1. TGF-beta/Smad
  2. TGF-β Receptor
  3. LY-364947

LY-364947 (Synonyms: HTS466284)

Cat. No.: HY-13462 Purity: 99.49%
Handling Instructions

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.

For research use only. We do not sell to patients.

LY-364947 Chemical Structure

LY-364947 Chemical Structure

CAS No. : 396129-53-6

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10 mM * 1 mL in DMSO USD 98 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    LY-364947 purchased from MCE. Usage Cited in: J Cell Physiol. 2019 May;234(5):6263-6273.

    NMCFs are treated with TGF-β1 (5 ng/mL) and LY364947 (LY, 3 μM) for 6 hr. The protein levels are analyzed by western blot analysis.

    LY-364947 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2019 Nov.

    MDA-MB-231 cells are pretreated with DMSO or LY364947 (1 μM) for 1 h, and then treated with or without TGF-β1 for 6 h. Immunoblotting is done using indicated antibody.

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    Description

    LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II[1].

    IC50 & Target

    IC50: 59 nM (TGFβR-I)

    In Vitro

    LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells[1]. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours[2]. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells[3].

    In Vivo

    LY-364947 (1 mg/kg, i.p.) accelerates lymphangiogenesis, as evidence by significantly increasing the LYVE-1-positive areas in a mouse model of chronic peritonitis. LY-364947 (1 mg/kg, i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells[2]. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice[3].

    Molecular Weight

    272.30

    Formula

    C₁₇H₁₂N₄

    CAS No.

    396129-53-6

    SMILES

    C1(C2=CNN=C2C3=NC=CC=C3)=CC=NC4=CC=CC=C14

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (91.81 mM; Need ultrasonic and warming)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.6724 mL 18.3621 mL 36.7242 mL
    5 mM 0.7345 mL 3.6724 mL 7.3448 mL
    10 mM 0.3672 mL 1.8362 mL 3.6724 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1.25 mg/mL (4.59 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1.25 mg/mL (4.59 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [2]

    BALB/c nude mice 5 to 6 weeks of age are used in the assay. Parental, or VEGF-C- or TGF-β1-expressing tumor cells (5×106) in 100 μL PBS are implanted subcutaneously into male nude mice and allowed to grow for 2 to 3 weeks to reach proliferative phase, before initiation of TβR-I inhibitor administration. TβR-I inhibitor LY-364947, dissolved in 5 mg/mL in DMSO and diluted with 100 μL PBS, or the vehicle control, is injected intraperitoneally at 1 mg/kg, 3 times a week for 3 weeks. Excised samples are directly frozen in dry-iced acetone for immunohistochemistry. Frozen samples are further sectioned at 10-μm thickness in a cryostat and subsequently incubated with primary and secondary antibodies. Samples are observed using a confocal microscope.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    LY-364947HTS466284LY364947LY 364947HTS 466284HTS-466284TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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    Product Name:
    LY-364947
    Cat. No.:
    HY-13462
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