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

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.

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CAS No. : 396129-53-6

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10 mM * 1 mL in DMSO
ready for reconstitution
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고객리뷰

Based on 24 publication(s) in Google Scholar

LY-364947 Related Antibodies

Top Publications Citing Use of Products

    LY-364947 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94.  [Abstract]

    Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI protein levels in the UM‑Chor1 cell line.

    LY-364947 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94.  [Abstract]

    Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI mRNA levels in the UM‑Chor1 cell line.

    LY-364947 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94.  [Abstract]

    Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h attenuated the invasiveness of UM‑Chor1 cells.

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

    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 MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Jan 29;522(1):270-277.  [Abstract]

    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.

    View All TGF-β Receptor Isoform Specific Products:

    View All Isoforms
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP GDF15

    • Biological Activity

    • Protocol

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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)
    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    60 nM
    Compound: HTS-466284
    Inhibition of TGF-beta-induced expression of PAI-luciferase reporter in HepG2 cells
    Inhibition of TGF-beta-induced expression of PAI-luciferase reporter in HepG2 cells
    		[PMID: 14643325]
    NIH3T3 IC50
    0.081 μM
    Compound: LY-364947
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    		[PMID: 18314943]
    NIH3T3 IC50
    0.081 μM
    Compound: LY-364947
    Inhibitory activity against TGF-beta-stimulated proliferation in NIH3T3 cells
    Inhibitory activity against TGF-beta-stimulated proliferation in NIH3T3 cells
    		[PMID: 16539403]
    Sf9 IC50
    0.051 μM
    Compound: 1
    Inhibition of human Transforming growth factor (TGF) beta-1 receptor (T204D mutation) autophosphorylation in Sf9 cells
    Inhibition of human Transforming growth factor (TGF) beta-1 receptor (T204D mutation) autophosphorylation in Sf9 cells
    		[PMID: 12954047]
    Sf9 IC50
    0.059 μM
    Compound: LY-364947
    Inhibition of recombinant human TGFbeta R1 expressed in Sf9 cells
    Inhibition of recombinant human TGFbeta R1 expressed in Sf9 cells
    		[PMID: 16539403]
    Sf9 IC50
    0.059 μM
    Compound: LY-364947
    Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
    Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
    		[PMID: 18314943]
    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].

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

    LY-364947 Related Antibodies
    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].

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

    272.30

    화학식

    C17H12N4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    보관
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    용액&용해도
    In Vitro: 

    DMSO : 15.62 mg/mL (57.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 몰농도 계산기

    • 농도 희석 계산기

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서

    Purity: 99.23%

    SDS (624 KB)

    COA (257 KB) HNMR (293 KB) RP-HPLC (246 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.6724 mL 18.3621 mL 36.7242 mL 91.8105 mL
    5 mM 0.7345 mL 3.6724 mL 7.3448 mL 18.3621 mL
    10 mM 0.3672 mL 1.8362 mL 3.6724 mL 9.1811 mL
    15 mM 0.2448 mL 1.2241 mL 2.4483 mL 6.1207 mL
    20 mM 0.1836 mL 0.9181 mL 1.8362 mL 4.5905 mL
    25 mM 0.1469 mL 0.7345 mL 1.4690 mL 3.6724 mL
    30 mM 0.1224 mL 0.6121 mL 1.2241 mL 3.0604 mL
    40 mM 0.0918 mL 0.4591 mL 0.9181 mL 2.2953 mL
    50 mM 0.0734 mL 0.3672 mL 0.7345 mL 1.8362 mL
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    LY-364947 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    LY-364947396129-53-6HTS466284LY364947LY 364947HTS 466284HTS-466284TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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    상품명:
    LY-364947
    Cat. No.:
    HY-13462
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    SAFETY DATA SHEET (SDS)

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