For research use only.

Catalog No.S2805 Synonyms: HTS 466284

36 publications

LY364947 Chemical Structure

CAS No. 396129-53-6

LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.

Selleck's LY364947 has been cited by 36 publications

Purity & Quality Control

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Biological Activity

Description LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
TGFβRI [1]
(Cell-free assay)
RIPK2 [2]
(Cell-free assay)
CK1δ [2]
(Cell-free assay)
(Cell-free assay)
MLK-7K [1]
(Cell-free assay)
59 nM 0.11 μM 0.22 μM 0.4 μM 1.4 μM
In vitro

LY364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I kinase with Ki of 28 nM. LY364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells. [3] LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. [4] LY364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mink Mv1Lu lung cells M2XZN2Z2dmO2aX;uJIF{e2G7 NFqz[VFKdmirYnn0bY9vKG:oIGTHSoJmfGFiUkGgbY5lfWOnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZifGmxbjDv[kBxO1SSLVz1fEBqdiCvaX7rJG13OUy3IHz1coch[2WubIOsJGlEPTB;MD6wOEDPxE1? NULFenVHOTZ3M{m0NFM>
Sf9 cells MWjGeY5kfGmxbjDhd5NigQ>? MYjJcohq[mm2aX;uJI9nKGi3bXHuJHRz[W6|Zn;ycYlv\yCpcn;3eIgh\mGldH;yJEhVT0ZrIHLleIEuOSC{ZXPldJRweiBqVEKwOGQhdXW2YYTpc44qKGG3dH;wbI9{eGixconsZZRqd25iaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNFUyKM7:TR?= MofxNVI6PTRyNEe=
Sf9 cells NHXKSYxHfW6ldHnvckBie3OjeR?= NFOxRllKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIGTHSoJmfGFiUkGg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyxiSVO1NF0xNjB3OTFOwG0> MmnwNVY2Ozl2MEO=
HepG2 cells MXTGeY5kfGmxbjDhd5NigQ>? NEjuTmhKdmirYnn0bY9vKG:oIGTHSk1j\XSjLXnu[JVk\WRiZYjwdoV{e2mxbjDv[kBRSUlvbIXjbYZmemG|ZTDy[ZBwenSncjDpckBJ\XCJMjDj[YxteyxiSVO1NF0xNjB4IN88US=> Ml\iNVQ3PDN|MkW=
NIH3T3 cells NH\kZ|hHfW6ldHnvckBie3OjeR?= NFTCdpZKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhXEeILXLleIEue3SrbYXsZZRm\CCycn;sbYZmemG2aX;uJIlvKE6LSEPUN{Bk\WyuczygTWM2OD1yLkC4NUDPxE1? NFfOTHUyPjV|OUSwNy=>
Sf9 cells M3zSd2Z2dmO2aX;uJIF{e2G7 Mn7sTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCWR1\i[ZRiKFJ{IHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NE41KM7:TR?= NYPlTZg1OTZ3M{m0NFM>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
FOXC2 / p-Smad / Smad / p-p38 / p38 / p-ATF2 / ATF2 ; 

PubMed: 26804168     

Immunoblotting for FOXC2, p- and t-Smad2/3 and p38 signaling components in LNCaP cells induced to undergo EMT using TGFβ1 (a physiological activator of p38 signaling), as well as in DU145 cells treated with LY364947, an inhibitor of TGFβ1 signaling. 


PubMed: 31387632     

Immunofluorescence of PANC-1 cells after treated with TGF-β (10 ng/mL) and/or LY364947 (10 μmol/L) for 48 h

In vivo LY364947 (1 mg/kg i.p.) accelerates lymphangiogenesis, as evidence by significantly increased the LYVE-1-positive areas, in a mouse model of chronic peritonitis. LY364947 (1 mg/kg i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. [4] LY364947 (25 mg /kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice. [5]


Kinase Assay:


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Filter-binding assay:

The IC50 of LY364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 μL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 μM pKSmad3(−3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30 °C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values.
Cell Research:


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  • Cell lines: HOXB9-MCF10A cells
  • Concentrations: 10 μM
  • Incubation Time: 24 h
  • Method:

    HOXB9-MCF10A cells were treated with 10 μM LY364947 for 24 h. Proteins were analyzed for phospho-Smad2 and total Smad2 levels

    (Only for Reference)
Animal Research:


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  • Animal Models: Tumor xenograft models with BxPC3 pancreatic adenocarcinoma cells.
  • Dosages: 1 mg/kg
  • Administration: Intraperitoneally administrated 3 times a week for 3 weeks.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL (3.67 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

* 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 272.3


CAS No. 396129-53-6
Storage powder
in solvent
Synonyms HTS 466284
Smiles C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4

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Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID