LDN-193189

Catalog No.S2618 Synonyms: DM3189

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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5 Customer Reviews

  • The small molecule BMP inhibitor LDN-193189 can partially block the increased BMP signaling in Jab1flox/flox, Col2a1-Cre mutants in a dose-dependent manner. Primary chondrocytes were cultured in DMEM medium containing 10% FBS and indicated amounts of LDN-193189 for 24 hours before being subjected to immunoblotting.

    J Cell Sci, 2013, 126: 234-43. LDN-193189 purchased from Selleck.

    LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.

    Int J Cancer 2014 136(5):E455-69. LDN-193189 purchased from Selleck.

  • The density of muscle fibers and myoseptum are partially rescued in morphants treated with LDN to decrease BMP signaling (D–F) .These were fixed at 24 hpf and labeled with an antibody against Pax7, which strongly labels neural crest derived cells and also labels dermomyotome cells.

    Dev Biol 2014 378:107-121. LDN-193189 purchased from Selleck.

    (C) Smad1/5/9 phosphorylation and Smad1 protein levels were monitored in BMP-2 stimulated cells for up to 60 min. β-actin served as a loading control; BMP, bone morphogenetic protein.

    Oncol Rep, 2017, 37(2):713-720. LDN-193189 purchased from Selleck.

  • The influence of SB431542 and LDN193189 on a-SMA in A549 cells. (a) Representative images of immunofluorescence analysis for a-SMA using confocal microscopy are shown (scale bar ¼ 25 lm). (b) Relative densitometry diagram and typical western blot bands of a-SMA expression in the six groups (A–F). Data are expressed as mean ± SD (n ¼ 5 in each group). #p < 0.05 versus CONTROL group, p < 0.05 versus SILICA group

    Toxicol Mech Methods, 2018, 28(4):286-292. LDN-193189 purchased from Selleck.

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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 NG\O[VNMcW6jc3WgRZN{[Xl? Mk\wbY5pcWKrdIOgeIhmKGurbnHz[UBi[3Srdnn0fUBw\iCDTFu0JIFv\CCDY4TSTWlCKHerdHigTWM2OMLidnHseYV{KG:oIEGwNUBidmRiMkGwJI5uNCC{ZYPw[YN1cX[nbIm= NV7DO21{OjV|NkizNlI>
EOC216 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LFNlAvOS1zMDFOwG0> NWPFd5A5Oi1zMDDk NWKxcmJ{TE2VTx?= NH7FfZRqdmS3Y3WgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{O3ZlI2OjJ5OEmz
OVAC429 MoHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknKNk82KM7:TR?= NIXW[3M1QCCq NV2ydGJvTE2VTx?= MXLk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| NVzYVnd2OjV{Mke4PVM>
SKOV3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v4cFIwPSEQvF2= MX:0PEBp NInwVZZFVVOR MVTk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| MkL1NlUzOjd6OUO=
OVCA429 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknGNk82KM7:TR?= MXm0PEBp MXvEUXNQ M{HSfYRm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= NGf5SGwzPTJ{N{i5Ny=>
EOC219 Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\INFIwPSEQvF2= MnnZOFghcA>? MYTEUXNQ NXf6TY5E\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MV:yOVIzPzh7Mx?=
A549 NFy5elhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\qdpc3OC53LUG2JO69VQ>? M{H2cWROW09? MlK5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnqzNlQ4PzhyMUG=
BEAS-2B  NYHnOZFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYGwMlUuOTZizszN NUjUd5FNTE2VTx?= M{W4c4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkTpNlQ4PzhyMUG=
hBMSCs M3zBUWZ2dmO2aX;uJGF{e2G7 NYXDTXRyOC5{wrFOwG0> NWe2UHpJPyCm NEKycm9i[m:uaYPo[ZMhfGinIIPpcIljcW6rbj3wdo9ud3SnZDDBUHAh[WO2aY\peJnDqHCjcoTsfS=> M4XSZVI1ODd4MUi3
PANC-1 NHX3e21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnOyOU02ODBibl2= MnH0OFghcA>? NET0S4pqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmLiNlM6Pjl5Mkm=
MIA PaCa-2 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT2OU02ODBibl2= MWm0PEBp MljUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVuyN|k3QTd{OR?=
Bx-PC3 NIPDeHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf2OU02ODBibl2= MV20PEBp M3LiNolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUXqcII3OjN7Nkm3Nlk>
PC3  NHezcplHfW6ldHnvckBCe3OjeR?= NEfXc3A2ODBibl2= NUnjWW94OiCq MnrQdoVxemW|c3XzJIFkfGm4YYTpc44hd2ZiU33h[FEwPS96IHHu[EBRNVOvYXSzJIxmfmWucx?= Mo\ENlI1PTJ6OEO=
LNCaP NHLScJNHfW6ldHnvckBCe3OjeR?= NHLHSJUx6oDVNUCwJI5O M{jzN|IhcA>? NGPtNZNz\X[ncoPld{Bz[XCjbYnjbY4ucW6mdXPl[EBk\WyuIHTlZZRp MVWyNlQ2Ojh6Mx?=
EOC MXHGeY5kfGmxbjDBd5NigQ>? M{G2UFExNTFyMECgcm0> NEniNnk4OiCq MYPy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSnZDDCUXAhWi2VbXHkNU82NzkEoB?= MlXJNlIzPDl2MUW=
HaCaT  NEPnSG1HfW6ldHnvckBCe3OjeR?= M1\2RVAvODBzLUGwJO69VQ>? NGTlRmczKGh? NH[2V45qdmirYnn0d{BDVVB{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGPtZYQyNzVxODD3bZRpKGGwIFnDOVDDqG:oII6wMlAxPcLizszN NFH4ZmQzOTd2MEm2Oi=>
HaCaT  M3HFUGZ2dmO2aX;uJGF{e2G7 NXzse4JjOC5yMEGtNVAh|ryP NHPPcXEzKGh? MV3pcohq[mm2czD0bIUh[WKrbHn0fUBw\iCDTFuyJJRwKHCqb4PwbI9zgWyjdHWgS3NVNVOvYXSxxsB4cXSqIHHuJGlEPTEEoH;mJFQ2yqCwTR?= MnPYNlE4PDB7Nk[=
HaCaT  Mn\CSpVv[3Srb36gRZN{[Xl? NIjiZoMxNjByMT2xNEDPxE1? MmTqNkBp M4rTc4lvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|MhfG9icHjvd5Bpd3K7bHH0[UBUdWGmMdMge4l1cCCjbjDJR|UxyqCxZjCxNFAhdk1? MnLTNlE4PDB7Nk[=
HaCaT  MVfGeY5kfGmxbjDBd5NigQ>? NXvONmpvOC5yMEGtNVAh|ryP M1:wdFIhcA>? NVq2Zmt2cW6qaXLpeJMhSUyNNDDhcoQhSUyNNTD3bZRpKEmFNUFCpJZidHWnczDv[kAxNjQEoN88UUBidmRiMD61xsDPxE1icnXzdIVkfGm4ZXz5 MnP5NlE4PDB7Nk[=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • Animal Models: Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
  • Formulation: LDN193189 is dissolved in DMSO and then diluted in water.
  • Dosages: ≤3 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 1 mg/mL (2.46 mM)
DMSO Insoluble
Water Insoluble
In vivo Add solvents to the product individually and in order:
Saline (suspension)
For best results, use promptly after mixing.
30mg/mL

* 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
Synonyms DM3189

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID