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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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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Notes:

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.
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  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]

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 <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
Formula

C26H27N5O2

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