LDN193189 (1062368-24-4) Description:
LDN193189 is a small molecule inhibitor of BMP type I receptors ALK2 and ALK3 (IC50 = 5 nM and 30 nM respectively).It only weakly inhibits ALK4, ALK5, and ALK7. LDN193189 functions primarily through prevention of Smad1, Smad5, and Smad8 phosphorylation. BMP signaling coordinates developmental patterning and has essential physiological roles in mature organisms. LDN-193189 has been used to reduce ectopic ossification in a mouse model. The role of BMP2 signals in the growth and angiogenesis of non-small-cell lung carcinoma (NSCLC) also suggest LDN-193189 may be a potent inhibitor of lung tumors.
Normal development and tissue repair are controlled in part by SMADs, a family of intracellular proteins that are activated by signaling via serine/threonine kinase receptors of the TGF-β superfamily.1 LDN-193189 inhibits SMAD1/5/8 phosphorylation by the bone morphogenetic protein (BMP) type I receptors, which are known as activin receptor-like kinases (ALKs), with an IC50 value of 4.9 nM.2 In in vitro kinase assays, it shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively).3 LDN-193189 has been used to inhibit BMP type I receptor activity to study the pathogenesis of fibrodysplasia ossificans progressive, a congenital hyperossification disorder, and to examine the role of osteogenesis in prostate tumor metastases in bone.
LDN193189 (1062368-24-4) Specifications:
|Synonyms||LDN 193189; LDN-193189|
|Molecular Weight||406.493 g/mol|
|Monoisotopic Mass||406.191 g/mol|
|Color||yellow to orange|
|Solubility||Soluble in DMSO|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|