LY364947

Catalog No.S2805 Synonyms: HTS 466284

LY364947 Chemical Structure

Molecular Weight(MW): 272.3

LY364947 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.

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3 Customer Reviews

  • The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.

    Chem Biol Interact 2014 217, 1-8. LY364947 purchased from Selleck.

    Suppression of phosphorylated (p-)SMAD family member 2 (Smad2) signaling by LY364947 reverses the inductive effect of jumonji AT-rich interactive domain 1B (JARID1B) on the expression of glioma cancer stem cell-related markers. The expression of transforming growth factor-β1 (TGF-β1), p-Smad2, Smad2, CD133, octamer-binding transcription factor 4 (Oct4), nestin and BMI1 proto-oncogene, polycomb ring finger (Bmi-1) protein levels in LY364947-exposed U251-pBabe-JARID1B and its control cells were measured by western blot analysis. β-actin was used as the internal control for western blot analysis.

    Int J Mol Med, 2016, 38(1):172-82. LY364947 purchased from Selleck.

  • HCECs were treated with TGF-β1 (10 ng/ml) alone, or in combination with LY364947 (2μM) for 3days. The protein expression of p16 and p21 in HCECs induced by TGF-β1.

    Aging (Albany NY), 2016, 8(10):2337-2354.. LY364947 purchased from Selleck.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description LY364947 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.
Targets
TGFβRI [1]
(Cell-free assay)
RIPK2 [2]
(Cell-free assay)
CK1δ [2]
(Cell-free assay)
TGFβRII [1]
(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 NG\F[WlHfW6ldHnvckBie3OjeR?= MW\Jcohq[mm2aX;uJI9nKFSJRnLleIEhWjFiaX7keYNm\CC2cnHud4NzcXC2aX;uZYwh[WO2aY\heIlwdiCxZjDwN3RRNUy3eDDpckBucW6tIF32NWx2KGy3bnegZ4VtdHNuIFnDOVA:OC5yNDFOwG0> MnXhNVY2Ozl2MEO=
Sf9 cells M1jZNGZ2dmO2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHRz[W6|Zn;ycYlv\yCpcn;3eIgh\mGldH;yJEhVT0ZrIHLleIEuOSC{ZXPldJRweiBqVEKwOGQhdXW2YYTpc44qKGG3dH;wbI9{eGixconsZZRqd25iaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNFUyKM7:TR?= Mn74NVI6PTRyNEe=
Sf9 cells M3;GdWZ2dmO2aX;uJIF{e2G7 NW\UW3JJUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDUS2Zj\XSjIGKxJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:OC5yNUmg{txO M2\YdlE3PTN7NECz
HepG2 cells MXXGeY5kfGmxbjDhd5NigQ>? MoO2TY5pcWKrdHnvckBw\iCWR1[tZoV1[S2rbnT1Z4VlKGW6cILld5Nqd25ib3[gVGFKNWy3Y3nm[ZJie2VicnXwc5J1\XJiaX6gTIVxTzJiY3XscJMtKEmFNUC9NE4xPiEQvF2= MVexOFY1OzN{NR?=
NIH3T3 cells NHu4bZpHfW6ldHnvckBie3OjeR?= M4DRcWlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBVT0ZvYnX0ZU1{fGmvdXzheIVlKHC{b3zp[oVz[XSrb36gbY4hVkmKM2SzJINmdGy|LDDJR|UxRTBwMEixJO69VQ>? NHHJcIIyPjV|OUSwNy=>
Sf9 cells NVrvN29FTnWwY4Tpc44h[XO|YYm= MnPaTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCWR1\i[ZRiKFJ{IHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NE41KM7:TR?= NX\2b41IOTZ3M{m0NFM>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:

[3]

+ Expand

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:

[6]

+ Expand
  • 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:

[4]

+ Expand
  • Animal Models: Tumor xenograft models with BxPC3 pancreatic adenocarcinoma cells.
  • Formulation: Dissolved in 5 mg/mL in DMSO and diluted with 100 μL PBS
  • 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 individually and in order:
4% DMSO+30% PEG 300+ddH2O
0.75mg/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 272.3
Formula

C17H12N4

CAS No. 396129-53-6
Storage powder
Synonyms HTS 466284

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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