LY2109761

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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5 Customer Reviews

  • 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.

    C. TGF-β/smad pathway inhibitor LY2109761 suppressed 5-FU-induced EMT. Magnification, ×40; scale bar = 100 μm. D. LY2109761 inhibited nucleus entrance of smad2 and slug's expression in 5-FU-induced EMT.

    Oncotarget, 2016, 7(18):25478-92. 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.

    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

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.
Targets
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  NVnaZnQ{TnWwY4Tpc44hSXO|YYm= MXexNOKh|ryPwrC= NWfVd|ZXOiCq NEXHV5JqdmirYnn0d{BifXSxcHjh[5khcW6mdXP0bY9vKGK7IHfhcIFv\2mw MXyyOVI3QDB2Nh?=
PC-3 NY\DT2hXTnWwY4Tpc44hSXO|YYm= MUKwMlIwOi92IN88US=> M3:wRVI1KGh? MYrEUXNQ MkjpbY5pcWKrdIOgWGdHNc7{MfMAl4lv\HWlZXSgV41i\DJiYXP0bZZifGmxbh?= NHj2dogzOjF5M{C1Ny=>
PMOs M4rmOGZ2dmO2aX;uJGF{e2G7 NV74NnpTOC5{L{KvOEDPxE1? MkPJNlQhcA>? M2mxbWROW09? M2\PTolvcGmkaYTzJHRITi4QskJihLNqdmS3Y3XkJHNu[WR{IHHjeIl3[XSrb36= MnXVNlIyPzNyNUO=
PC-3 NEfzUItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NID5dpcxNjJxMjFOwG0> MmDiNlQhcA>? MY\EUXNQ M3Tvc4Jtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> M2r2U|IzOTd|MEWz
PMOs NF\NVnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DjdFAvOi9{IN88US=> M3fDdFI1KGh? MWHEUXNQ NHj5eFFjdG:la4OgeIhmKGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJJBzd2S3Y3XkJIJ6KFSJRj5OtlE> MnLkNlIyPzNyNUO=
U87MG NVezWot3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKxOU8yOCEQvF2= NIKzUZEzKGh? NETRWmpmdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 NHjEdZYzOjByNkm5PC=>
T98 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3qRZlnPS9zMDFOwG0> M1TWflIhcA>? M2TnRoVvcGGwY3XzJJJi\Gmxc3Xud4l1cX[rdIm= NES5dXEzOjByNkm5PC=>
U87MG MVnBdI9xfG:|aYOgRZN{[Xl? MXuxNEDPxE1? M3\WUFIhcA>? NWftdHk{\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQhTE6DIHThcYFo\SCjbnSgZZBweHSxc3nzJJJifGW| MVqyNlAxPjl7OB?=
NMA-23 M3zrVWFxd3C2b4Ppd{BCe3OjeR?= NGXyeWwyOCEQvF2= NVfaXW5JOiCq MVrlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDEUmEh\GGvYXflJIFv\CCjcH;weI9{cXNicnH0[ZM> MUeyNlAxPjl7OB?=
HLE  NIrmNIVHfW6ldHnvckBCe3OjeR?= NXKyd2YzOC5yMT2xNFDDqG6P MUK0PEBp MUjpcohq[mm2czD0bIUhdWmpcnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXm2UJBUOjB6NES4O|g>
HLF MkPLSpVv[3Srb36gRZN{[Xl? NYDXSHVOOC5yMT2xNFDDqG6P NGPxR4s1QCCq NWK1O2h[cW6qaXLpeJMhfGinIH3p[5JifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MmLwNlA5PDR6N{i=
10A/HER2YVMA NFLUVYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVKwMlEuOC53IN88US=> MVi5JIQ> NYHqbZpvemWmdXPld{B1cGVic3n6[UwhcW64YYPpeoVv\XO|IHHu[EBk\WyuIH71cYJmeiCxZjDjc4xwdmmncx?= NV6zWYFxOjB|OEOxPVc>
MC38  MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjkSFk2KM7:TR?= MVu1JIQ> NVX1S205cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NYnFT2FFOTl7MEm3OFQ>
U937 NEeyZZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jVW|UuOjBizszN MYeyOE04OiCq MlnubY5pcWKrdIOgZ4VtdCCpcn;3eIghe2yrZ3j0cJk> MnvZNVg1QTJzMUO=
HLE  MXjDfZRwfG:6aYT5JGF{e2G7 M{S4RVAvODBzLUKwJO69VQ>? MXW0PEBp MV7pcoR2[2W|IHPlcIwh[3m2b4TvfIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkLJNVg{OTh2NEO=
HLF NUL5empQS3m2b4TvfIl1gSCDc4PhfS=> NILFOVcxNjByMT2yNEDPxE1? M3LUPVQ5KGh? M4XhTYlv\HWlZYOgZ4VtdCCleYTveI95cXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NUT4N2RsOTh|MUi0OFM>

... 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]

Protocol

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 individually and in order:
0.5% CMC+0.25% Tween 80
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
Formula

C26H27N5O2

CAS No. 700874-71-1
Storage powder
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