货号 | 11802-1mg |
描述 | 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.2Inin 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.4,5 |
供应商 | Cayman |
应用文献 | |
1.Brivanlou, A.H., and Darnell, J.E., Jr. Signal transduction and the control of gene expression. Science 295, 813-818 (2002). 2.Cuny, G.D.,Yu, P.B.,Laha, J.K., et al. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorganic & Medicinal Chemistry Letters 18(15), 4388-4392 (2008). 3.Sanvitale, C.E.,Kerr, G.,Chaikuad, A., et al. A new class of small molecule inhibitor of BMP signaling. PLoS One 8(4), 62721 (2013). 4.Yu, P.B.,Deng, D.Y.,Lai, C.S., et al. BMP type I receptor inhibition reduces heterotopic ossification. Nature Medicine 14(12), 1363-1369 (2008). 5.Lee, Y.C.,Cheng, C.J.,Bilen, M.A., et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Research 71(15), 5194-5203 (2011). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 406.5 |
分子式 | C25H22N6 |
CAS号 | 1062368-24-4 |
稳定性 | ≥ 2 years |
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