LDN-193189 2HCl

For research use only.

Catalog No.S7507 Synonyms: DM-3189 2HCl

47 publications

LDN-193189 2HCl Chemical Structure

CAS No. 1435934-00-1

LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.

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Selleck's LDN-193189 2HCl has been cited by 47 publications

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Biological Activity

Description LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.
Features Selective BMP type I receptor inhibitor.
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
EOC216 NIjRUGdE\WyuII\pZYJqdGm2eTDhd5NigQ>? MkLXNE4yNCBzLDCyMEA2NCBzMDFOwG0> MXOxMEA{NCB3LDC3MEA6KGSjeYO= NYXqXGNo\XiqaXLpeIVlKGFiZH;z[UBl\XCnbnTlcpQhVESQLXnu[JVk\WRiZHXjdoVie2ViaX6geoli[mmuaYT5 M4[2elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkK3PFk{Lz5{NUKyO|g6OzxxYU6=
PC3 M3TQZmZ2dmO2aX;uJIF{e2G7 Mk\TOVAxKG6P M4PZPGxFVi1zOUOxPFkhemWycnXzd4VlKGGldHn2ZZRqd25ib3[gV41i\DFxNT:4MEBidmRiYXzzc{Bz\XC{ZYPz[YQhWC2VbXHkN{Bt\X[nbIO= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR3Mki4N{c,OjJ2NUK4PFM9N2F-
C2C12 MWrGeY5kfGmxbjDhd5NigQ>? NVzEVG1ZOC53IN88US=> MorZNUBl[Xl? MoLrUGRPNTF7M{G4PUBxem:vb4Tld{BugW:pZX7ld4l{ MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NkizNlIoRjJ3M{[4N|IzRC:jPh?=
C2C12 M{jlV2Z2dmO2aX;uJIF{e2G7 NEXQN5Y{OCCvaX7z MVfJcohq[mm2aX;uJI9nKEKPUE[tbY5lfWOnZDDBUGszKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCvb4Xz[UBEOkNzMjDj[YxteyCneIDy[ZN{cW6pIFLSSU1NfWNiYX\0[ZIhOzBibXnud{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTCwMlAyPCEQvF2u MmroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{Mke5OFYoRjNyMkK3PVQ3RC:jPh?=
BT-12 MkC2dWhVWyCjc4PhfS=> Mnu5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells NYT0SWUzeUiWUzDhd5NigQ>? M1vkcZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| NI\qPVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh30 NELiU4pyUFSVIHHzd4F6 MnnkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? M4rndVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
C2C12 Ml;YSpVv[3Srb36gZZN{[Xl? MVKwMlEhfU1? M33CS2lvcGmkaYTpc44hd2ZiQVzLOUBqdiCvb4Xz[UBEOkNzMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBVT0[kZYThNU1qdmS3Y3XkJHNu[WRzL{WgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC3TTDifUBY\XO2ZYLuJIJtd3RibXX0bI9l M3\qWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUCzNFI2Lz5{OEGwN|AzPTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pSmad ; 

PubMed: 19029982     


Immunoblot of PASMCs treated with LDN-193189 showing differential inhibition of BMP4 (10 ng/ml) or TGF-β (0.5 ng/ml) signaling (IC50 ~ 5 nM and ≥ 1 μM, respectively).

Smad / ID1 / PARP / Cleaved PARP ; 

PubMed: 31098401     


Western blot analysis of time- and concentration-dependent effects on downstream signalling in response to LDN-193189 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.

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

Animal Research:[1]
- Collapse
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro Water 52 mg/mL (108.46 mM)
DMSO Insoluble
Ethanol 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 479.4
Formula

C25H24Cl2N6

CAS No. 1435934-00-1
Storage powder
in solvent
Synonyms DM-3189 2HCl
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID