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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4 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.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

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 NGHvb4VMcW6jc3WgRZN{[Xl? MXvpcohq[mm2czD0bIUhc2mwYYPlJIFkfGm4aYT5JI9nKEGOS{SgZY5lKEGldGLJTWEhf2m2aDDJR|UxyqC4YXz1[ZMhd2ZiMUCxJIFv\CB{MUCgco0tKHKnc4DlZ5RqfmWueR?= NEnsVHozPTN4OEOyNi=>
EOC216 NVLacJJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmwMlEuOTBizszN NFToO24zNTFyIHS= NF3pUHFFVVOR MYfpcoR2[2ViY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NUXCTIxxOjV{Mke4PVM>
OVAC429 NGfndFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKyM|Uh|ryP M{DSVlQ5KGh? MUXEUXNQ MkPL[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= NI\ocZMzPTJ{N{i5Ny=>
SKOV3 M4i1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jJfVIwPSEQvF2= M2LMT|Q5KGh? M{S4SWROW09? Mlmw[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= M4j6[VI2OjJ5OEmz
OVCA429 NETQTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M376UVIwPSEQvF2= NXvkNmw6PDhiaB?= M{nQWmROW09? NHzJXFNl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz NFnIVlYzPTJ{N{i5Ny=>
EOC219 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvCNk82KM7:TR?= MWC0PEBp NHHIOZRFVVOR MUfk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| NX7VeYgzOjV{Mke4PVM>
A549 NYnWbI1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfqSWMxNjVvMU[g{txO NXv5ZotkTE2VTx?= NHe0Oo5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUOxVHYxOjR5N{iwNVE>
BEAS-2B  MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnSe|cxNjVvMU[g{txO NIfobIZFVVOR MkLrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlnBNlQ4PzhyMUG=
hBMSCs NFPVSGRHfW6ldHnvckBCe3OjeR?= M{LtRlAvOsLizszN M{fSVFch\A>? M33qR4Fjd2yrc3jld{B1cGVic3nsbYJqdmmwLYDyc41wfGWmIFHMVEBi[3Srdnn0feKheGG{dHz5 MYiyOFA4PjF6Nx?=
PANC-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3wOU02ODBibl2= NWLMbFR6PDhiaB?= NX21c2tkcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mnj1NlM6Pjl5Mkm=
MIA PaCa-2 NXP6OZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nselUuPTByIH7N NYTROXZFPDhiaB?= MoLpbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnqxNlM6Pjl5Mkm=
Bx-PC3 MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDHOU02ODBibl2= M36xe|Q5KGh? NHHCW5RqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1vXNlI{QTZ7N{K5
PC3  MXvGeY5kfGmxbjDBd5NigQ>? NGfiTVA2ODBibl2= NEfyOmEzKGh? NXXYZlJnemWycnXzd4V{KGGldHn2ZZRqd25ib3[gV41i\DFxNT:4JIFv\CCSLWPtZYQ{KGyndnXsdy=> NHTXN3MzOjR3Mki4Ny=>
LNCaP NUj3WHVETnWwY4Tpc44hSXO|YYm= MkPPNQKBmzVyMDDuUS=> MX[yJIg> M2TCVJJmfmW{c3XzJJJieGGveXPpck1qdmS3Y3XkJINmdGxiZHXheIg> MWiyNlQ2Ojh6Mx?=
EOC MlToSpVv[3Srb36gRZN{[Xl? MX:xNE0yODByIH7N M1rIb|czKGh? Mor6doVlfWOnczD0bIUheGixc4Doc5J6dGG2ZXSgRm1RKFJvU33h[FEwPS96wrC= NWLCU4c1OjJ{NEm0NVU>
HaCaT  MmLRSpVv[3Srb36gRZN{[Xl? NWrTW4tQOC5yMEGtNVAh|ryP NGjZNokzKGh? MoPSbY5pcWKrdIOgRm1ROi2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCVbXHkNU82Nzhid3n0bEBidiCLQ{WwxsBw\iC-MD6wNFXDqM7:TR?= M4HMXVIyPzRyOU[2
HaCaT  NFfjNpBHfW6ldHnvckBCe3OjeR?= M1HGNVAvODBzLUGwJO69VQ>? MYGyJIg> NGfScGRqdmirYnn0d{B1cGViYXLpcIl1gSCxZjDBUGszKHSxIIDoc5NxcG:{eXzheIUhT1OWLWPtZYQyyqC5aYToJIFvKEmFNUFCpI9nKDR3wrDuUS=> M3S5c|IyPzRyOU[2
HaCaT  NWjT[lB7TnWwY4Tpc44hSXO|YYm= MlexNE4xODFvMUCg{txO M4fkcFIhcA>? NXjzXo5rcW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOyC2bzDwbI9{eGixconsZZRmKFOvYXSxxsB4cXSqIHHuJGlEPTEEoH;mJFExOCCwTR?= M1\MVFIyPzRyOU[2
HaCaT  MYHGeY5kfGmxbjDBd5NigQ>? NYrQSFcxOC5yMEGtNVAh|ryP MWWyJIg> MnvJbY5pcWKrdIOgRWxMPCCjbnSgRWxMPSC5aYToJGlEPTEEoI\hcJVmeyCxZjCwMlPDqM7:TTDhcoQhOC53wrFOwG0hemW|cHXjeIl3\Wy7 NGrGPVczOTd2MEm2Oi=>

... 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 warmed (2.46 mM)
DMSO slightly soluble or insoluble
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
Saline (suspension)
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
in solvent
Synonyms DM3189

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID