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 70 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 NILIbppMcW6jc3WgRZN{[Xl? MnzsbY5pcWKrdIOgeIhmKGurbnHz[UBi[3Srdnn0fUBw\iCDTFu0JIFv\CCDY4TSTWlCKHerdHigTWM2OMLidnHseYV{KG:oIEGwNUBidmRiMkGwJI5uNCC{ZYPw[YN1cX[nbIm= NI\3XYgzPTN4OEOyNi=>
EOC216 MorhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX3NE4yNTFyIN88US=> NV3sUotYOi1zMDDk NF;pZpZFVVOR NVjVZ2pncW6mdXPlJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFnKWXozPTJ{N{i5Ny=>
OVAC429 NUHrbXhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HoSlIwPSEQvF2= Mny4OFghcA>? M4TBV2ROW09? MYDk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| NWLT[pQ3OjV{Mke4PVM>
SKOV3 NGP3PHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkKwNk82KM7:TR?= MYS0PEBp MmmxSG1UVw>? NWfkbYh4\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MUCyOVIzPzh7Mx?=
OVCA429 MlTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWToZZZSOi93IN88US=> M1fGVFQ5KGh? NInTNpJFVVOR Mmfz[IVkemWjc3XzJJRp\SCyZYLj[Y51[WenIH;mJINmdGy|IHnuJHMheGijcx?= NV\mbIZQOjV{Mke4PVM>
EOC219 NVTZeZJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i4[FIwPSEQvF2= M13tW|Q5KGh? NYrwWJF4TE2VTx?= MWfk[YNz\WG|ZYOgeIhmKHCncnPlcpRi\2Vib3[gZ4VtdHNiaX6gV{BxcGG| MoLTNlUzOjd6OUO=
A549 NWXxcnBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MViwMlUuOTZizszN NHG0VWpFVVOR Mki5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUGyOFc4QDBzMR?=
BEAS-2B  MnvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:wMlUuOTZizszN MlXQSG1UVw>? NGnUOY5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmXSNlQ4PzhyMUG=
hBMSCs M1fmTGZ2dmO2aX;uJGF{e2G7 NUWw[2JwOC5{wrFOwG0> NG\QXFM4KGR? NUnBclFF[WKxbHnzbIV{KHSqZTDzbYxq[mmwaX6tdJJwdW:2ZXSgRWxRKGGldHn2bZR6yqCyYYL0cJk> M1j4TlI1ODd4MUi3
PANC-1 NV3JPVVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1mzPVUuPTByIH7N MoewOFghcA>? MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXzTcmFUOjN7Nkm3Nlk>
MIA PaCa-2 MmDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:1MVUxOCCwTR?= NHHL[3M1QCCq NGnLS5pqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3;i[VI{QTZ7N{K5
Bx-PC3 M37MTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO1MVUxOCCwTR?= MnnGOFghcA>? NXn4RpNLcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MkT1NlM6Pjl5Mkm=
PC3  M1f1XmZ2dmO2aX;uJGF{e2G7 Mm[4OVAxKG6P MWeyJIg> MnX4doVxemW|c3XzJIFkfGm4YYTpc44hd2ZiU33h[FEwPS96IHHu[EBRNVOvYXSzJIxmfmWucx?= NYHRdFg3OjJ2NUK4PFM>
LNCaP M2rLTWZ2dmO2aX;uJGF{e2G7 NXTEOIc{OOLCk{WwNEBvVQ>? NF\NdJozKGh? MlSwdoV3\XK|ZYOgdoFx[W27Y3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> MX:yNlQ2Ojh6Mx?=
EOC Mn3NSpVv[3Srb36gRZN{[Xl? MWmxNE0yODByIH7N MUS3NkBp NHf5WXdz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTl[EBDVVBiUj3TcYFlOS93L{lCpC=> MWKyNlI1QTRzNR?=
HaCaT  NEjh[|JHfW6ldHnvckBCe3OjeR?= M1jrR|AvODBzLUGwJO69VQ>? MYCyJIg> NVPycJRRcW6qaXLpeJMhSk2SMj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTcYFlOS93L{ige4l1cCCjbjDJR|UxyqCxZjD+NE4xODYEoN88US=> MVWyNVc1ODl4Nh?=
HaCaT  MnHlSpVv[3Srb36gRZN{[Xl? MXWwMlAxOS1zMDFOwG0> NUTmbmM1OiCq NYOzN21LcW6qaXLpeJMhfGinIHHibYxqfHlib3[gRWxMOiC2bzDwbI9{eGixconsZZRmKEeVVD3TcYFlOcLid3n0bEBidiCLQ{WwxsBw\iB2NdMgcm0> NHLT[pgzOTd2MEm2Oi=>
HaCaT  MkPjSpVv[3Srb36gRZN{[Xl? MoPPNE4xODFvMUCg{txO MXWyJIg> M1:1ZYlvcGmkaYTzJJRp\SCjYnnsbZR6KG:oIFHMT|MhfG9icHjvd5Bpd3K7bHH0[UBUdWGmMdMge4l1cCCjbjDJR|UxyqCxZjCxNFAhdk1? MWqyNVc1ODl4Nh?=
HaCaT  NHr4dndHfW6ldHnvckBCe3OjeR?= M17QXFAvODBzLUGwJO69VQ>? Mm\mNkBp M3LiOolvcGmkaYTzJGFNUzRiYX7kJGFNUzVid3n0bEBKSzVywrD2ZYx2\XNib3[gNE4{yqEQvF2gZY5lKDBwNdMg{txOKHKnc4DlZ5RqfmWueR?= MW[yNVc1ODl4Nh?=

... 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