LY2109761

For research use only.

Catalog No.S2704

57 publications

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. LY2109761 blocks autophagy and induces apoptosis.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 432 In stock
USD 270 In stock
USD 370 In stock
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Selleck's LY2109761 has been cited by 57 publications

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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. LY2109761 blocks autophagy and induces apoptosis.
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  NVTzdIpDTnWwY4Tpc44hSXO|YYm= MXexNOKh|ryPwrC= MXyyJIg> NXXORlhDcW6qaXLpeJMh[XW2b4DoZYd6KGmwZIXjeIlwdiCkeTDnZYxidmerbh?= MXWyOVI3QDB2Nh?=
PC-3 M2LYN2Z2dmO2aX;uJGF{e2G7 NIfQZWoxNjJxMj:0JO69VQ>? MYKyOEBp NXG2WJhJTE2VTx?= NVq0[XlkcW6qaXLpeJMhXEeILd8yNgKBm2mwZIXj[YQhW22jZEKgZYN1cX[jdHnvci=> MYWyNlE4OzB3Mx?=
PMOs NED6d29HfW6ldHnvckBCe3OjeR?= M{LYe|AvOi9{L{Sg{txO NG\jSWMzPCCq M17KW2ROW09? NVHWTWVscW6qaXLpeJMhXEeILd8yNgKBm2mwZIXj[YQhW22jZEKgZYN1cX[jdHnvci=> MWKyNlE4OzB3Mx?=
PC-3 NWS5c|NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\BT|AvOi9{IN88US=> NWXDRVhiOjRiaB?= M3i1d2ROW09? M3\vRYJtd2OtczD0bIUhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gdJJw\HWlZXSgZpkhXEeILd8yNS=> MnW5NlIyPzNyNUO=
PMOs NYXpdGdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\UTYVFOC5{L{Kg{txO NUOzRno6OjRiaB?= MUfEUXNQ NFnKb3RjdG:la4OgeIhmKGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJJBzd2S3Y3XkJIJ6KFSJRj5OtlE> NEntOoozOjF5M{C1Ny=>
U87MG MljnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrmd3A{PS9zMDFOwG0> NXfH[5dKOiCq NH7JR|RmdmijbnPld{Bz[WSrb4PlcpNqfGm4aYT5 Mn;ENlIxODZ7OUi=
T98 MnLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTEOU8yOCEQvF2= M3ruXlIhcA>? Monl[Y5p[W6lZYOgdoFlcW:|ZX7zbZRqfmm2eR?= M2\UflIzODB4OUm4
U87MG NHjWT4pCeG:ydH;zbZMhSXO|YYm= MnzaNVAh|ryP MmD6NkBp M3rySIVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJGRPSSCmYX3h[4Uh[W6mIHHwc5B1d3OrczDyZZRmew>? MnK1NlIxODZ7OUi=
NMA-23 M3;LWGFxd3C2b4Ppd{BCe3OjeR?= NVvwbYFuOTBizszN NILLem4zKGh? MlvD[Y5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgSG5CKGSjbXHn[UBidmRiYYDvdJRwe2m|IILheIV{ NGm3UpQzOjByNkm5PC=>
HLE  NVTTZ|JPTnWwY4Tpc44hSXO|YYm= MoKwNE4xOS1zMEFCpI5O M4HYXFQ5KGh? M3zp[IlvcGmkaYTzJJRp\SCvaXfyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MkHLNlA5PDR6N{i=
HLF MoXwSpVv[3Srb36gRZN{[Xl? M{[wNFAvODFvMUCwxsBvVQ>? Mk\SOFghcA>? NGPJ[ZBqdmirYnn0d{B1cGVibXnndoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M33rUlIxQDR2OEe4
10A/HER2YVMA MnW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;DNE4yNTBwNTFOwG0> MYm5JIQ> NWj0PVl5emWmdXPld{B1cGVic3n6[UwhcW64YYPpeoVv\XO|IHHu[EBk\WyuIH71cYJmeiCxZjDjc4xwdmmncx?= MVKyNFM5OzF7Nx?=
MC38  M1vLPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDnXFNFPSEQvF2= NVfaSWtqPSCm MV3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MVmxPVkxQTd2NB?=
U937 NVLyTWNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:zOU0zOCEQvF2= MXeyOE04OiCq MYDpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MVWxPFQ6OjFzMx?=
HLE  NGLWV3FEgXSxdH;4bZR6KEG|c3H5 M{XJXFAvODBzLUKwJO69VQ>? NWjRbVVsPDhiaB?= MmnJbY5lfWOnczDj[YxtKGO7dH;0c5hqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{T6XlE5OzF6NESz
HLF M4HLSmN6fG:2b4jpeJkhSXO|YYm= M1e4VlAvODBzLUKwJO69VQ>? M2\QT|Q5KGh? M{[2dYlv\HWlZYOgZ4VtdCCleYTveI95cXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3HCTFE5OzF6NESz

... Click to View More Cell Line Experimental Data

Assay
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.

E-cadherin; 

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]

Protocol

Cell Research:[1]
- Collapse
  • 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]
- Collapse
  • Animal Models: Athymic nude mice with orthotopic implantation of L3.6pl/GLT cells
  • 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
Formula

C26H27N5O2

CAS No. 700874-71-1
Storage powder
in solvent
Synonyms N/A
Smiles C1C[N]2N=C(C3=NC=CC=C3)C(=C2C1)C4=CC=NC5=C4C=CC(=C5)OCCN6CCOCC6

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID