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| LDN-193189 Basic information |
| Product Name: | LDN-193189 | | Synonyms: | LDN193189
LDN193189 HCl;4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline;LDN-193189;LDN 193189;DM-3189;DM 3189;LDN-193189;LDN 193189;CS-205;LDN193189 free base;LDN193189(DM3189);LDN193189 | | CAS: | 1062368-24-4 | | MF: | C25H22N6 | | MW: | 406.48 | | EINECS: | | Product Categories: | Smad;TGF-beta;TGF-beta/Smad;Inhibitors | | Mol File: | 1062368-24-4.mol |
| LDN-193189 Chemical Properties |
| density | 1.33 | | storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | | solubility | H2O: soluble5mg/mL, clear (warmed) | | form | powder | | pka | 8.79±0.10(Predicted) | | color | yellow to orange | | InChIKey | XHBVYDAKJHETMP-UHFFFAOYSA-N |
| WGK Germany | 3 | | HS Code | 29339900 |
| LDN-193189 Usage And Synthesis |
| Description | 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 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 | 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. | | references | [1] yu pb, deng dy, lai cs, hong cc, cuny gd, bouxsein ml, hong dw, mcmanus pm, katagiri t, sachidanandan c, kamiya n, fukuda t, mishina y, peterson rt, bloch kd. bmp type i receptor inhibition reduces heterotopic [corrected] ossification. nat med. 2008 dec;14(12):1363-9.[2] boergermann jh1, kopf j, yu pb, knaus p. dorsomorphin and ldn-193189 inhibit bmp-mediated smad, p38 and akt signalling in c2c12 cells. int j biochem cell biol. 2010 nov;42(11):1802-7. [3] helbing t1, herold em, hornstein a, wintrich s, heinke j, grundmann s, patterson c, bode c, moser m. inhibition of bmp activity protects epithelial barrier function in lung injury. j pathol. 2013 sep;231(1):105-16. doi: 10.1002/path.4215. epub 2013 jul 10. |
| LDN-193189 Preparation Products And Raw materials |
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