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LDN-193189, BMP inhibitor

LDN-193189, BMP inhibitor

$79.00
A highly potent and selective BMP pathway inhibitor (selective for ALK2 and ALK3); can replace Noggin protein in cellular and in vivo use.
Catalog No. Unit Price Qty
M60008-2s 2mg solid $79.00
M60008-2 10 mM in DMSO (0.493 mL) $79.00
M60008-25s 25mg solid $550.00

Details

Product Information
Molecular Weight: 406.48
Formula: C25H22N6
Purity: ≥98%
CAS#: 1062368-24-4
Solubility: DMSO up to 100 mM
Chemical Name: 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

LDN193189 is a cell-permeable, highly potent and selective BMP pathway inhibitor by inhibiting BMP type I receptors ALK2 (IC50=5 nM) and ALK3 (IC50=30 nM), but not ALK4, ALK5, and ALK7 (> 0.5 µM). It prevents Smad1, Smad5, and Smad8 phosphorylation. It is a useful tool compound to modulate stem cell differentiation (for example, neural differentiation of human ESC/iPSC in combination with SB431542). It was also used in animal models to treat FOP and ectopic ossification, as well as NSCLC lung cancer.

 

How to Use:

  • In vitro: LDN-193189 is typically used at 0.1 µM final concentration in stem cell differentiation conditions.
  • In vivo: Intraperitoneal (IP) administration of 3 mg/kg LDN-193189 was used once or twice daily.

 

Reference: 

  • 1.  Cuny GD, et al.  Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. (2008), Bioorg Med Chem Lett. 18(15):4388-92.
  • 2.  Paul B Yu, et al. BMP type I receptor inhibition reduces heterotopic ossification. (2008), Nature Med. 14: 1363-1369.
  • 3.  Yu PB, et al.  Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. (2008), Nature Chem Biol. 4: 33-41.
  • 4.  Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. (2009), Nature Biotechnology 27, 275-280.
  • 5.  Boergermann JH, et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. (2010), Int J Biochem Cell Biol. 42(11):1802-7.
  • 6.  Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis.  (2011), Cancer Res 71:5194-5203.
  • 7.  Najm FJ, et al. Rapid and robust generation of functional oligodendrocyte progenitor cells from epiblast stem cells. (2011) Nature Methods 8, 957–962



 

 Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 406.48
Formula: C25H22N6
Purity: ≥98%
CAS#: 1062368-24-4
Solubility: DMSO up to 100 mM
Chemical Name: 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

LDN193189 is a cell-permeable, highly potent and selective BMP pathway inhibitor by inhibiting BMP type I receptors ALK2 (IC50=5 nM) and ALK3 (IC50=30 nM), but not ALK4, ALK5, and ALK7 (> 0.5 µM). It prevents Smad1, Smad5, and Smad8 phosphorylation. It is a useful tool compound to modulate stem cell differentiation (for example, neural differentiation of human ESC/iPSC in combination with SB431542). It was also used in animal models to treat FOP and ectopic ossification, as well as NSCLC lung cancer.

 

How to Use:

  • In vitro: LDN-193189 is typically used at 0.1 µM final concentration in stem cell differentiation conditions.
  • In vivo: Intraperitoneal (IP) administration of 3 mg/kg LDN-193189 was used once or twice daily.

 

Reference: 

  • 1.  Cuny GD, et al.  Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. (2008), Bioorg Med Chem Lett. 18(15):4388-92.
  • 2.  Paul B Yu, et al. BMP type I receptor inhibition reduces heterotopic ossification. (2008), Nature Med. 14: 1363-1369.
  • 3.  Yu PB, et al.  Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. (2008), Nature Chem Biol. 4: 33-41.
  • 4.  Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. (2009), Nature Biotechnology 27, 275-280.
  • 5.  Boergermann JH, et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. (2010), Int J Biochem Cell Biol. 42(11):1802-7.
  • 6.  Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis.  (2011), Cancer Res 71:5194-5203.
  • 7.  Najm FJ, et al. Rapid and robust generation of functional oligodendrocyte progenitor cells from epiblast stem cells. (2011) Nature Methods 8, 957–962



 

 Products are for research use only. Not for human use.

Reviews

  1. review Review by info@xcessbio.com
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    Value

    Question:

    A few months ago, I ordered 20mg of LDN-193189 for some in vivo experiments. I continuously infused the Bmp pathway inhibitor via osmotic mini pumps. However, I need to measure steady-state plasma levels of the inhibitor for publication purposes. Can you send me a protocol on how to do this? Also, is LDN-193189 soluble in methanol? For a different application, I cannot use DMSO to solubilize the drug.

     

    Our reply:

    XcessBio is a reagent company, so we do not have capability to do in vivo studies. For minipumps dosing, you can see attached publication for your reference. They used mini pumps to dose another compound and measure steady-state plasma levels of drug. Unfortunately LDN-193189 has low solubility in MeOH or EtOH. From publication, this drug has some solubility in water, about ~10 mg/mL, maybe good enough for you to test it. 


    mini pumps dosing, cpd EPZ004777.pdf

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