Description

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.

Uses

LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva[1][2][3].

in vivo

storage

-20°C

References

[1] BMP type 1 receptor inhibition reduces heterotropic ossification
[2] STUART M CHAMBERS. Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors[J]. Nature biotechnology, 2012, 30 7: 715-720. DOI:10.1038/nbt.2249
[3] FAITH R KREITZER. A robust method to derive functional neural crest cells from human pluripotent stem cells.[J]. American journal of stem cells, 2013, 2 2: 119-131.
[4] YU-CHEN LEE. BMP4 promotes prostate tumor growth in bone through osteogenesis.[J]. Cancer research, 2011: 5194-5203. DOI:10.1158/0008-5472.can-10-4374