LDN-193189

For research use only.

Catalog No.S2618 Synonyms: DM3189

99 publications

LDN-193189 Chemical Structure

Molecular Weight(MW): 406.48

LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

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Selleck's LDN-193189 has been cited by 99 publications

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Biological Activity

Description LDN-193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
Targets
ALK2 [1]
(C2C12 cells)
ALK3 [1]
(C2C12 cells)
5 nM 30 nM
In vitro

LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. [1] A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C2C12 NWnnfXBxU2mwYYPlJGF{e2G7 M{fJVIlvcGmkaYTzJJRp\SCtaX7hd4Uh[WO2aY\peJkhd2ZiQVzLOEBidmRiQXP0VmlKSSC5aYToJGlEPTEEoI\hcJVmeyCxZjCxNFEh[W6mIEKxNEBvdSxicnXzdIVkfGm4ZXz5 NWjhSopGOjV|NkizNlI>
EOC216 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\RNE4yNTFyIN88US=> MYeyMVExKGR? MUXEUXNQ NH7ze2hqdmS3Y3WgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVXBfI9{OjV{Mke4PVM>
OVAC429 M4P4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXiyM|Uh|ryP NYf1VWxGPDhiaB?= NFrlWJFFVVOR M4jufYRm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= MWiyOVIzPzh7Mx?=
SKOV3 NFuyNFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmzOZozNzVizszN MofYOFghcA>? MYnEUXNQ MmnX[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= Ml3mNlUzOjd6OUO=
OVCA429 MmrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWiyM|Uh|ryP NI\pNoY1QCCq MXfEUXNQ NE\CT2xl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz M1vKPFI2OjJ5OEmz
EOC219 NWCyRWY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfDSWNGOi93IN88US=> MkjiOFghcA>? NETKWpVFVVOR M2TXfIRm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= MkThNlUzOjd6OUO=
A549 NFHjcFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fQXlAvPS1zNjFOwG0> Mn7TSG1UVw>? MlX3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmrFNlQ4PzhyMUG=
BEAS-2B  NVn4T4F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f1cVAvPS1zNjFOwG0> M3P2PWROW09? NYTHeGF6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYLqO5pZOjR5N{iwNVE>
hBMSCs MkPESpVv[3Srb36gRZN{[Xl? NFS5c|kxNjMEoN88US=> NWPEUpFZPyCm MorWZYJwdGm|aHXzJJRp\SC|aXzpZolvcW5vcILvcY91\WRiQVzQJIFkfGm4aYT5xsBx[XK2bIm= NIKyWpUzPDB5NkG4Oy=>
PANC-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PES|UuPTByIH7N MX[0PEBp NYfMeWpycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGmyZ24zOzl4OUeyPS=>
MIA PaCa-2 NH7U[WhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fie|UuPTByIH7N MnrrOFghcA>? MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWrlNIVzOjN7Nkm3Nlk>
Bx-PC3 M4DpWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3uy[|UuPTByIH7N M{PBUVQ5KGh? NYe5coh2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NUiwO4c1OjN7Nkm3Nlk>
PC3  MWfGeY5kfGmxbjDBd5NigQ>? MnLZOVAxKG6P M3\IZVIhcA>? M2nPSpJmeHKnc4Pld{Bi[3SrdnH0bY9vKG:oIGPtZYQyNzVxODDhcoQhWC2VbXHkN{Bt\X[nbIO= NVi4NohrOjJ2NUK4PFM>
LNCaP M2nCS2Z2dmO2aX;uJGF{e2G7 NFL6NWkx6oDVNUCwJI5O MXyyJIg> M4DSUJJmfmW{c3XzJJJieGGveXPpck1qdmS3Y3XkJINmdGxiZHXheIg> MkfYNlI1PTJ6OEO=
EOC MXLGeY5kfGmxbjDBd5NigQ>? MVyxNE0yODByIH7N M2Ky[FczKGh? MnzvdoVlfWOnczD0bIUheGixc4Doc5J6dGG2ZXSgRm1RKFJvU33h[FEwPS96wrC= MV:yNlI1QTRzNR?=
HaCaT  M{n0XGZ2dmO2aX;uJGF{e2G7 NGjadYUxNjByMT2xNEDPxE1? M{[4NlIhcA>? M{n3eYlvcGmkaYTzJGJOWDJvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiU33h[FEwPS96IIfpeIgh[W5iSVO1NOKhd2ZifkCuNFA2yqEQvF2= NX\pco92OjF5NEC5OlY>
HaCaT  MW\GeY5kfGmxbjDBd5NigQ>? Mo\zNE4xODFvMUCg{txO MkPwNkBp NXHjbHJicW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOiC2bzDwbI9{eGixconsZZRmKEeVVD3TcYFlOcLid3n0bEBidiCLQ{WwxsBw\iB2NdMgcm0> NYLIPIdIOjF5NEC5OlY>
HaCaT  MXTGeY5kfGmxbjDBd5NigQ>? NFjVUnYxNjByMT2xNEDPxE1? M4XEflIhcA>? MonZbY5pcWKrdIOgeIhmKGGkaXzpeJkhd2ZiQVzLN{B1dyCyaH;zdIhwenmuYYTlJHNu[WRzwrD3bZRpKGGwIFnDOVDDqG:oIEGwNEBvVQ>? NUnDO4Z2OjF5NEC5OlY>
HaCaT  NIWybYtHfW6ldHnvckBCe3OjeR?= NIHmSWMxNjByMT2xNEDPxE1? NE[ze|kzKGh? NFTwfmJqdmirYnn0d{BCVEt2IHHu[EBCVEt3IIfpeIghUUN3MNMgeoFtfWW|IH;mJFAvO8LizszNJIFv\CByLkZCpO69VSC{ZYPw[YN1cX[nbIm= M{HSZlIyPzRyOU[2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pSMAD1 / pSMAD5 / pSMAD8 / SMAD1 / SMAD5 / SMAD8 / ID1 / SMAD4 / PARP / Cleaved PARP; 

PubMed: 31098401     


In vitro molecular pharmacology of LDN-193189 and LDN-214117. Western blot analysis of time- and concentration-dependent effects on downstream signalling in response to a LDN-193189 and b LDN-214117 in DIPG cells. Increasing concentrations (0–10 µM) at 4 and 8 h are shown for SU-DIPG-VI, HSJD-DIPG-IV and HSJD-DIPG-007. GAPDH is the loading control.

31098401
Immunofluorescence
Tbx18 / Hcn4; 

PubMed: 30906456     


Representative immunofluorescence microscopy images of epicardial progenitor cells from the four groups with staining for Hcn4 (red). The nuclei were counterstained with DAPI (blue) and the YFP expressed by the cells is apparent (scale bar, 50 µm). (Tbx18 was conjugated to YFP).

30906456
Growth inhibition assay
Cell viability; 

PubMed: 31098401     


Screening of ALK2 inhibitors in vitro. Concentration-response curves for eight ALK2 inhibitors tested against three ACVR1 mutant cell cultures (HSJD-DIPG-007 (R206H), SU-DIPG-IV (G328V), HSJD-DIPG-018 (R258G), purple) and two wild-type cultures (SU-DIPG-VI, QCTB-R059, grey). a Pyrazolo[1,5-a]pyrimidines—dorsomorphin, LDN-193189, DMH1, LDN-212854. b Pyridines—K02288, LDN-214117, LDN-213844, LDN-213819. Concentration of compound is plotted on a log scale (x-axis) against cell viability (y-axis). Mean plus standard deviation are plotted from at least n = 3 experiments.

31098401
In vivo In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities. [1] LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. [2] In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. [3] In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. [4]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
  • Dosages: ≤3 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO Insoluble
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 406.48
Formula

C25H22N6

CAS No. 1062368-24-4
Storage powder
in solvent
Synonyms DM3189
Smiles C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID