LDN-193189 化学特性,用途語,生産方法
説明
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. 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 IC
50 value of 4.9 nM. In
in vitro kinase assays, it shows specificity for ALK1, 2, 3, and 6 (IC
50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC
50s = 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.
使用
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline, is a selective inhibitor of bone morphogenetic protein (BMP) pathway, useful in the treatment of diseases. Potent BMP Inhibitor?, Promotes hPSC Neural Induction?.
Biochem/physiol Actions
Although LDN193189 is a structural analog of dorsomorphin, these two drugs are found to establish different cellular responses. In vitro analysis reveals that LDN193189 inhibits a number of intracellular kinases such as, mitogen activated protein kinase 14 and 8 ( p38and c-Jun N-terminal kinase respectively), as well as those associated with AKT (serine/threonine kinase) and mTOR (mammalian target of rapamycin) signaling mechanisms. LDN193189 is known to elevate the levels hemoglobin and thus helps to prevent the onset of anemia of inflammation.
LDN-193189 上流と下流の製品情報
原材料
準備製品