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LDN-193189 2HCl

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Catalog No. T35348Cas No. 1435934-00-1
Alias LDN-193189 2HCl, DM-3189 2HCl

LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.

LDN-193189 2HCl

LDN-193189 2HCl

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Purity: 99.87%
Catalog No. T35348Alias LDN-193189 2HCl, DM-3189 2HClCas No. 1435934-00-1
LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$67In StockIn Stock
10 mg$87In StockIn Stock
25 mg$148In StockIn Stock
50 mg$237In StockIn Stock
100 mg$353In StockIn Stock
500 mg$837In StockIn Stock
1 mL x 10 mM (in DMSO)$72In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.87%
Appearance:Solid
Color:Orange
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Product Introduction

Bioactivity
Description
LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.
Targets&IC50
ALK1 (cell-free assay):0.8 nM, ALK2 (cell-free assay):0.8 nM, ALK3 (cell-free assay):5.3 nM, ALK6 (cell-free assay):16.7 nM
In vitro
LDN193189 can effectively inhibit BMP4-mediated activation of Smad1, Smad5, and Smad8, with IC50 of 5 nM. It can also effectively inhibit the transcriptional activity of BMP type I receptors ALK2 and ALK3, with IC50 of 5 nM and 30 nM, respectively. LDN193189 also has an inhibitory effect on transcriptional activation induced by persistently activated ALK2R206H or ALK2Q207D mutant proteins.[1]
A recent study showed that LDN-193189 blocks the production of oxidative free radicals induced by oxidized LDL in human arterial endothelial cells.[4]
In vivo
LDN-193189 (3 mg/kg, intraperitoneal injection; birth in conditional caALK2) caused weak calcification of the left tibia and fibula, which was visible on day 13 and blocked on day 15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density, or abnormal behavior.[1]
LDN193189 forms curved Zebrafish embryos by inhibiting the signal pathway induced by bone morphogenetic protein (BMP) 6 and has no effect on vascular development.[2]
In mice with PCa-118b tumors, LDN-193189 treatment slowed down tumor growth and reduced bone formation in the tumor.[3]
In LDLR -/- mice, LDN-193189 inhibited the development of arterial atherosclerosis. In addition, LDN-193189 has inhibitory effects on vascular inflammation, osteogenic activity, and calcification.[4]
SynonymsLDN-193189 2HCl, DM-3189 2HCl
Chemical Properties
Molecular Weight479.4
FormulaC25H24Cl2N6
Cas No.1435934-00-1
SmilesC1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=C6C=CC=CC6=NC=C1.Cl.Cl
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 8.77 mg/mL (18.29 mM), Sonication is recommended.
H2O: 45 mg/mL (93.87 mM), Sonication is recommended.
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM2.0859 mL10.4297 mL20.8594 mL104.2970 mL
5 mM0.4172 mL2.0859 mL4.1719 mL20.8594 mL
10 mM0.2086 mL1.0430 mL2.0859 mL10.4297 mL
H2O
1mg5mg10mg50mg
20 mM0.1043 mL0.5215 mL1.0430 mL5.2149 mL
50 mM0.0417 mL0.2086 mL0.4172 mL2.0859 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
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