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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Cited by 56 Publications

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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 NHnHdHVMcW6jc3WgRZN{[Xl? NXHhNFFxcW6qaXLpeJMhfGinIHvpcoF{\SCjY4Tpeol1gSCxZjDBUGs1KGGwZDDBZ5RTUUmDIIfpeIghUUN3MNMgeoFtfWW|IH;mJFExOSCjbnSgNlExKG6vLDDy[ZNx\WO2aY\lcJk> MUiyOVM3QDN{Mh?=
EOC216 NWK4boN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnWXWRlOC5zLUGwJO69VQ>? NUDWdVVtOi1zMDDk NHTpUlNFVVOR MXfpcoR2[2ViY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnT5NlUzOjd6OUO=
OVAC429 NVvnS3ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\teGozNzVizszN MXe0PEBp NEHRTY1FVVOR Mm\p[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= NELRSnUzPTJ{N{i5Ny=>
SKOV3 M{Lhe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHmNk82KM7:TR?= MmXaOFghcA>? NHHvTpNFVVOR M3PKc4Rm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= NV\ufHBHOjV{Mke4PVM>
OVCA429 NYrWV20{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nyWlIwPSEQvF2= NIjjNlc1QCCq NGnLV2FFVVOR NIf4N5ll\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz M3vrR|I2OjJ5OEmz
EOC219 MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUWyPVJjOi93IN88US=> NEjvVGQ1QCCq NYjSNHhVTE2VTx?= NIOxZmxl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz NGOwO44zPTJ{N{i5Ny=>
A549 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\hRlQ4OC53LUG2JO69VQ>? NFPVWGNFVVOR Mo\MbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3[3clI1Pzd6MEGx
BEAS-2B  NFiyTG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\Bb|AvPS1zNjFOwG0> MVfEUXNQ M{Cyd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M37u[FI1Pzd6MEGx
hBMSCs M3;l[2Z2dmO2aX;uJGF{e2G7 M1\sU|AvOsLizszN MXu3JIQ> M1fhS4Fjd2yrc3jld{B1cGVic3nsbYJqdmmwLYDyc41wfGWmIFHMVEBi[3Srdnn0feKheGG{dHz5 MoHtNlQxPzZzOEe=
PANC-1 M1;YZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUK1MVUxOCCwTR?= MoXxOFghcA>? NEPkN|VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF7SXXgzOzl4OUeyPS=>
MIA PaCa-2 M3TsVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H0WlUuPTByIH7N MW[0PEBp MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX:yN|k3QTd{OR?=
Bx-PC3 NHrtV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXsOU02ODBibl2= MUe0PEBp NV24VY1VcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mn;FNlM6Pjl5Mkm=
PC3  MX3GeY5kfGmxbjDBd5NigQ>? NGfmN2o2ODBibl2= M2TPXlIhcA>? NYHpdWg3emWycnXzd4V{KGGldHn2ZZRqd25ib3[gV41i\DFxNT:4JIFv\CCSLWPtZYQ{KGyndnXsdy=> MXiyNlQ2Ojh6Mx?=
LNCaP MmHHSpVv[3Srb36gRZN{[Xl? MkjMNQKBmzVyMDDuUS=> MnzpNkBp MV7y[ZZmenOnczDyZZBidXmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo NEnQO28zOjR3Mki4Ny=>
EOC M3viT2Z2dmO2aX;uJGF{e2G7 MVyxNE0yODByIH7N M2fsNVczKGh? MXny[YR2[2W|IITo[UBxcG:|cHjvdplt[XSnZDDCUXAhWi2VbXHkNU82NzkEoB?= MmDkNlIzPDl2MUW=
HaCaT  MUXGeY5kfGmxbjDBd5NigQ>? M33zSlAvODBzLUGwJO69VQ>? NGLucJczKGh? M1fXOYlvcGmkaYTzJGJOWDJvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiU33h[FEwPS96IIfpeIgh[W5iSVO1NOKhd2ZifkCuNFA2yqEQvF2= NIH4[5YzOTd2MEm2Oi=>
HaCaT  NXe1V|ZlTnWwY4Tpc44hSXO|YYm= M1TOc|AvODBzLUGwJO69VQ>? MmnENkBp NYf5R5ZjcW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOiC2bzDwbI9{eGixconsZZRmKEeVVD3TcYFlOcLid3n0bEBidiCLQ{WwxsBw\iB2NdMgcm0> MVOyNVc1ODl4Nh?=
HaCaT  MVfGeY5kfGmxbjDBd5NigQ>? NVvERnU6OC5yMEGtNVAh|ryP NYD6e48{OiCq NHn1O3RqdmirYnn0d{B1cGViYXLpcIl1gSCxZjDBUGs{KHSxIIDoc5NxcG:{eXzheIUhW22jZEJCpJdqfGhiYX6gTWM2OMLib3[gNVAxKG6P NHW0eXczOTd2MEm2Oi=>
HaCaT  MUfGeY5kfGmxbjDBd5NigQ>? M4XmbFAvODBzLUGwJO69VQ>? Mn;XNkBp M{DMVYlvcGmkaYTzJGFNUzRiYX7kJGFNUzVid3n0bEBKSzVywrD2ZYx2\XNib3[gNE4{yqEQvF2gZY5lKDBwNdMg{txOKHKnc4DlZ5RqfmWueR?= MXiyNVc1ODl4Nh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pSMAD1 / pSMAD5 / pSMAD8 / SMAD1 / SMAD5 / SMAD8 / ID1 / SMAD4 / PARP / Cleaved PARP; 

PubMed: 31098401     


In vitro molecular pharmacology of LDN-193189 and LDN-214117. Western blot analysis of time- and concentration-dependent effects on downstream signalling in response to a LDN-193189 and b LDN-214117 in DIPG cells. Increasing concentrations (0–10 µM) at 4 and 8 h are shown for SU-DIPG-VI, HSJD-DIPG-IV and HSJD-DIPG-007. GAPDH is the loading control.

31098401
Immunofluorescence
Tbx18 / Hcn4; 

PubMed: 30906456     


Representative immunofluorescence microscopy images of epicardial progenitor cells from the four groups with staining for Hcn4 (red). The nuclei were counterstained with DAPI (blue) and the YFP expressed by the cells is apparent (scale bar, 50 µm). (Tbx18 was conjugated to YFP).

30906456
Growth inhibition assay
Cell viability; 

PubMed: 31098401     


Screening of ALK2 inhibitors in vitro. Concentration-response curves for eight ALK2 inhibitors tested against three ACVR1 mutant cell cultures (HSJD-DIPG-007 (R206H), SU-DIPG-IV (G328V), HSJD-DIPG-018 (R258G), purple) and two wild-type cultures (SU-DIPG-VI, QCTB-R059, grey). a Pyrazolo[1,5-a]pyrimidines—dorsomorphin, LDN-193189, DMH1, LDN-212854. b Pyridines—K02288, LDN-214117, LDN-213844, LDN-213819. Concentration of compound is plotted on a log scale (x-axis) against cell viability (y-axis). Mean plus standard deviation are plotted from at least n = 3 experiments.

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

Animal Research:[1]
- Collapse
  • 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 DMSO Insoluble
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms DM3189

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID