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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.1 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).2 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.3,4 This product is also available as part of Cayman's Hepatocyte Maintenance Reagent Kit (Item No. 44676).
WARNING This product is not for human or veterinary use.
1. Structure-
2. A new class of small molecule inhibitor of BMP signaling. PLoS One 8(4), 62721 (2013).
3. BMP type I receptor inhibition reduces heterotopic ossification. Nat. Med. 14(12), 1363-1369 (2008).
4. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res. 71(15), 5194-5203 (2011).