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Purity: ≥98%
LDN193189 2HCl is the dihydrochloride salt of LDN193189, which is a highly potent and selective small molecule inhibitor of the BMP (bone morphogenetic protein ) signaling pathway. It inhibits the transcriptional activity of the BMP type I receptor kinases such as ALK2 (activin receptor-like kinase-2) and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, it exhibits 200-fold selectivity for BMP versus TGF-β. LDN193189 has been showed to inhibit BMP induced phosphorylation of Smad signaling (Smad1/5/8) and non-Smad signaling including p38 and Akt in C2C12 cells. LDN-193189 inhibits activation of the BMP signaling effectors SMAD1, SMAD5 and SMAD8 in tissues expressing caALK2 induced by adenovirus specifying Cre (Ad.Cre).
| ln Vitro |
With IC50 values of 5 nM and 30 nM, respectively, LDN-193189 effectively suppresses the transcriptional activity of the BMP type I receptors ALK2 and ALK3[1]. With IC50 values of less than 500 nM, LDN-193189 exhibits negligible effects on activin and TGF-β type I receptors ALK4, ALK5, and ALK7[1]. ActRIIA is bound by LDN-193189 at a Kd value of 14 nM[2]. LDN-193189 (0.5 μM; 30 min) targeting the suppression of myogenic transcription factors and Smad2/3 signaling triggered by GDF8[2]. Effectively inhibiting GDF8-induced Smad3/4 reporter gene activity is LDN-193189 (0.05, 0.5, and 5 μM)[2]. GDF8-treated myoblasts see their myogenesis restored by LDN-193189 (0–5 μM)[2].
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| ln Vivo |
LDN-193189 (ip; 3 mg/kg; daily; 35 days) may have an impact on how breast cancer cells interact with their surroundings in the bone[3]. LDN-193189 (ip; 3 mg/kg; single) reduces functional impairment and ectopic ossification [1].
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| References |
[1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.
[2]. Daniel Horbelt, et al. Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation. J Biol Chem. 2015 Feb 6;290(6):3390-404. [3]. Julien Vollaire, et al. The Bone Morphogenetic Protein Signaling Inhibitor LDN-193189 Enhances Metastasis Development in Mice. Front Pharmacol. 2019 Jun 19;10:667. |
| Molecular Formula |
C25H24CL2N6
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| Molecular Weight |
479.4
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| CAS # |
1435934-00-1
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| Related CAS # |
LDN193189;1062368-24-4;LDN193189 Tetrahydrochloride;2310134-98-4
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| SMILES |
C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16.Cl.Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0859 mL | 10.4297 mL | 20.8594 mL | |
| 5 mM | 0.4172 mL | 2.0859 mL | 4.1719 mL | |
| 10 mM | 0.2086 mL | 1.0430 mL | 2.0859 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibitor binding to ActRII.J Biol Chem.2015 Feb 6;290(6):3390-404.
Dorsomorphin and LDN-193189 inhibit GDF8-induced signaling pathways in undifferentiated and in differentiated primary human myoblasts and in C2C12 premyoblasts.J Biol Chem.2015 Feb 6;290(6):3390-404. |
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Ligand-specific effects of kinase inhibitors on Smad2/3 and Smad1/5 phosphorylation.
Dorsomorphin treatment facilitates myotube formation.J Biol Chem.2015 Feb 6;290(6):3390-404. |
Dorsomorphin and LDN-193189 efficiently inhibit GDF8 induced Smad3/4 reporter gene activity.J Biol Chem.2015 Feb 6;290(6):3390-404. |
Dorsomorphin and LDN-193189 counteract GDF8-induced repression of myogenic differentiation.J Biol Chem.2015 Feb 6;290(6):3390-404. |
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Dorsomorphin and LDN-193189 promote the formation of a contractile myotube network.J Biol Chem.2015 Feb 6;290(6):3390-404. |
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