LDN-193189 HCl chemical structure
Chemical structureResearch use only
CAT. NO. DC7451Featured

LDN-193189 HCl

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Product overview

Description & Application

LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities. LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone Formation in the tumors. In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. For the detailed information of LDN193189 HCl, the solubility of LDN193189 HCl in water, the solubility of LDN193189 HCl in DMSO, the solubility of LDN193189 HCl in PBS buffer, the animal experiment (test) of LDN193189 HCl, the cell expriment (test) of LDN193189 HCl, the in vivo, in vitro and clinical trial test of LDN193189 HCl, the EC50, IC50,and Affinity of LDN193189 HCl, Please contact DC Chemicals.

ParameterValue
Chemical Name4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline dihydrochloride
CAS No.1435934-00-1
SynonymsLDN-193189 monohydrochloride; LDN-193189 HCl; LDN193189; LDN-193189; LDN 193189; LDN193189; DM-3189; DM 3189; DM3189;
FormulaC25H24Cl2N6
M.Wt479.409
SMILES[H]Cl.[H]Cl.C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities. LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone Formation in the tumors. In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. For the detailed information of LDN193189 HCl, the solubility of LDN193189 HCl in water, the solubility of LDN193189 HCl in DMSO, the solubility of LDN193189 HCl in PBS buffer, the animal experiment (test) of LDN193189 HCl, the cell expriment (test) of LDN193189 HCl, the in vivo, in vitro and clinical trial test of LDN193189 HCl, the EC50, IC50,and Affinity of LDN193189 HCl, Please contact DC Chemicals.

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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