1. TGF-beta/Smad
  2. TGF-β Receptor
  3. LDN193189

LDN193189  (Synonyms: DM-3189)

Cat. No.: HY-12071 Purity: 99.42%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

LDN193189 Chemical Structure

LDN193189 Chemical Structure

CAS No. : 1062368-24-4

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Customer Review

Based on 44 publication(s) in Google Scholar

Other Forms of LDN193189:

Top Publications Citing Use of Products

42 Publications Citing Use of MCE LDN193189

IHC
WB

    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.

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    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.

    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.
    Molecular Weight

    406.48

    Appearance

    Solid

    Formula

    C25H22N6

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 12 mg/mL (29.52 mM; ultrasonic and adjust pH to 2 with HCl)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4601 mL 12.3007 mL 24.6015 mL
    5 mM 0.4920 mL 2.4601 mL 4.9203 mL
    10 mM 0.2460 mL 1.2301 mL 2.4601 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 1.2 mg/mL (2.95 mM); Clear solution

    • 2.

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

      Solubility: ≥ 1.2 mg/mL (2.95 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.48%

    References
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    LDN193189 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    LDN193189
    Cat. No.:
    HY-12071
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