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Chemical Structure| 1062368-24-4 Chemical Structure| 1062368-24-4

Structure of LDN193189
CAS No.: 1062368-24-4

Chemical Structure| 1062368-24-4

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LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor, efficiently inhibiting the transcriptional activity of BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. It is used for researching bone morphogenetic protein signaling, such as fibrodysplasia ossificans progressiva.

Synonyms: DM-3189

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Product Details of LDN193189

CAS No. :1062368-24-4
Formula : C25H22N6
M.W : 406.48
SMILES Code : C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16
Synonyms :
DM-3189
MDL No. :MFCD17392570
InChI Key :CDOVNWNANFFLFJ-UHFFFAOYSA-N
Pubchem ID :25195294

Safety of LDN193189

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • ALK1

    ALK1, IC50:0.8 nM

  • ALK2

    ALK2, IC50:0.8 nM

  • ALK6

    ALK6, IC50:16.7 nM

  • ALK3

    ALK3, IC50:5.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MC3T3-E1 cells 0.5 μM 3 days LDN193189 inhibited BMP9-induced activation of the Smad1/5/9 signaling pathway, leading to increased expression of Stat1 and P21, and partially neutralizing the inhibitory effect of BMP9 on SASPs. PMC9076651
bone marrow–derived macrophages (BMDM) 100 nM 24 h To investigate the effect of BMP signaling inhibition on macrophage activation, results showed that BMP inhibitor combined with β-glucan and LPS increased proinflammatory IL-6 gene expression. PMC10906463
human embryonic stem cell-derived dopaminergic neurons 100 nM 11 days Used for the differentiation of dopaminergic neurons, promoting neuron generation PMC11148862
human-induced pluripotent stem cell–derived microglia-like cells (hiPSC-MG) 0.1 μM Used to generate spinal motor neurons as part of the experimental model. PMC10121169
human pluripotent stem cells (PS cells) 200 nM 2 days Enhanced differentiation of PS cells into somite-like stage, promoting PAX7-induced myogenesis PMC6845233
IMECs 1 μM 48 h Inhibits cancer stem cell phenotype, reduces ALDH1+ cell population PMC3739305
HC11 cells 1 μM 48 h Inhibits cancer stem cell phenotype, reduces ALDH1+ cell population PMC3739305
MMTV-Myc primary tumor cells 1 μM 48 h Inhibits cancer stem cell phenotype, reduces ALDH1+ cell population PMC3739305

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice aged mice model intraperitoneal injection 3 mg/kg once every other day for 12 weeks LDN193189 reversed the inhibitory effect of BMP9 on Stat1 and downstream senescent genes, and eliminated the improvement of BMP9 on bone mass and trabecular microarchitecture in aged mice. PMC9076651
mice breast cancer bone metastasis model osmotic pump 3 mg/kg continuous for 7 or 28 days To investigate the effect of BMP signaling inhibition on breast cancer bone metastasis models, results showed that early BMP inhibition increased bone metastasis growth but reduced lung metastasis. PMC10906463
Mice Ext1 -cKO mouse model Intraperitoneal injection 10 mg/kg Every other day for 3 weeks LDN-193189 significantly reduced the number of hypertrophic chondrocytes and cartilage thickness in Ext1 -cKO mice, and downregulated pSmad1/5/9 expression. PMC7606622
BALB/c nude mice xenograft nude mouse model subcutaneously injected 4 mg/kg, 5 mg/kg 3 weeks (5 days on, 2 days off) LDN-193189 effectively suppressed tumor growth in nude mice bearing gef-resistant NSCLC cells in vivo. PMC6118096
Mice MMTV-Myc transgenic mouse model Intraperitoneal injection 2.5 mg/kg Once daily for 16 days Reduces tumor initiating ability, increases tumor latency PMC3739305

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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