LDN-193189

Catalog No.S2618 Synonyms: DM3189

For research use only.

LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.

LDN-193189 Chemical Structure

CAS No. 1062368-24-4

Selleck's LDN-193189 has been cited by 177 publications

Purity & Quality Control

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Biological Activity

Description LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.
Targets
ALK1 [5]
(Cell-free assay)
ALK2 [5]
(Cell-free assay)
ALK3 [5]
(Cell-free assay)
ALK6 [5]
(Cell-free assay)
0.8 nM 0.8 nM 5.3 nM 16.7 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 NUPZVItRU2mwYYPlJGF{e2G7 MmTBbY5pcWKrdIOgeIhmKGurbnHz[UBi[3Srdnn0fUBw\iCDTFu0JIFv\CCDY4TSTWlCKHerdHigTWM2OMLidnHseYV{KG:oIEGwNUBidmRiMkGwJI5uNCC{ZYPw[YN1cX[nbIm= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN4OEOyNkc,OjV|NkizNlI9N2F-
EOC216 NXzFWGt1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrDNE4yNTFyIN88US=> Ml73Nk0yOCCm MULEUXNQ NHzkWWFqdmS3Y3WgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{Mke4PVMoRjJ3MkK3PFk{RC:jPh?=
OVAC429 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6yM|Uh|ryP NUjROZBkPDhiaB?= NWP3b4RpTE2VTx?= MXfk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| NFPCW3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyO|g6Oyd-MkWyNlc5QTN:L3G+
SKOV3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqyM|Uh|ryP NW\URYlHPDhiaB?= NES0UlhFVVOR M3nJR4Rm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= M4nWdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkK3PFk{Lz5{NUKyO|g6OzxxYU6=
OVCA429 NYPxS2FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGyM|Uh|ryP M4jrNVQ5KGh? NF7DclVFVVOR NFSyVndl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz NV7henZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNlc5QTNpPkK1NlI4QDl|PD;hQi=>
EOC219 M3LXfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHPNk82KM7:TR?= NInwTnQ1QCCq NXvRVlFPTE2VTx?= NVjEd2x4\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> M2O0XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkK3PFk{Lz5{NUKyO|g6OzxxYU6=
A549 M2nVfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf3ZmFYOC53LUG2JO69VQ>? MmPGSG1UVw>? M2C3dolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkjWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{iwNVEoRjJ2N{e4NFEyRC:jPh?=
BEAS-2B  NHq5[mxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Pv[lAvPS1zNjFOwG0> MXPEUXNQ M37mXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{iwNVEoRjJ2N{e4NFEyRC:jPh?=
hBMSCs MnfCSpVv[3Srb36gRZN{[Xl? NUe3dHRYOC5{wrFOwG0> Moq5O{Bl NX:3RYdw[WKxbHnzbIV{KHSqZTDzbYxq[mmwaX6tdJJwdW:2ZXSgRWxRKGGldHn2bZR6yqCyYYL0cJk> NVjGdYhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwO|YyQDdpPkK0NFc3OTh5PD;hQi=>
PANC-1 M1vsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvreWdwPS13MECgcm0> NIDycXo1QCCq NYf3TWJQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nkm3NlkoRjJ|OU[5O|I6RC:jPh?=
MIA PaCa-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUS1MVUxOCCwTR?= M1LOSFQ5KGh? M{jad4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mnv3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nkm3NlkoRjJ|OU[5O|I6RC:jPh?=
Bx-PC3 NYrvVXFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDYOU02ODBibl2= MWW0PEBp NUTvPIU5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFGxWow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2PVczQSd-MkO5Olk4Ojl:L3G+
PC3  NXSxOGRzTnWwY4Tpc44hSXO|YYm= NXPYfGZpPTByIH7N M1m1bVIhcA>? Mme4doVxemW|c3XzJIFkfGm4YYTpc44hd2ZiU33h[FEwPS96IHHu[EBRNVOvYXSzJIxmfmWucx?= M1zPPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEWyPFg{Lz5{MkS1Nlg5OzxxYU6=
LNCaP MVvGeY5kfGmxbjDBd5NigQ>? MYKw5qCUPTByIH7N NHSxXXYzKGh? MXTy[ZZmenOnczDyZZBidXmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo NFO5OYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS1Nlg5Oyd-MkK0OVI5QDN:L3G+
EOC MXXGeY5kfGmxbjDBd5NigQ>? MYCxNE0yODByIH7N MmnrO|IhcA>? M4jOTpJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHXkJGJOWCCULWPtZYQyNzVxONMg NGjjc2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK0PVQyPSd-MkKyOFk1OTV:L3G+
HaCaT  M3;FXGZ2dmO2aX;uJGF{e2G7 NHexdpExNjByMT2xNEDPxE1? NYLYSpVvOiCq MkPybY5pcWKrdIOgRm1ROi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCVbXHkNU82Nzhid3n0bEBidiCLQ{WwxsBw\iC-MD6wNFXDqM7:TR?= NHrifWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe0NFk3Pid-MkG3OFA6PjZ:L3G+
HaCaT  NH\NUJFHfW6ldHnvckBCe3OjeR?= NGHjNY4xNjByMT2xNEDPxE1? Mlm2NkBp M2W2UIlvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|IhfG9icHjvd5Bpd3K7bHH0[UBIW1RvU33h[FHDqHerdHigZY4hUUN3MNMgc4YhPDYEoH7N NX7YPJZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3OFA6PjZpPkKxO|QxQTZ4PD;hQi=>
HaCaT  Ml\5SpVv[3Srb36gRZN{[Xl? M3u4R|AvODBzLUGwJO69VQ>? MlW0NkBp NXfmVXJpcW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOyC2bzDwbI9{eGixconsZZRmKFOvYXSxxsB4cXSqIHHuJGlEPTEEoH;mJFExOCCwTR?= NYXTTIg2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3OFA6PjZpPkKxO|QxQTZ4PD;hQi=>
HaCaT  NFS2SXJHfW6ldHnvckBCe3OjeR?= NILBR5ExNjByMT2xNEDPxE1? NEHCdm0zKGh? MWLpcohq[mm2czDBUGs1KGGwZDDBUGs2KHerdHigTWM2OMLidnHseYV{KG:oIECuN:Kh|ryPIHHu[EAxNjYEoN88UUBz\XOyZXP0bZZmdHl? M3jvXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{SwPVY3Lz5{MUe0NFk3PjxxYU6=
C2C12 MYPGeY5kfGmxbjDhd5NigQ>? MoOzN|AhdWmwcx?= NFrKUIZKdmirYnn0bY9vKG:oIFLNVFYucW6mdXPl[EBCVEt{IITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDtc5V{\SCFMlOxNkBk\WyuczDlfJBz\XO|aX7nJGJTTS2OdXOgZYZ1\XJiM{CgcYlveyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjBzNDFOwG0v Mlr1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{Mke5OFYoRjNyMkK3PVQ3RC:jPh?=
BT-12 NELIbGdyUFSVIHHzd4F6 NGnYUFByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= NFPkeHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
fibroblast cell MWLxTHRUKGG|c3H5 NVnkPIh6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IHPvcpRzd2xiSHige4lt\CC2eYDlJIZq[nKxYnzhd5Qh[2WubIO= M1X2S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 NYLkVnlLeUiWUzDhd5NigQ>? MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh|MDDj[Yxtew>? MnvyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
KB-3-1 M{e2NGZ2dmO2aX;uJIF{e2G7 M{e4[3Au\2y7Y3;wdo91\WmwIIP1ZpN1emG2ZYOgbYRmdnSrZnnl[EBqdiCNQj2zMVEh[WSnbn;jZZJkcW6xbXGgZ4VtdCCuaX7lMEByUFSVIITo[ZJieGW3dHnjJIxq[nKjcomgd4Nz\WWw NVfFelV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G1NVUzQDRpPkOxOVE2Ojh2PD;hQi=>
C2C12 Ml:1SpVv[3Srb36gZZN{[Xl? MoW3NE4yKHWP M3j4[WlvcGmkaYTpc44hd2ZiQVzLOUBqdiCvb4Xz[UBEOkNzMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBVT0[kZYThNU1qdmS3Y3XkJHNu[WRzL{WgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC3TTDifUBY\XO2ZYLuJIJtd3RibXX0bI9l NYfEPIhnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNFMxOjVpPkK4NVA{ODJ3PD;hQi=>
Assay
Methods Test Index PMID
Western blot pSMAD1 / pSMAD5 / pSMAD8 / SMAD1 / SMAD5 / SMAD8 / ID1 / SMAD4 / PARP / Cleaved PARP 31098401
Immunofluorescence Tbx18 / Hcn4 30906456
Growth inhibition assay Cell viability 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 (from reference)

Animal Research:

[1]

  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 406.48
Formula

C25H22N6

CAS No. 1062368-24-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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