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LDN-193189 2HCl

LDN-193189 2HCl
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Purity:99.78%
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LDN-193189 2HCl

Catalog No. T35348Cas 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.
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Pack SizePriceAvailabilityQuantity
5 mg$67In Stock
10 mg$87In Stock
25 mg$148In Stock
50 mg$237In Stock
100 mg$353In Stock
500 mg$837In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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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.
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]
AliasLDN-193189 2HCl, DM-3189 2HCl
Chemical Properties
Molecular Weight479.4
FormulaC25H24Cl2N6
Cas No.1435934-00-1
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 4.79 mg/mL (10 mM)
H2O: 45.0 mg/mL (93.9 mM)
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.0859 mL10.4297 mL20.8594 mL104.2970 mL
5 mM0.4172 mL2.0859 mL4.1719 mL20.8594 mL
H2O
1mg5mg10mg50mg
10 mM0.2086 mL1.0430 mL2.0859 mL10.4297 mL
20 mM0.1043 mL0.5215 mL1.0430 mL5.2149 mL
50 mM0.0417 mL0.2086 mL0.4172 mL2.0859 mL
100 mM0.0209 mL0.1043 mL0.2086 mL1.0430 mL

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