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Biological Activity:
A highly potent small molecule BMP inhibitor; inhibiting BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation; useful tool in stem cell biology.
LDN-193189 shows significant in vivo clinical utility, inhibiting FOP and ectopic ossification and a potential agent in the treatment of NSCLC lung tumors.
References:
EM Langenfeld and J Langenfeld. Bone Morphogenetic Protein-2 Stimulates Angiogenesis in Developing Tumors. Mol. Cancer Res. 2004, 2, 141–149. [online]
PB Yu et al. BMP type I receptor inhibition reduces heterotopic ossification. Nat. Med. 2008, 14, 1363-1369. [online]
GD Cuny et al. Structure–activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorg. Med. Chem. Lett. 2008, 18, 4388–4392. [online]
PB Yu et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat. Chem. Biol. 2008, 4, 33-41. [online]
Chemical Name: 4-[6-(4-Piperazin-1-yl-phenyl)-pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline hydrochloride
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