LDN193189(DM3189)
LDN-193189
CAS: 1062368-24-4
Molecular Formula: C25H22N6
LDN193189(DM3189) - Names and Identifiers
| Name | LDN-193189 |
| Synonyms | CS-205 DM 3189 DM-3189 LDN193189 LDN-193189 LDN 193189 LDN193189(DM3189) LDN193189 free base LDN193189 LDN193189 HCl 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline |
| CAS | 1062368-24-4 |
| InChIKey | XHBVYDAKJHETMP-UHFFFAOYSA-N |
LDN193189(DM3189) - Physico-chemical Properties
| Molecular Formula | C25H22N6 |
| Molar Mass | 406.48 |
| Density | 1.33 |
| Solubility | H2O: soluble5mg/mL, clear (warmed) |
| Appearance | powder |
| Color | yellow to orange |
| pKa | 8.79±0.10(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Use | LDN-193189 is a selective inhibitor of BMP signaling pathway, which inhibits the transcriptional activity of BMP type I receptors ALK2 and ALK3. IC50 is 5 nM and 30 nM respectively. The selectivity of BMP is 200 times higher than that of TGF-β. |
| In vitro study | LDN193189 effectively inhibits BMP4-mediated activation of Smad1,Smad5 and Smad8 with IC 50 of 5 nM, and effectively inhibits the transcriptional activity of type I receptors ALK2 and ALK3 of BMP, the IC 50 is 5 nM and 30 nM, respectively. In addition, LDN193189 also inhibited the transcriptional activity induced by the constitutively active ALK2R206H or ALK2Q207D muteins. A recent study showed that LDN-193189 blocked the production of reactive oxygen species induced by oxidized low-density lipoprotein in atherogenic human aortic endothelial cells. LDN193189 effectively inhibits BMP4-mediated activation of Smad1,Smad5 and Smad8 with IC 50 of 5 nM, and effectively inhibits the transcriptional activity of type I receptors ALK2 and ALK3 of BMP, the IC 50 is 5 nM and 30 nM, respectively. In addition, LDN193189 also inhibited constitutively active ALK2. A recent study showed that LDN-193189 blocked oxidized low-density lipoprotein-induced reactive oxygen species production in atherogenic human aortic endothelial cells. |
| In vivo study | In the use of Ad.Cre conditional caALK2 transgenic mice, with 7 days of age (P7),LDN-193189(3 mg/kg, I. P.) resulted in mild calcification of adjacent left tibia and fibula at P13, and to prevent the occurrence of radiation lesions in P15 without causing weight loss or growth retardation, spontaneous fracture, decreased bone density or abnormal behavior. LDN193189 has no effect on vascular development by inhibiting the signal transduction pathway induced by bone morphogenetic protein (BMP)6 in zebrafish embryos. In mice with PCa-118b tumors, LDN-193189 attenuated tumor growth and decreased bone formation in the tumors. In low-density lipoprotein receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibited the development of atherosclerosis. In addition, LDN-193189 also showed an associated Vasculitis inhibition of Osteogenic Activity and calcification. in the use of Ad.Cre conditional caALK2 transgenic mice, with 7 days of age (P7),LDN-193189(3 mg/kg, I. P.) resulted in mild calcification of adjacent left tibia and fibula at P13, and to prevent the occurrence of radiation lesions in P15 without causing weight loss or growth retardation, spontaneous fracture, decreased bone density or abnormal behavior. LDN193189 has no effect on vascular development by inhibiting the signal transduction pathway induced by bone morphogenetic protein (BMP)6 in zebrafish embryos. In mice with PCa-118b tumors, LDN-193189 attenuated tumor growth and decreased bone formation in the tumors. In low-density lipoprotein receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibited the development of atherosclerosis. In addition, LDN-193189 also showed an associated Vasculitis inhibition of Osteogenic Activity and calcification. |
LDN193189(DM3189) - Risk and Safety
| WGK Germany | 3 |
| HS Code | 29339900 |
LDN193189(DM3189) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.086 ml | 10.43 ml | 20.859 ml |
| 5 mM | 0.417 ml | 2.086 ml | 4.172 ml |
| 10 mM | 0.209 ml | 1.043 ml | 2.086 ml |
| 5 mM | 0.042 ml | 0.209 ml | 0.417 ml |
Last Update：2024-01-02 23:10:35
LDN193189(DM3189) - Reference Information
| biological activity | LDN-193189 is a selective inhibitor of BMP signaling pathway, inhibition of the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, was 200 times more selective for BMP than for TGF-β. LDN-193189 (DM3189) is a selective BMP signaling pathway inhibitor, which inhibits the transcriptional activity of ALK2 and ALK3, in C2C12 cells, IC50 was 5 nM and 30 nM, respectively, and the selectivity of BMP was 200 times higher than that of TGF-β. |
| in vitro study | LDN193189 effectively inhibits BMP4-mediated activation of Smad1,Smad5 and Smad8 with IC 50 of 5 nM, and effectively inhibit the transcriptional activity of type I receptors ALK2 and ALK3 of BMP, IC 50 is 5 nM and 30 nM respectively. In addition, LDN193189 also inhibited the transcriptional activity induced by the constitutively active ALK2R206H or ALK2Q207D muteins. A recent study showed that LDN-193189 blocked the production of reactive oxygen species induced by oxidized low-density lipoprotein in atherogenic human aortic endothelial cells. LDN193189 effectively inhibits BMP4-mediated activation of Smad1,Smad5 and Smad8 with IC 50 of 5 nM, and effectively inhibits the transcriptional activity of type I receptors ALK2 and ALK3 of BMP, the IC 50 is 5 nM and 30 nM, respectively. In addition, LDN193189 also inhibited constitutively active ALK2. A recent study showed that LDN-193189 blocked oxidized low-density lipoprotein-induced reactive oxygen species production in atherogenic human aortic endothelial cells. |
| in vivo studies | in the use of Ad.Cre conditional caALK2 transgenic mice, with 7 days of age (P7),LDN-193189(3 mg/kg, I. P.) resulted in mild calcification of adjacent left tibia and fibula at P13, and to prevent the occurrence of radiation lesions in P15 without causing weight loss or growth retardation, spontaneous fracture, decreased bone density or abnormal behavior. LDN193189 has no effect on vascular development by inhibiting the signal transduction pathway induced by bone morphogenetic protein (BMP)6 in zebrafish embryos. In mice with PCa-118b tumors, LDN-193189 attenuated tumor growth and decreased bone formation in the tumors. In low-density lipoprotein receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibited the development of atherosclerosis. In addition, LDN-193189 also showed an associated Vasculitis inhibition of Osteogenic Activity and calcification. in the use of Ad.Cre conditional caALK2 transgenic mice, with 7 days of age (P7),LDN-193189(3 mg/kg, I. P.) resulted in mild calcification of adjacent left tibia and fibula at P13, and to prevent the occurrence of radiation lesions in P15 without causing weight loss or growth retardation, spontaneous fracture, decreased bone density or abnormal behavior. LDN193189 has no effect on vascular development by inhibiting the signal transduction pathway induced by bone morphogenetic protein (BMP)6 in zebrafish embryos. In mice with PCa-118b tumors, LDN-193189 attenuated tumor growth and decreased bone formation in the tumors. In low-density lipoprotein receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibited the development of atherosclerosis. In addition, LDN-193189 also showed an associated Vasculitis inhibition of Osteogenic Activity and calcification. |
| Target | TargetValue ALK2 (C2C12 cells) 5 nM ALK3 (C2C12 cells) 30 nM |
| Target | Value |
| ALK2 (C2C12 cells) | 5 nM |
| ALK3 (C2C12 cells) | 30 nM |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: LDN-193189 Visit Supplier Webpage Request for quotationCAS: 1062368-24-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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