LDN-193189 dihydrochloride

LDN-193189 inhibits transcriptional activity of the (Bone Morphogenetic Protein) BMP type I receptors known as activin receptor-like kinases (ALKs). It inhibits ALK2 and ALK3 with IC₅₀ values of 5 nM and 30 nM respectively and shows weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7. It inhibits phosphorylation of the BMP signaling effectors SMAD1, SMAD5 and SMAD8 with IC₅₀ value of 5 nM. LDN-193189 significantly reduces tumor growth in SCID mice bearing MDA-PCa-118b tumors.