LDN-193189 化学構造
分子量: 406.48



Quality Control & MSDS


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  • 研究分野



製品説明 LDN-193189は、ALK2ALK3の選択的な阻害剤で、IC50がそれぞれ5 nMと30 nMです。
ターゲット ALK2 ALK3
IC50 5 nM [1] 30 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
C2C12 MnPvT4lv[XOnIFHzd4F6 M3jwdolvcGmkaYTzJJRp\SCtaX7hd4Uh[WO2aY\peJkhd2ZiQVzLOEBidmRiQXP0VmlKSSC5aYToJGlEPTEEoI\hcJVmeyCxZjCxNFEh[W6mIEKxNEBvdSxicnXzdIVkfGm4ZXz5 Mkm3NlU{Pjh|MkK=
EOC216 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj4fplxOC5zLUGwJO69VQ>? NUG0dXlrOi1zMDDk MoDESG1UVw>? M4fHTIlv\HWlZTDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NVH5UG9jOjV{Mke4PVM>
OVAC429 M2f1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXywdpFUOi93IN88US=> NWTQdWppPDhiaB?= MVzEUXNQ M2PBU4Rm[3KnYYPld{B1cGVicHXyZ4VvfGGpZTDv[kBk\WyuczDpckBUKHCqYYO= NH3PXYQzPTJ{N{i5Ny=>
SKOV3 MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:yWlIwPSEQvF2= MX60PEBp NHvDSVhFVVOR NGHvSJBl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz NWT1bZlIOjV{Mke4PVM>
OVCA429 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nzWFIwPSEQvF2= NIP6S3Q1QCCq M17wNWROW09? NWrsSIht\GWlcnXhd4V{KHSqZTDw[ZJk\W62YXflJI9nKGOnbHzzJIlvKFNicHjhdy=> MYiyOVIzPzh7Mx?=
EOC219 NFHod2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;kNk82KM7:TR?= NGjPXGw1QCCq NEP2OWFFVVOR NHHDWIdl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubIOgbY4hWyCyaHHz Ml;0NlUzOjd6OUO=
A549 NYLmWJpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDWT4dnOC53LUG2JO69VQ>? M{nq[mROW09? M3nTU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mly3NlQ4PzhyMUG=
BEAS-2B  MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjjNE42NTF4IN88US=> MkPmSG1UVw>? NUnFfINbcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4jBOlI1Pzd6MEGx
hBMSCs M1zBUWZ2dmO2aX;uJGF{e2G7 MlfPNE4zyqEQvF2= MWO3JIQ> M4f1cYFjd2yrc3jld{B1cGVic3nsbYJqdmmwLYDyc41wfGWmIFHMVEBi[3Srdnn0feKheGG{dHz5 MX[yOFA4PjF6Nx?=
PANC-1 NHexd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHRdG1NPS13MECgcm0> NX\meXZEPDhiaB?= M4LhU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4H4XFI{QTZ7N{K5
MIA PaCa-2 NUT0TVJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLJUm1KPS13MECgcm0> NHzKems1QCCq M3PIUIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M33tUFI{QTZ7N{K5
Bx-PC3 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7p[4pqPS13MECgcm0> MXu0PEBp MmnXbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1nqclI{QTZ7N{K5
PC3  NHTjOI9HfW6ldHnvckBCe3OjeR?= Mk[zOVAxKG6P MkfoNkBp MUTy[ZBz\XO|ZYOgZYN1cX[jdHnvckBw\iCVbXHkNU82NzhiYX7kJHAuW22jZEOgcIV3\Wy| M3i1[FIzPDV{OEiz
LNCaP NF;S[VdHfW6ldHnvckBCe3OjeR?= M1qzZlDjiJN3MECgcm0> MX[yJIg> MXry[ZZmenOnczDyZZBidXmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo NVHBPHNyOjJ2NUK4PFM>
EOC NYDYXWhKTnWwY4Tpc44hSXO|YYm= NELLUnIyOC1zMECwJI5O NGL4eVA4OiCq NWr2Snl6emWmdXPld{B1cGVicHjvd5Bpd3K7bHH0[YQhSk2SIGKtV41i\DFxNT:4xsA> MU[yNlI1QTRzNR?=
HaCaT  NH6wV3ZHfW6ldHnvckBCe3OjeR?= NGjOfncxNjByMT2xNEDPxE1? NEO0OVMzKGh? M4i4VIlvcGmkaYTzJGJOWDJvaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiU33h[FEwPS96IIfpeIgh[W5iSVO1NOKhd2ZifkCuNFA2yqEQvF2= NHnt[5IzOTd2MEm2Oi=>
HaCaT  NHruNmtHfW6ldHnvckBCe3OjeR?= MonENE4xODFvMUCg{txO M1XQW|IhcA>? NInUNldqdmirYnn0d{B1cGViYXLpcIl1gSCxZjDBUGszKHSxIIDoc5NxcG:{eXzheIUhT1OWLWPtZYQyyqC5aYToJIFvKEmFNUFCpI9nKDR3wrDuUS=> NWm0PZBwOjF5NEC5OlY>
HaCaT  NFjCTGlHfW6ldHnvckBCe3OjeR?= MUCwMlAxOS1zMDFOwG0> M1HnR|IhcA>? MmfrbY5pcWKrdIOgeIhmKGGkaXzpeJkhd2ZiQVzLN{B1dyCyaH;zdIhwenmuYYTlJHNu[WRzwrD3bZRpKGGwIFnDOVDDqG:oIEGwNEBvVQ>? M4f4W|IyPzRyOU[2

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Alkaline phosphatase activity C2C12 cells are seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. The wells are treated in quadruplicate with BMP ligands and LDN-193189 or vehicle. The cells are collected after 6 days in culture in 50 μL Tris-buffered saline and 1% Triton X-100. The lysates are added to p-nitro-phenylphosphate reagent in 96-well plates for 1 hours and then evaluated alkaline phosphatase activity (absorbance at 405 nm). Cell viability and quantity are measured by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements.

動物実験: [1]

動物モデル Ad.Cre on P7 is injected into conditional caALK2–transgenic and wild-type mice.
製剤 LDN193189 is dissolved in DMSO and then diluted in water.
投薬量 ≤3 mg/kg
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download LDN-193189 SDF
分子量 406.48


CAS No. 1062368-24-4
保管 2年-20℃
6月-80℃in solvent
別名 DM3189
溶解度 (25°C) * In vitro DMSO <1 mg/mL (<1 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo Saline (suspension) 30mg/mL
* <1 mg/ml means slightly soluble or 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.
化学名 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

カスタマーフィードバック (3)

Click to enlarge
Source , , J Cell Sci, 2013, 126: 234-43. LDN-193189 purchased from Selleck
Method Western Blot
Cell Lines Primary rib chondrocytes
Concentrations 100/200 nM
Incubation Time 24 h
Results LDN-193189 can partially reverse the increased phospho-Smad1/5 expression in Jab1flox/flox, Col2a1-Cre mutant chondrocytes in a dose-dependent manner.

Click to enlarge
Source Int J Cancer, 2014, 136(5):E455-69. LDN-193189 purchased from Selleck
Method Immunocytochemistry
Cell Lines OVCA429 cells
Concentrations 2, 5 uM
Incubation Time 6 h
Results Initiation of cell death at an early time point (6 hr) was confirmed by treating OVCA429 cells with the cell permeable viability dye AO and EB that is only able to pass membranes of dead or dying cells. A statistically significant difference in the percent of cells staining positively was observed with 10 mM LDN.

Click to enlarge
Source Dev Biol, 2014, 378:107-121. LDN-193189 purchased from Selleck
Method Immunocytochemistry and in situ hybridization
Cell Lines Zebrafish
Concentrations 2 uM
Incubation Time 24 h
Results The distribution and number of Pax7-expressing cells at 24 h was different between controls and sulf1 morphants, which we quantified at the 15th somite at 24 hpf. When treated with LDN, there was obviously decreasd expressing of Pax7,comparing with controls.

文献中の引用 (11)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID