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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USD 370 In stock

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3 Customer Reviews

  • 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.

    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.

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

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  NFO1ZVNHfW6ldHnvckBCe3OjeR?= M4\EWVExyqEQvF5CpC=> Mni2NkBp NXfufGdJcW6qaXLpeJMh[XW2b4DoZYd6KGmwZIXjeIlwdiCkeTDnZYxidmerbh?= MXWyOVI3QDB2Nh?=
PC-3 MoTaSpVv[3Srb36gRZN{[Xl? NXX6bJB4OC5{L{KvOEDPxE1? MkHXNlQhcA>? M2DSRmROW09? NFHqfoRqdmirYnn0d{BVT0ZvzsKx5qCUcW6mdXPl[EBUdWGmMjDhZ5RqfmG2aX;u M2\2NlIzOTd|MEWz
PMOs NVjyXWJDTnWwY4Tpc44hSXO|YYm= NXHsbFQ3OC5{L{KvOEDPxE1? NEfBSlgzPCCq MWDEUXNQ NFrEN2FqdmirYnn0d{BVT0ZvzsKx5qCUcW6mdXPl[EBUdWGmMjDhZ5RqfmG2aX;u NG[zVIwzOjF5M{C1Ny=>
PC-3 MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C4UlAvOi9{IN88US=> Ml;nNlQhcA>? M{fONWROW09? Ml\sZoxw[2u|IITo[UBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDwdo9lfWOnZDDifUBVT0ZvzsKx NF[4TYMzOjF5M{C1Ny=>
PMOs NFnTfFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInPVGUxNjJxMjFOwG0> M4L2VFI1KGh? NGXYNVdFVVOR M2Cwe4Jtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> NYDE[|kzOjJzN{OwOVM>
U87MG M3z4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;BWnlbPS9zMDFOwG0> NVf1Tm14OiCq NX;OWFh5\W6qYX7j[ZMhemGmaX;z[Y5{cXSrdnn0fS=> Mk[3NlIxODZ7OUi=
T98 NEDhU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIL6No02NzFyIN88US=> NH7aOpkzKGh? NF3FXlJmdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 NVy1bGo6OjJyME[5PVg>
U87MG NUPzRmoxSXCxcITvd4l{KEG|c3H5 NXPHW2x[OTBizszN NVnEUHVbOiCq MXPlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> M1HNXFIzODB4OUm4
NMA-23 MX7BdI9xfG:|aYOgRZN{[Xl? MVSxNEDPxE1? NF65TpQzKGh? M1TjeoVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCmYX3h[4Uh[W6mIHHwc5B1d3OrczDyZZRmew>? M3TZUlIzODB4OUm4
HLE  MYXGeY5kfGmxbjDBd5NigQ>? NUW0cmtbOC5yMT2xNFDDqG6P Mmi5OFghcA>? MmjRbY5pcWKrdIOgeIhmKG2rZ4LheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF3jVlEzODh2NEi3PC=>
HLF M1\PUmZ2dmO2aX;uJGF{e2G7 M4DnblAvODFvMUCwxsBvVQ>? M3r6XVQ5KGh? NIjNOGpqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NF3GUG8zODh2NEi3PC=>
10A/HER2YVMA NWXHW2QyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6wMlEuOC53IN88US=> NGS2VIo6KGR? MmHzdoVlfWOnczD0bIUhe2m8ZTygbY53[XOrdnXu[ZN{KGGwZDDj[YxtKG63bXLldkBw\iClb3zvcolmew>? NEKwcIUzODN6M{G5Oy=>
MC38  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3KOUDPxE1? NXnQ[YU1PSCm NHmxWHlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? NVnaeZF6OTl7MEm3OFQ>
U937 M2fkbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlraOU0zOCEQvF2= NYfIdYlXOjRvN{KgbC=> MUTpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MY[xPFQ6OjFzMx?=
HLE  NYPxU3FPS3m2b4TvfIl1gSCDc4PhfS=> M3;hOVAvODBzLUKwJO69VQ>? MmDjOFghcA>? MWXpcoR2[2W|IHPlcIwh[3m2b4TvfIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHiwdJYyQDNzOES0Ny=>
HLF MXjDfZRwfG:6aYT5JGF{e2G7 NUPPc2EyOC5yMEGtNlAh|ryP MoTkOFghcA>? NYr5W4k6cW6mdXPld{Bk\WyuIHP5eI91d3irdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MXexPFMyQDR2Mx?=

... Click to View More Cell Line Experimental Data

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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% CMC+0.25% Tween 80 16 mg/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.

Chemical Information

Molecular Weight 441.52


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID