LDN-193189

For research use only.

Catalog No.S2618 Synonyms: DM3189

138 publications

LDN-193189 Chemical Structure

CAS No. 1062368-24-4

LDN-193189 (DM3189) 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 138 publications

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Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description LDN-193189 (DM3189) 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 MmS5T4lv[XOnIFHzd4F6 M2PSVIlvcGmkaYTzJJRp\SCtaX7hd4Uh[WO2aY\peJkhd2ZiQVzLOEBidmRiQXP0VmlKSSC5aYToJGlEPTEEoI\hcJVmeyCxZjCxNFEh[W6mIEKxNEBvdSxicnXzdIVkfGm4ZXz5 MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN4OEOyNkc,OjV|NkizNlI9N2F-
EOC216 NVjxS49OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\NPVAvOS1zMDFOwG0> M{jiVlIuOTBiZB?= MVfEUXNQ NFnHfpFqdmS3Y3WgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1zrTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkK3PFk{Lz5{NUKyO|g6OzxxYU6=
OVAC429 MnLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjkRppTOi93IN88US=> MX20PEBp NH;1cVFFVVOR MYjk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| NXi0T5J2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNlc5QTNpPkK1NlI4QDl|PD;hQi=>
SKOV3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSyM|Uh|ryP NGC5fWw1QCCq NEPHS4JFVVOR Mon1[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{N{i5N{c,OjV{Mke4PVM9N2F-
OVCA429 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfvNk82KM7:TR?= MV20PEBp NIHHOXBFVVOR NVixR|B2\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{N{i5N{c,OjV{Mke4PVM9N2F-
EOC219 M3mzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmyM|Uh|ryP NFfjVYc1QCCq NXXMSopuTE2VTx?= NInoXYZl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{N{i5N{c,OjV{Mke4PVM9N2F-
A549 M{PD[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqwMlUuOTZizszN NYT5eGVETE2VTx?= NWKwVGMzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{iwNVEoRjJ2N{e4NFEyRC:jPh?=
BEAS-2B  NGr3fmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[wMlUuOTZizszN NVHQRodRTE2VTx?= M37mZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFPGdIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PFAyOSd-MkS3O|gxOTF:L3G+
hBMSCs NHvxNFhHfW6ldHnvckBCe3OjeR?= NUnTe5hsOC5{wrFOwG0> NV3r[I5{PyCm NXzIWGlC[WKxbHnzbIV{KHSqZTDzbYxq[mmwaX6tdJJwdW:2ZXSgRWxRKGGldHn2bZR6yqCyYYL0cJk> NGXrSpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC3OlE5Pyd-MkSwO|YyQDd:L3G+
PANC-1 M1XsNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYG1MVUxOCCwTR?= MXu0PEBp NYPzbJc{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4fsTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[5O|I6Lz5{M{m2PVczQTxxYU6=
MIA PaCa-2 M4XMbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7lUIM2NTVyMDDuUS=> M{XDfFQ5KGh? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV7sUY5SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5Olk4OjlpPkKzPVY6PzJ7PD;hQi=>
Bx-PC3 NF;CZ|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL3PHA{PS13MECgcm0> NGXRNpQ1QCCq MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4OUeyPUc,OjN7Nkm3Nlk9N2F-
PC3  NU[4TZRkTnWwY4Tpc44hSXO|YYm= MXu1NFAhdk1? MYiyJIg> NETUSIxz\XC{ZYPz[ZMh[WO2aY\heIlwdiCxZjDTcYFlOS93L{igZY5lKFBvU33h[FMhdGW4ZXzz MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3Mki4N{c,OjJ2NUK4PFM9N2F-
LNCaP MVnGeY5kfGmxbjDBd5NigQ>? NXvkeXg4OOLCk{WwNEBvVQ>? NEL3UJUzKGh? M4\BSZJmfmW{c3XzJJJieGGveXPpck1qdmS3Y3XkJINmdGxiZHXheIg> NITlRmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS1Nlg5Oyd-MkK0OVI5QDN:L3G+
EOC MnnKSpVv[3Srb36gRZN{[Xl? NUjOW5JpOTBvMUCwNEBvVQ>? M3jVd|czKGh? M4TYWpJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHXkJGJOWCCULWPtZYQyNzVxONMg MmnYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NEm0NVUoRjJ{MkS5OFE2RC:jPh?=
HaCaT  MnewSpVv[3Srb36gRZN{[Xl? MYiwMlAxOS1zMDFOwG0> M1\Yd|IhcA>? Mmi4bY5pcWKrdIOgRm1ROi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCVbXHkNU82Nzhid3n0bEBidiCLQ{WwxsBw\iC-MD6wNFXDqM7:TR?= NIfqeWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe0NFk3Pid-MkG3OFA6PjZ:L3G+
HaCaT  M2LpUmZ2dmO2aX;uJGF{e2G7 MlHZNE4xODFvMUCg{txO NWLQZmNMOiCq M3rkcYlvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|IhfG9icHjvd5Bpd3K7bHH0[UBIW1RvU33h[FHDqHerdHigZY4hUUN3MNMgc4YhPDYEoH7N NUPWOZFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3OFA6PjZpPkKxO|QxQTZ4PD;hQi=>
HaCaT  NYHQOmxkTnWwY4Tpc44hSXO|YYm= MX[wMlAxOS1zMDFOwG0> MoLSNkBp M4TLdIlvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|MhfG9icHjvd5Bpd3K7bHH0[UBUdWGmMdMge4l1cCCjbjDJR|UxyqCxZjCxNFAhdk1? MoTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5NEC5OlYoRjJzN{SwPVY3RC:jPh?=
HaCaT  MXLGeY5kfGmxbjDBd5NigQ>? Mnz0NE4xODFvMUCg{txO MnrhNkBp NGG2eHBqdmirYnn0d{BCVEt2IHHu[EBCVEt3IIfpeIghUUN3MNMgeoFtfWW|IH;mJFAvO8LizszNJIFv\CByLkZCpO69VSC{ZYPw[YN1cX[nbIm= Mo[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5NEC5OlYoRjJzN{SwPVY3RC:jPh?=
C2C12 NIL6V2NHfW6ldHnvckBie3OjeR?= MoixN|AhdWmwcx?= NWDwUnZLUW6qaXLpeIlwdiCxZjDCUXA3NWmwZIXj[YQhSUyNMjD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gcY92e2ViQ{LDNVIh[2WubIOg[ZhxemW|c3nu[{BDWkVvTIXjJIFnfGW{IEOwJI1qdnNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC5yMUSg{txONg>? NX;ZNHlORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNlc6PDZpPkOwNlI4QTR4PD;hQi=>
BT-12 MlnrdWhVWyCjc4PhfS=> M3HjbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= Mk\2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
fibroblast cell MXXxTHRUKGG|c3H5 MWDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? M3vifFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 M3e5fJFJXFNiYYPzZZk> NWrPXoExeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= MojBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
KB-3-1 NGfyUIlHfW6ldHnvckBie3OjeR?= M2e1fnAu\2y7Y3;wdo91\WmwIIP1ZpN1emG2ZYOgbYRmdnSrZnnl[EBqdiCNQj2zMVEh[WSnbn;jZZJkcW6xbXGgZ4VtdCCuaX7lMEByUFSVIITo[ZJieGW3dHnjJIxq[nKjcomgd4Nz\WWw MnfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
C2C12 NXPwUnBMTnWwY4Tpc44h[XO|YYm= NGfCeFAxNjFidV2= MoGwTY5pcWKrdHnvckBw\iCDTFu1JIlvKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJHRITmKndHGxMYlv\HWlZXSgV41i\DFxNTDwbI9{eGixconsZZRqd25iYYSgNE4yKHWPIHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDFyM{CyOUc,OjhzMEOwNlU9N2F-

... 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