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.
Peptides & proteins
LDN-193189, LDN 193189, 4-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline dihydrochloride
1) Yu, PB., et al. 2008. Nat Med. 14(12): 1363-1369. PMID: 19029982; 2) Yu, PB., et al. 2008. Nat Chem Biol. 4(1): 33-41. PMID: 18026094; 3) Cuny, GD. 2008. Bioorg Med Chem Lett. 18(15): 4388-4392. PMID: 18621530; 4) Heisenberg, CP. and Solnica-Krezel, L. 2008. Curr Opin Genet Dev. 18(4): 311-316. PMID: 18721878
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12 months from receipt