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> LDN193189 [1062368-24-4]

LDN193189 [1062368-24-4]

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Formaat : 5mg

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LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.

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LDN193189 Chemical Structure

LDN193189 Chemical Structure

CAS No. : 1062368-24-4

This product is a controlled substance and not for sale in your territory.

Based on 60 publication(s) in Google Scholar

Other Forms of LDN193189:

  • LDN193189 Tetrahydrochloride In-stock
  • LDN-193189 dihydrochloride Obtenir un devis
  • LDN193189 hydrochloride Obtenir un devis
  • LDN193189 (GMP) Obtenir un devis

    LDN193189 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2020 Jun 8;2020:4175613.  [Abstract]

    Western blot and grey analysis of CYP11a1, CYP19a1, BCL2, CALR, CHOP, caspase3, caspase12, PERK, and GRP78. qRT-PCR analyzed ATF4, caspase3, and GRP78 mRNAs. The relieving function of BMP4 on ER stress is diminished after blockade of BMP receptor I (BMPRI) with DM-3189.

    LDN193189 purchased from MedChemExpress. Usage Cited in: Cardiovasc Toxicol. 2019 Jun;19(3):264-275.  [Abstract]

    H9c2 cells are treated as following: control, DOX, DOX + rhBMP (Bmpr1a agonist) and DOX + LDN193189 (Bmpr1a inhibitor). Cells with red fluorescence indicate favorable MMP while green fluorescence indicates damage.

    Voir tous les produits spécifiques à Isoform TGF-β Receptor:

    Voir toutes les isoformes
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B
    Description

    LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva[1][2][3].

    IC50 & Target[1]

    ACVR1

    5 nM (IC50)

    BMPR1A

    30 nM (IC50)

    In Vitro

    LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively[1].
    LDN-193189 has weake effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 with IC50 values of ≥ 500 nM[1].
    LDN-193189 binds ActRIIA with Kd value of 14 nM[2].
    LDN-193189 (0.5 μM; 30 min) targets GDF8 induced Smad2/3 signaling and repression of myogenic transcription factors[2].
    LDN-193189 (0.05, 0.5, 5 μM) efficiently inhibits GDF8 induced Smad3/4 reporter gene activity[2].
    LDN-193189 (0-5 μM) rescues myogenesis in myoblasts treated with GDF8[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    LDN193189 Related Antibodies

    Western Blot Analysis[2]

    Cell Line: Primary human myoblasts, C2C12 cells
    Concentration: 0.5 μM
    Incubation Time: 30 min
    Result: Inhibited GDF8-induced signaling pathways in undifferentiated and in differentiated primary human myoblasts and in C2C12 premyoblasts.
    In Vivo

    LDN-193189 (i.p.; 3 mg/kg; daily; for 35 days) might affect the interaction between breast cancer cells and the bone environment[3].
    LDN-193189 (i.p.; 3 mg/kg; single) shows a reduction in ectopic ossification and functional impairment[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Ahymic NMRI nude female mice (6-week-old)[3]
    Dosage: 3 mg/kg
    Administration: Itraperitoneal, daily, for 35 days
    Result: Ehanced etastases development in vivo.
    Animal Model: C57BL/6 mice[1]
    Dosage: 3 mg/kg
    Administration: Intraperitoneal, single
    Result: Diminished ectopic bone formation and preserved joint spaces over the same interval without inducing fractures, osteopenia or skeletal abnormalities.
    Masse moléculaire

    406.49

    Formule

    C25H22N6
    CAS No.

    1062368-24-4
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : 10 mg/mL (24.60 mM; ultrasonic and warming and adjust pH to 2 with 1M HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4601 mL 12.3004 mL 24.6009 mL
    5 mM 0.4920 mL 2.4601 mL 4.9202 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Calculateur de molarité

    • Calculateur de dilution

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1 mg/mL (2.46 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 1 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1 mg/mL (2.46 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 1 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Pureté et documentation

    Purity: 99.48%

    SDS (393 KB)

    COA (254 KB) LCMS (161 KB)

    Instruction de manipulation (2659 KB)
    Références

    • [1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.  [Content Brief]

      [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.  [Content Brief]

      [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.  [Content Brief]

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4601 mL 12.3004 mL 24.6009 mL 61.5021 mL
    5 mM 0.4920 mL 2.4601 mL 4.9202 mL 12.3004 mL
    10 mM 0.2460 mL 1.2300 mL 2.4601 mL 6.1502 mL
    15 mM 0.1640 mL 0.8200 mL 1.6401 mL 4.1001 mL
    20 mM 0.1230 mL 0.6150 mL 1.2300 mL 3.0751 mL
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    LDN193189 Related Classifications

    Help & FAQs

    Keywords:

    LDN1931891062368-24-4DM-3189LDN 193189LDN-193189DM3189DM 3189OrganoidTGF-β ReceptorTransforming growth factor beta receptorsbone morphogenetic protein (BMP)BMP I receptortranscriptionALK2ALK3bone morphogenetic protein signallingfibrodysplasia ossificans progressivaInhibitorinhibitorinhibit

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