt in C2C12 cells. LDN193189 only weakly inhibits ALK4, ALK5, and ALK7. LDN193189 affects not only the Smad but also the non-Smad signalling pathways induced by either BMP2, BMP6 or GDF5. LDN193189 inhibits ectopic ossification and it is a potential agent in the treatment of NSCLC lung tumors, showing significant in-vivo clinical utility. LDN193189 has been used to reduce ectopic ossification in a mouse model of Fibrodysplasia ossificans progressiva.