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 171 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 MoTZT4lv[XOnIFHzd4F6 NGrmO3BqdmirYnn0d{B1cGVia3nuZZNmKGGldHn2bZR6KG:oIFHMT|Qh[W6mIFHjeHJKUUFid3n0bEBKSzVywrD2ZYx2\XNib3[gNVAyKGGwZDCyNVAhdm1uIILld5Bm[3SrdnXsfS=> NEjndos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO2PFMzOid-MkWzOlg{OjJ:L3G+
EOC216 M{GwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zvUVAvOS1zMDFOwG0> NWf4[FhUOi1zMDDk NWW2T|NqTE2VTx?= MXXpcoR2[2ViY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MlvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{Mke4PVMoRjJ3MkK3PFk{RC:jPh?=
OVAC429 NW\3Sos{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLRNk82KM7:TR?= MUe0PEBp NH7nWoFFVVOR NVnxNms6\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MoT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{Mke4PVMoRjJ3MkK3PFk{RC:jPh?=
SKOV3 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDwNk82KM7:TR?= MmHXOFghcA>? NYTQbZdITE2VTx?= NXv2S5FR\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> NHnrRpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyO|g6Oyd-MkWyNlc5QTN:L3G+
OVCA429 NXrLe2w3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TCXFIwPSEQvF2= MWS0PEBp M2SzTWROW09? NFewc2pl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz M4q0bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkK3PFk{Lz5{NUKyO|g6OzxxYU6=
EOC219 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjFNk82KM7:TR?= MmrWOFghcA>? NFf0bFZFVVOR MnXW[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= M{fXR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkK3PFk{Lz5{NUKyO|g6OzxxYU6=
A549 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL3NE42NTF4IN88US=> M3fwcWROW09? NYTKbI9IcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NX;xW4tbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|gxOTFpPkK0O|c5ODFzPD;hQi=>
BEAS-2B  M2PPRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LOZ|AvPS1zNjFOwG0> MWfEUXNQ M2LKWYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYTISpNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|gxOTFpPkK0O|c5ODFzPD;hQi=>
hBMSCs NF3FPGdHfW6ldHnvckBCe3OjeR?= NHzzSI0xNjMEoN88US=> MmjKO{Bl NVjRSGRS[WKxbHnzbIV{KHSqZTDzbYxq[mmwaX6tdJJwdW:2ZXSgRWxRKGGldHn2bZR6yqCyYYL0cJk> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB5NkG4O{c,OjRyN{[xPFc9N2F-
PANC-1 MkXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvoR2pzPS13MECgcm0> MoTXOFghcA>? MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MofPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nkm3NlkoRjJ|OU[5O|I6RC:jPh?=
MIA PaCa-2 NEL3cXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUmxe2p1PS13MECgcm0> NFnidG81QCCq MUTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF\tT2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2PVczQSd-MkO5Olk4Ojl:L3G+
Bx-PC3 NWPWe3JtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVm1MVUxOCCwTR?= MlrNOFghcA>? MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4XLUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OU[5O|I6Lz5{M{m2PVczQTxxYU6=
PC3  NUC1UpJTTnWwY4Tpc44hSXO|YYm= NWTVblc{PTByIH7N NX7Fd3Z3OiCq NH\N[2Nz\XC{ZYPz[ZMh[WO2aY\heIlwdiCxZjDTcYFlOS93L{igZY5lKFBvU33h[FMhdGW4ZXzz NUn5[FM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0OVI5QDNpPkKyOFUzQDh|PD;hQi=>
LNCaP NWixTmN3TnWwY4Tpc44hSXO|YYm= M{LFW|DjiJN3MECgcm0> MUCyJIg> MkDDdoV3\XK|ZYOgdoFx[W27Y3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> M{TxOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEWyPFg{Lz5{MkS1Nlg5OzxxYU6=
EOC NYT4d3pxTnWwY4Tpc44hSXO|YYm= MnfNNVAuOTByMDDuUS=> M3XEPVczKGh? Mlq2doVlfWOnczD0bIUheGixc4Doc5J6dGG2ZXSgRm1RKFJvU33h[FEwPS96wrC= MnrDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NEm0NVUoRjJ{MkS5OFE2RC:jPh?=
HaCaT  NVvYXYdRTnWwY4Tpc44hSXO|YYm= NETKVpgxNjByMT2xNEDPxE1? MV[yJIg> MYTpcohq[mm2czDCUXAzNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKFOvYXSxM|UwQCC5aYToJIFvKEmFNUFCpI9nKH5yLkCwOeKh|ryP M2nad|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{SwPVY3Lz5{MUe0NFk3PjxxYU6=
HaCaT  MkLoSpVv[3Srb36gRZN{[Xl? M1X5d|AvODBzLUGwJO69VQ>? NILocYwzKGh? M1\tfolvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|IhfG9icHjvd5Bpd3K7bHH0[UBIW1RvU33h[FHDqHerdHigZY4hUUN3MNMgc4YhPDYEoH7N MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd2MEm2Okc,OjF5NEC5OlY9N2F-
HaCaT  M4X1cGZ2dmO2aX;uJGF{e2G7 MVywMlAxOS1zMDFOwG0> NInSOnYzKGh? M3r6V4lvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|MhfG9icHjvd5Bpd3K7bHH0[UBUdWGmMdMge4l1cCCjbjDJR|UxyqCxZjCxNFAhdk1? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd2MEm2Okc,OjF5NEC5OlY9N2F-
HaCaT  MXHGeY5kfGmxbjDBd5NigQ>? NEizW|ExNjByMT2xNEDPxE1? MoH4NkBp NV3kN3N1cW6qaXLpeJMhSUyNNDDhcoQhSUyNNTD3bZRpKEmFNUFCpJZidHWnczDv[kAxNjQEoN88UUBidmRiMD61xsDPxE1icnXzdIVkfGm4ZXz5 NHjtWpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe0NFk3Pid-MkG3OFA6PjZ:L3G+
C2C12 NGnVdWtHfW6ldHnvckBie3OjeR?= M4CxTVMxKG2rboO= NYfP[Y5pUW6qaXLpeIlwdiCxZjDCUXA3NWmwZIXj[YQhSUyNMjD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gcY92e2ViQ{LDNVIh[2WubIOg[ZhxemW|c3nu[{BDWkVvTIXjJIFnfGW{IEOwJI1qdnNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC5yMUSg{txONg>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ{N{m0Okc,OzB{Mke5OFY9N2F-
BT-12 NEW0cGZyUFSVIHHzd4F6 NV3v[WdleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz Ml\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
fibroblast cell M3rmdpFJXFNiYYPzZZk> M{Hub5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| MmXNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 NEjRZo1yUFSVIHHzd4F6 NH;pfGFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnizNEBk\Wyucx?= NEfuXFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
KB-3-1 MY\GeY5kfGmxbjDhd5NigQ>? MYjQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvMz2xJIFl\W6xY3HyZ4lvd22jIHPlcIwhdGmwZTygdWhVWyC2aHXyZZBmfXSrYzDsbYJz[XK7IIPjdoVmdg>? MlW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
C2C12 MU\GeY5kfGmxbjDhd5NigQ>? MV[wMlEhfU1? NECz[o5KdmirYnn0bY9vKG:oIFHMT|UhcW5ibX;1d4UhSzKFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hXEeIYnX0ZVEucW6mdXPl[EBUdWGmMT:1JJBpd3OyaH;yfYxifGmxbjDheEAxNjFidV2gZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? M{XsRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUCzNFI2Lz5{OEGwN|AzPTxxYU6=
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.
  • (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 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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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