Home TGF-beta/Smad TGF-beta/Smad inhibitor LDN-193189 For research use only.

LDN-193189

Synonyms: DM3189

LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!

LDN-193189 Chemical Structure

LDN-193189 Chemical Structure

CAS: 1062368-24-4

Selleck's LDN-193189 has been cited by 224 publications

Purity & Quality Control

Batch: Purity: 99.43%
99.43

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C2C12 Kinase Assay inhibits the kinase activity of ALK4 and ActRIIA with IC50 values of 101 and 210 nm, respectively 25368322
EOC216 Growth Inhibition Assay 0.1-10 μM 2-10 d DMSO induce cell death in a dose-dependent manner 25227893
OVAC429 Growth Inhibition Assay 2/5 μM 48 h DMSO decreases the percentage of cells in S phas 25227893
SKOV3 Growth Inhibition Assay 2/5 μM 48 h DMSO decreases the percentage of cells in S phas 25227893
OVCA429 Growth Inhibition Assay 2/5 μM 48 h DMSO decreases the percentage of cells in S phas 25227893
EOC219 Growth Inhibition Assay 2/5 μM 48 h DMSO decreases the percentage of cells in S phas 25227893
A549 Growth Inhibition Assay 0.5-16 μM DMSO inhibits cell growth in a dose-dependent manner 24778011
BEAS-2B  Growth Inhibition Assay 0.5-16 μM DMSO inhibits cell growth in a dose-dependent manner 24778011
hBMSCs Function Assay 0.2 μM 7 d abolishes the silibinin-promoted ALP activity partly 24076187
PANC-1 Growth Inhibition Assay 5-500 nM 48 h inhibits cell growth in a dose-dependent manner 23969729
MIA PaCa-2 Growth Inhibition Assay 5-500 nM 48 h inhibits cell growth in a dose-dependent manner 23969729
Bx-PC3 Growth Inhibition Assay 5-500 nM 48 h inhibits cell growth in a dose-dependent manner 23969729
PC3  Function Assay 500 nM 2 h represses activation of Smad1/5/8 and P-Smad3 levels 22452883
LNCaP Function Assay 0–500 nM 2 h reverses rapamycin-induced cell death 22452883
EOC Function Assay 10-1000 nM 72 h reduces the phosphorylated BMP R-Smad1/5/8  22249415
HaCaT  Function Assay 0.001-10 μM 2 h inhibits BMP2-induced phosphorylation of Smad1/5/8 with an IC50 of ~0.005 μM 21740966
HaCaT  Function Assay 0.001-10 μM 2 h inhibits the ability of ALK2 to phosphorylate GST-Smad1 with an IC50 of 45 nM 21740966
HaCaT  Function Assay 0.001-10 μM 2 h inhibits the ability of ALK3 to phosphorylate Smad1 with an IC50 of 100 nM 21740966
HaCaT  Function Assay 0.001-10 μM 2 h inhibits ALK4 and ALK5 with IC50 values of 0.3 μM and 0.5 μM respectively 21740966
C2C12 Function assay 30 mins Inhibition of BMP6-induced ALK2 transcriptional activity in mouse C2C12 cells expressing BRE-Luc after 30 mins by luciferase reporter gene assay, EC50 = 0.014 μM. 30227946
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
fibroblast cell qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
KB-3-1 Function assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
C2C12 Function assay 0.1 uM Inhibition of ALK5 in mouse C2C12 cells assessed as decrease in TGFbeta1-induced Smad1/5 phosphorylation at 0.1 uM by Western blot method 28103025
Click to View More Cell Line Experimental Data

Biological Activity

Description LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
Targets
ALK1 [5]
(Cell-free assay)		 ALK2 [5]
(Cell-free assay)		 ALK3 [5]
(Cell-free assay)		 ALK6 [5]
(Cell-free assay)
0.8 nM 0.8 nM 5.3 nM 16.7 nM
In vitro
In vitro

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. [1]

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. [4]
Kinase Assay Alkaline phosphatase activity
C2C12 cells are seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. The wells are treated in quadruplicate with BMP ligands and LDN-193189 or vehicle. The cells are collected after 6 days in culture in 50 μL Tris-buffered saline and 1% Triton X-100. The lysates are added to p-nitro-phenylphosphate reagent in 96-well plates for 1 hours and then evaluated alkaline phosphatase activity (absorbance at 405 nm). Cell viability and quantity are measured by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements.
Cell Research Cell lines PASMCs 
Concentrations 5 nM
Incubation Time 12 h
Method

Cells were treated with various concnetrations of LDN-193189.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pSMAD1 / pSMAD5 / pSMAD8 / SMAD1 / SMAD5 / SMAD8 / ID1 / SMAD4 / PARP / Cleaved PARP 31098401
Immunofluorescence Tbx18 / Hcn4 30906456
Growth inhibition assay Cell viability 31098401
In Vivo
In vivo

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. [1]

LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. [2]

In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. [3]

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. [4]
Animal Research Animal Models Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
Dosages ≤3 mg/kg
Administration Administered via i.p.

Chemical lnformation & Solubility

Molecular Weight 406.48 Formula

C25H22N6
CAS No. 1062368-24-4 SDF Download LDN-193189 SDF
Smiles C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3
Storage (From the date of receipt)

In vitro
Batch:

0.01M HCl : 2.5 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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