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 71 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 M1TaRmNmdGxidnnhZoltcXS7IHHzd4F6 Mln3NE4yNCBzLDCyMEA2NCBzMDFOwG0> M1TqeFEtKDNuIEWsJFctKDliZHH5dy=> Ml3a[ZhpcWKrdHXkJIEh\G:|ZTDk[ZBmdmSnboSgUGRPNWmwZIXj[YQh\GWlcnXhd4UhcW5idnnhZoltcXS7 NWjrbGRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNlc5QTNpPkK1NlI4QDl|PD;hQi=>
PC3 NXTXU|BjTnWwY4Tpc44h[XO|YYm= NWjTTos5PTByIH7N NILBZmpNTE5vMUmzNVg6KHKncILld5Nm\CCjY4TpeoF1cW:wIH;mJHNu[WRzL{WvPEwh[W6mIHHsd48hemWycnXzd4VlKFBvU33h[FMhdGW4ZXzz MoW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2NUK4PFMoRjJ{NEWyPFg{RC:jPh?=
C2C12 MX;GeY5kfGmxbjDhd5NigQ>? MlnqNE42KM7:TR?= NULufHA{OSCmYYm= NY\DTmdiVESQLUG5N|E5QSCycn;tc5RmeyCveX;n[Y5me2m| NFvhNZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO2PFMzOid-MkWzOlg{OjJ:L3G+
C2C12 MUfGeY5kfGmxbjDhd5NigQ>? NGDmPJI{OCCvaX7z NY[0U2dvUW6qaXLpeIlwdiCxZjDCUXA3NWmwZIXj[YQhSUyNMjD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gcY92e2ViQ{LDNVIh[2WubIOg[ZhxemW|c3nu[{BDWkVvTIXjJIFnfGW{IEOwJI1qdnNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC5yMUSg{txONg>? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ{N{m0Okc,OzB{Mke5OFY9N2F-
BT-12 NVLhUGNPeUiWUzDhd5NigQ>? NYTzT4N5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz Mln4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
fibroblast cells MlrKdWhVWyCjc4PhfS=> MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MYjxTHRUKGG|c3H5 NH7CfFNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnizNEBk\Wyucx?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
C2C12 MmLNSpVv[3Srb36gZZN{[Xl? M3jpVVAvOSC3TR?= Ml3qTY5pcWKrdHnvckBw\iCDTFu1JIlvKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJHRITmKndHGxMYlv\HWlZXSgV41i\DFxNTDwbI9{eGixconsZZRqd25iYYSgNE4yKHWPIHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MoDJQIEhfGG{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.
  • (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 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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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