LDN-193189 2HCl

Catalog No.S7507 Synonyms: DM-3189 2HCl

For research use only.

LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

LDN-193189 2HCl Chemical Structure

CAS No. 1435934-00-1

Selleck's LDN-193189 2HCl has been cited by 78 publications

Purity & Quality Control

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Biological Activity

Description LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
Features Selective BMP type I receptor inhibitor.
Targets
ALK1 [5]
(Cell-free assay)
ALK2 [5]
(Cell-free assay)
ALK3 [5]
(Cell-free assay)
ALK6 [5]
(Cell-free assay)
0.8 nM 0.8 nM 5.3 nM 16.7 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
EOC216 NUX4UZZbS2WubDD2bYFjcWyrdImgZZN{[Xl? NWDHc3ZNOC5zLDCxMEAzNCB3LDCxNEDPxE1? M1XC[lEtKDNuIEWsJFctKDliZHH5dy=> NHy3T4lmgGirYnn0[YQh[SCmb4PlJIRmeGWwZHXueEBNTE5vaX7keYNm\CCmZXPy[YF{\SCrbjD2bYFjcWyrdIm= NEfibXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyO|g6Oyd-MkWyNlc5QTN:L3G+
PC3 MVrGeY5kfGmxbjDhd5NigQ>? NFvPSpE2ODBibl2= M2e0NWxFVi1zOUOxPFkhemWycnXzd4VlKGGldHn2ZZRqd25ib3[gV41i\DFxNT:4MEBidmRiYXzzc{Bz\XC{ZYPz[YQhWC2VbXHkN{Bt\X[nbIO= M3;tXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEWyPFg{Lz5{MkS1Nlg5OzxxYU6=
C2C12 NE\FWHNHfW6ldHnvckBie3OjeR?= MU[wMlUh|ryP M3TOW|Eh\GG7 MnjYUGRPNTF7M{G4PUBxem:vb4Tld{BugW:pZX7ld4l{ NUHNeZdxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOlg{OjJpPkK1N|Y5OzJ{PD;hQi=>
C2C12 NHfj[3pHfW6ldHnvckBie3OjeR?= NG\QWZM{OCCvaX7z NXjRNJR6UW6qaXLpeIlwdiCxZjDCUXA3NWmwZIXj[YQhSUyNMjD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gcY92e2ViQ{LDNVIh[2WubIOg[ZhxemW|c3nu[{BDWkVvTIXjJIFnfGW{IEOwJI1qdnNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC5yMUSg{txONg>? M3nL[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkK3PVQ3Lz5|MEKyO|k1PjxxYU6=
BT-12 NEf5eXlyUFSVIHHzd4F6 NV;aSmJHeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells NGjrS3dyUFSVIHHzd4F6 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 NIjQV4NyUFSVIHHzd4F6 Ml;PdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? M36y[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
C2C12 NVvyZnNjTnWwY4Tpc44h[XO|YYm= MlPjNE4yKHWP M3rOUWlvcGmkaYTpc44hd2ZiQVzLOUBqdiCvb4Xz[UBEOkNzMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBVT0[kZYThNU1qdmS3Y3XkJHNu[WRzL{WgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC3TTDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MlnjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzMEOwNlUoRjJ6MUCzNFI2RC:jPh?=
Assay
Methods Test Index PMID
Western blot pSmad ; Smad / ID1 / PARP / Cleaved PARP 19029982 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 (from reference)

Animal Research:

[1]

  • Animal Models: Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
  • Dosages: ≤3 mg/kg
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 479.4
Formula

C25H24Cl2N6

CAS No. 1435934-00-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3.Cl.Cl

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Tech Support

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