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

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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 M4fad2tqdmG|ZTDBd5NigQ>? M2PJOIlvcGmkaYTzJJRp\SCtaX7hd4Uh[WO2aY\peJkhd2ZiQVzLOEBidmRiQXP0VmlKSSC5aYToJGlEPTEEoI\hcJVmeyCxZjCxNFEh[W6mIEKxNEBvdSxicnXzdIVkfGm4ZXz5 MlT5NlU{Pjh|MkK=
EOC216 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH23N5ExNjFvMUCg{txO MofyNk0yOCCm NULEU5BXTE2VTx?= NVjVZ5lrcW6mdXPlJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFuwUG8zPTJ{N{i5Ny=>
OVAC429 Mo\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[3NlIwPSEQvF2= NFru[oU1QCCq MnnNSG1UVw>? NF[zOZll\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz Mo\nNlUzOjd6OUO=
SKOV3 Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jwbVIwPSEQvF2= MXm0PEBp NHf3SJhFVVOR MWPk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| MVqyOVIzPzh7Mx?=
OVCA429 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPkRlBtOi93IN88US=> MnzjOFghcA>? NYjjWWE3TE2VTx?= MV7k[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| M{S1OlI2OjJ5OEmz
EOC219 NXTQfVF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDoR3EzNzVizszN MWO0PEBp NGf3Z2VFVVOR M2q2TYRm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= NF;IZ2UzPTJ{N{i5Ny=>
A549 NFvhXoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViwMlUuOTZizszN MnLvSG1UVw>? MoPvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXeyOFc4QDBzMR?=
BEAS-2B  M2ruUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PUS|AvPS1zNjFOwG0> NEDae45FVVOR NHHLcmpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVj4S402OjR5N{iwNVE>
hBMSCs M1jMPGZ2dmO2aX;uJGF{e2G7 NWewc3ZlOC5{wrFOwG0> MX[3JIQ> NYfnV2Rl[WKxbHnzbIV{KHSqZTDzbYxq[mmwaX6tdJJwdW:2ZXSgRWxRKGGldHn2bZR6yqCyYYL0cJk> MXqyOFA4PjF6Nx?=
PANC-1 M2rpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrJUXpQPS13MECgcm0> NULqcpIyPDhiaB?= MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGTmSHIzOzl4OUeyPS=>
MIA PaCa-2 M2fwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDCNFJZPS13MECgcm0> MXG0PEBp MnK3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3rqcVI{QTZ7N{K5
Bx-PC3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnmdG9WPS13MECgcm0> MVy0PEBp NUHVfJlpcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVWyN|k3QTd{OR?=
PC3  MUHGeY5kfGmxbjDBd5NigQ>? MmjxOVAxKG6P MnnhNkBp M3fMWJJmeHKnc4Pld{Bi[3SrdnH0bY9vKG:oIGPtZYQyNzVxODDhcoQhWC2VbXHkN{Bt\X[nbIO= MmrCNlI1PTJ6OEO=
LNCaP MUXGeY5kfGmxbjDBd5NigQ>? MUWw5qCUPTByIH7N NYDO[4t6OiCq NXu4cFdremW4ZYLz[ZMhemGyYX35Z4lvNWmwZIXj[YQh[2WubDDk[YF1cA>? MXWyNlQ2Ojh6Mx?=
EOC NV\RXG9vTnWwY4Tpc44hSXO|YYm= MnPnNVAuOTByMDDuUS=> MkP6O|IhcA>? MXPy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSnZDDCUXAhWi2VbXHkNU82NzkEoB?= NVjNSWFlOjJ{NEm0NVU>
HaCaT  NUO0SGc2TnWwY4Tpc44hSXO|YYm= MlPaNE4xODFvMUCg{txO NITaS5IzKGh? NIHRSZpqdmirYnn0d{BDVVB{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGPtZYQyNzVxODD3bZRpKGGwIFnDOVDDqG:oII6wMlAxPcLizszN Mlz6NlE4PDB7Nk[=
HaCaT  MknySpVv[3Srb36gRZN{[Xl? MnTBNE4xODFvMUCg{txO MkD0NkBp NXHEfnhUcW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOiC2bzDwbI9{eGixconsZZRmKEeVVD3TcYFlOcLid3n0bEBidiCLQ{WwxsBw\iB2NdMgcm0> MnHsNlE4PDB7Nk[=
HaCaT  NGPlR4JHfW6ldHnvckBCe3OjeR?= NUe4c2JLOC5yMEGtNVAh|ryP NWrNV3JpOiCq NXvuc41ZcW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOyC2bzDwbI9{eGixconsZZRmKFOvYXSxxsB4cXSqIHHuJGlEPTEEoH;mJFExOCCwTR?= MojjNlE4PDB7Nk[=
HaCaT  MYnGeY5kfGmxbjDBd5NigQ>? M1\QTFAvODBzLUGwJO69VQ>? MljGNkBp NH23N4ZqdmirYnn0d{BCVEt2IHHu[EBCVEt3IIfpeIghUUN3MNMgeoFtfWW|IH;mJFAvO8LizszNJIFv\CByLkZCpO69VSC{ZYPw[YN1cX[nbIm= NWS5fVN[OjF5NEC5OlY>

... 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 <1 mg/mL
Water <1 mg/mL
In vivo Saline (suspension) 30mg/mL

* 1 mg/ml means slightly soluble or 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID