LDN-193189, BMP inhibitor


Catalog No. size PriceQuantity
M60008-2D 10 mM in DMSO (0.493 mL) $79
M60008-2S 2mg solid $79
M60008-25S 25mg solid $550

Description

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.

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