1435934-00-1

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. 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). 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.

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1) Yu?et al.?(2008),?BMP type 1 receptor inhibition reduces heterotropic ossification; Nature Med.,14?1363 2) Chambers?et al.?(2012),?Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors; Nature Biotechnol.?30?715 3) Kreitzer?et al. (2013)?A robust method to derive functional neural crest cells from human pluripotent stem cells; Am. J. Stem Cells,?2?119 4) Lee?et al.?(2011)?BMP4 promotes prostate tumor growth in bone through osteogenesis; Cancer Res.?71?5194