Catalog No.S2704

LY2109761 Chemical Structure

Molecular Weight(MW): 441.52

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.

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Cited by 17 Publications

5 Customer Reviews

  • The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.

    Invest Ophthalmol Vis Sci 2014 55(3), 1770-9. LY2109761 purchased from Selleck.

  • validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,

    Toxicology 2014 326C, 9-17. LY2109761 purchased from Selleck.

  • PLoS One 2013 8(12), e83521. LY2109761 purchased from Selleck.

  • C, Western blot analysis of serum cultured GB2 cells treated with each 20 μm inhibitor. The representative Western blot is shown for each protein and the bar charts represent the quantified values (mean ± s.d.) of three replicates. The fold changes were normalized by the relative densities regarding α-Tubulin.

    Mol Cell Proteomics, 2016, 15(3):1017-31. LY2109761 purchased from Selleck.

  • The expression of p‐AKT after TGFβ1 or LY2109761 treatment on vector‐ and ADAMTS9‐transfected BT549 and SK‐BR‐3 cells.

    J Cell Mol Med, 2018, 22(2):1257-1271. LY2109761 purchased from Selleck.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2.
TβRI [1]
(Cell-free assay)
TβRII [1]
(Cell-free assay)
38 nM(Ki) 300 nM(Ki)
In vitro

LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when combined with gemcitabine in combination index value of 0.36581. Blocking TβRI/II kinase activity with LY2109761 (5 μM) completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, significantly enhances the detachment-induced apoptosis by 26% at 8 hours treatment, and completely suppresses TGF-β–induced Smad2 phosphorylation. [1] LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. [2] LY2109761 pretreatment enhances radiosensitivity of glioblastoma cells via TGF-β signaling blockage. LY2109761 (10 μM) reduces the self-renewal and proliferation of GBM-derived cancer stem–like cells (CSLC), which can be significantly enhanced when combined with radiation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2  MYLGeY5kfGmxbjDBd5NigQ>? M3;IcFExyqEQvF5CpC=> MnG0NkBp NF3RbFVqdmirYnn0d{BifXSxcHjh[5khcW6mdXP0bY9vKGK7IHfhcIFv\2mw M3LFVVI2OjZ6MES2
PC-3 NF\YTXZHfW6ldHnvckBCe3OjeR?= NWrBUFhnOC5{L{KvOEDPxE1? MlizNlQhcA>? NYS4[5FxTE2VTx?= NH3wTZNqdmirYnn0d{BVT0ZvzsKx5qCUcW6mdXPl[EBUdWGmMjDhZ5RqfmG2aX;u M{HxRVIzOTd|MEWz
PMOs MlS4SpVv[3Srb36gRZN{[Xl? NW\Zb3pFOC5{L{KvOEDPxE1? MluxNlQhcA>? Mn35SG1UVw>? NV;pXpBmcW6qaXLpeJMhXEeILd8yNgKBm2mwZIXj[YQhW22jZEKgZYN1cX[jdHnvci=> NELUeY8zOjF5M{C1Ny=>
PC-3 MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHWxclUxNjJxMjFOwG0> MliwNlQhcA>? MYfEUXNQ M{XUUIJtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> MkLYNlIyPzNyNUO=
PMOs MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvkfVFoOC5{L{Kg{txO M4j2blI1KGh? NEnTXo5FVVOR NXW0RYts[myxY3vzJJRp\SCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBxem:mdXPl[EBjgSCWR1[t{tIy MmrENlIyPzNyNUO=
U87MG MkjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkGzOU8yOCEQvF2= NFftbYQzKGh? NEHaRYNmdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 MX2yNlAxPjl7OB?=
T98 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XmUlUwOTBizszN NEfTdI8zKGh? NIm0NFFmdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 NYDxbo9bOjJyME[5PVg>
NMA-23 M4Do[GFxd3C2b4Ppd{BCe3OjeR?= M{WwSlExKM7:TR?= Mn;TNkBp M2\lO4VvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCmYX3h[4Uh[W6mIHHwc5B1d3OrczDyZZRmew>? MmHONlIxODZ7OUi=
HLE  MVLGeY5kfGmxbjDBd5NigQ>? NEPC[|cxNjBzLUGwNOKhdk1? NFPmN5A1QCCq NFzHeXRqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NWTtVoN6OjB6NES4O|g>
HLF MWjGeY5kfGmxbjDBd5NigQ>? NY\GXpVlOC5yMT2xNFDDqG6P NXXLdFVoPDhiaB?= M1rPXIlvcGmkaYTzJJRp\SCvaXfyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVWyNFg1PDh5OB?=
10A/HER2YVMA MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PEclAvOS1yLkWg{txO NHj3TnQ6KGR? M4PkXZJm\HWlZYOgeIhmKHOrenWsJIlvfmG|aY\lcoV{eyCjbnSgZ4VtdCCwdX3i[ZIhd2ZiY3;sc45q\XN? NYniVppTOjB|OEOxPVc>
MC38  M1;5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LFXFUh|ryP M2Dk[|Uh\A>? NFfNVodqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? NWH0OlRMOTl7MEm3OFQ>
U937 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7SOU0zOCEQvF2= MYiyOE04OiCq M2\sUolvcGmkaYTzJINmdGxiZ4Lve5RpKHOuaXfoeIx6 M2r3fVE5PDl{MUGz
HLE  MmHrR5l1d3SxeHn0fUBCe3OjeR?= M1fUWVAvODBzLUKwJO69VQ>? MlrzOFghcA>? Mnq0bY5lfWOnczDj[YxtKGO7dH;0c5hqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFLDSpkyQDNzOES0Ny=>
HLF NUTQeZJuS3m2b4TvfIl1gSCDc4PhfS=> M3[4[lAvODBzLUKwJO69VQ>? M1K4dFQ5KGh? MkG5bY5lfWOnczDj[YxtKGO7dH;0c5hqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1LLd|E5OzF6NESz

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-Smad2 / Smad ; 

PubMed: 29416682     

The expression of p-Smad-2 was down regulated by LY2109761 at the dose ranging from 0.1 to 100 μM.


PubMed: 29416682     

The migration-related protein E-cadherin was signifcantly promoted by LY2109761 in a dose dependent manner, ranging from 1 to 100 μM/L.

β-catenin / MMP-9 / MMP-2 / nm23 / uPA / COX-2 ; 

PubMed: 19909744     

Protein lysates from livers of control mice and LY2109761-treated mice were analyzed by western blotting as indicated. β-actin was used as loading control. NS: non-specific band.

CDK2 / CDK4 / Cyclin D1 / p-Rb ; 

PubMed: 19909744     

Protein lysates from livers of control mice and LY2109761-treated mice were analyzed by western blotting as indicated. β-actin was used as loading control. NS: non-specific band.

29416682 19909744
In vivo Administration of LY2109761 (50 mg/kg) alone or in combination with gemcitabine (25 mg/kg) significantly reduces the tumor volume by ~70% and ~90%, respectively, prolongs the survival with the median survival duration of 45.0 days and 77.5 days, respectively, and reduces spontaneous abdominal metastases in the L3.6pl/GLT Xenograft mice model. [1] In consistent with the in vitro effect, administration of LY2109761 alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively, decreases tumor invasion and tumor microvessel density, and significantly enhances radiation-induced tumor growth delay in the U87MG xenograft mice model. [3]


Cell Research:[1]
+ Expand
  • Cell lines: Colo357FG/GLT, and Colo357L3.6pl/GLT
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 48 hours
  • Method: Cells are exposed to increasing doses of LY2109761 (~10 μM) for 48 hours. The medium containing drugs is removed, the cells are washed twice with PBS, and fresh medium is added. After 5 days of incubation, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay is used to obtain relative variable cell numbers.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Athymic nude mice with orthotopic implantation of L3.6pl/GLT cells
  • Formulation: Dissolved in the SX-1292 oral vehicle containing 1% sodium carboxymethylcellulose, 0.5% sodium lauryl sulfate, and 0.05% antifoam
  • Dosages: 50 mg/kg
  • Administration: Twice a day p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (4.52 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC+0.25% Tween 80
For best results, use promptly after mixing.
16 mg/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 441.52


CAS No. 700874-71-1
Storage powder
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID