1. TGF-beta/Smad
  2. TGF-β Receptor

LY-364947 (Synonyms: HTS466284)

Cat. No.: HY-13462 Purity: 98.91%
Handling Instructions

LY-364947 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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 98 In-stock
Estimated Time of Arrival: December 31
5 mg USD 89 In-stock
Estimated Time of Arrival: December 31
10 mg USD 118 In-stock
Estimated Time of Arrival: December 31
50 mg USD 358 In-stock
Estimated Time of Arrival: December 31
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    LY-364947 purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Sep 24.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


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

    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]

    Solvent & Solubility
    In Vitro: 

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

    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.
    Kinase Assay

    The IC50 of LY-364947 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.

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

    Animal Administration

    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.

    Molecular Weight




    CAS No.




    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

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    Cat. No.: HY-13462