2. TGF-beta/Smad Autophagy
  3. TGF-β Receptor Autophagy
  4. LY2109761

LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.

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CAS 番号 : 700874-71-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 在庫あり
Solution
10 mM * 1 mL in DMSO USD 88 在庫あり
Solid
5 mg $80 在庫あり
10 mg $140 在庫あり
50 mg $430 在庫あり
100 mg $650 在庫あり
200 mg $950 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

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カスタマーレビュー

Based on 68 publication(s) in Google Scholar

Other Forms of LY2109761:

LY2109761 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    LY2109761 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836.  [Abstract]

    LY2109761 at 100 nM, 10 μM, or 50 μM is added for 30 min to block TGFβR1/2 prior to TGF-β1-treatment, then proteins are collected, and the levels of Sphk2, fibronectin, and α-SMA are detected by Western blotting.

    LY2109761 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2018 Nov:103:173-181.  [Abstract]

    TRPM7 mRNA and protein expressions are effectively suppressed by LY2109761 and SIS3 in ASMCs compared with those in 10 ng/mL TGF-β1-stimulated cells.

    LY2109761 purchased from MedChemExpress. Usage Cited in: Cell Biol Int. 2017 Sep;41(9):960-968.  [Abstract]

    The phosphorylation level of Smad2 is significantly inhibited by LY2109761. The M2 macrophage-induced increase of α-SMA and decrease of E-cadherin and CK-18 are inhibited by LY2109761.

    LY2109761 purchased from MedChemExpress. Usage Cited in: J Hepatol. 2015 Oct;63(4):863-73.  [Abstract]

    Blocking the TGF-beta and ERK signalling effectively inhibits EDIL3 mediated angiogenesis and invasion. Western blotting analysis of the expression of p-ERK and p-Smad2 in DMSO- and VX-11e or LY2109761-treated HuH7-p-lenti-EDIL3 cells. GAPDH is used as a loading control.

    LY2109761 purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2015 Jun;35(6):1667-74.  [Abstract]

    Inhibition of the TGF-β1/Smad2 pathway decreases H2O2-induced human umbilical vein endothelial cell (HUVEC) apoptosis, but not oxidative stress. Western blot analysis is performed to determine protein expression in the HUVECs in the control, model, AST Ⅳ and LY2109761 groups.

    TGF-β Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

    • 生物活性

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    • 純度とドキュメンテーション

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    製品説明

    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.

    IC50 & Target

    Ki: 38 nM (TβRI), 300 nM (TβRII)
    Cellular Effect
    Cell Line Type Value Description References
    Calu-6 EC50
    0.236 3
    Compound: 15d
    Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
    Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
    		[PMID: 18314943]
    Calu-6 EC50
    0.236 3
    Compound: 15d
    Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
    Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
    		[PMID: 18314943]
    NIH3T3 IC50
    0.21 3
    Compound: 15d
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    		[PMID: 18314943]
    NIH3T3 IC50
    0.21 3
    Compound: 15d
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    		[PMID: 18314943]
    Sf9 IC50
    0.069 3
    Compound: 15d
    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]
    Calu-6 EC50
    0.236 3
    Compound: 15d
    Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
    Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
    		[PMID: 18314943]
    NIH3T3 IC50
    0.21 3
    Compound: 15d
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
    		[PMID: 18314943]
    Sf9 IC50
    0.069 3
    Compound: 15d
    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]
    体外実験

    LY2109761 significantly inhibits the growth of L3.6pl/GLT soft agar colonies in a dose-dependent manner, and results in appr 33% inhibition at 2 μM and 73% inhibition at 20 μM. Targeting TβRI/II kinase activity with LY2109761 (5 μM) almost completely suppresses both the basal and TGF-β1-stimulated migration of L3.6pl/GLT cells[1].
    LY2109761 induces a dose-dependent reduction in phosphorylation of Smad-2. HLE endogenous phosphorylation of Smad-2 is inhibited by LY2109761. LY2109761 blocks migration on different ECM proteins and invasion of both HLE and HLF through a 3-dimensional structure. LY2109761 increases E-cadherin mRNA expression after 24 hours and protein levels after 48 hours[2].
    LY2109761 pretreatment reduces clonogenic survival in cell cultures of U87MG and T98 following radiation, resulting in an increase in the radiosensitivity with a DEF0.1 of 1.30 and 1.37, respectively[3].

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

    LY2109761 関連抗体
    体内実験

    LY2109761 (50 mg/kg, p.o.) greatly reduces the tumor volume and increases the median survival duration of the mice to 45.0 days. The mice treated with LY2109761 develop significantly fewer metastatic lesions and, in some of them, no metastatic lesion, as indicated by the GFP signal, can be identified in the abdomen[1].
    LY2109761 enhances radiation-induced tumor growth delay in a U87MG subcutaneous xenograft tumor model in BALB/c nude mice. LY2109761 increases survival in an orthotopical CSLC glioblastoma model and enhanced antitumor activity of radiation[2].

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

    441.52

    分子式

    C26H27N5O2
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    N12N=C(C(C3=C4C=CC(OCCN5CCOCC5)=CC4=NC=C3)=C1CCC2)C6=NC=CC=C6
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 6.67 mg/mL (15.11 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 2.2649 mL 11.3245 mL 22.6490 mL
    5 mM 0.4530 mL 2.2649 mL 4.5298 mL
    10 mM 0.2265 mL 1.1325 mL 2.2649 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  0.5% CMC-Na/0.5% Tween-80 in Saline water

      Solubility: 1 mg/mL (2.26 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    純度とドキュメンテーション

    純度: 99.72%

    COA (250 KB) HNMR (150 KB) LCMS (102 KB) Elemental Analysis Report (108 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    L3.6pl/GLT cells are washed twice with cold PBS and lysed at 4°C into RIPA buffer (50 mM Tris HCl [pH 8], 150 mM NaCl, 1% NP-40, 0.5% sodium deoxycolate, and 0.1% SDS). Tumor and liver specimens are homogenized into RIPA buffer with an electric homogenizer and then maintained in constant agitation for two hours at 4°C. The lysates are cleared by centrifugation. Each lysate (20 µg of protein) is separated by 8% SDS-PAGE and probed with polyclonal rabbit antibodies against total ERK1/2, TβRI, and TβRII or with monoclonal mouse antibodies against phosphorylated Smad2, total Smad2, phosphorylated ERK1/2, and phosphorylated and total JNK. Immunoreactive proteins are visualized with Lumi-Light Western blotting substrate according to the manufacturer's instructions. phosphorylated Smad2/Smad2 band density ratios are calculated using the ImageQuant software.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Fifty mice are randomLy allocated into five groups (n=5 mice per group) to receive p.o. vehicle for 50 μL of LY2109761 or 50 mg/kg LY2109761 twice a day p.o. On day 0, mice are anesthetized with 1.5% isofluorane-air mixture, a small left abdominal flank incision is created, and the spleen is carefully exteriorized. L3.6pl/GLT or C5LM2/GLT cells (1.0×105 cells/50 μL of HBSS), cultured in the presence of LY2109761 (5 μM) or DMSO from day −5 to day 0, are inoculated into the spleen with a 30-gauge needle. A visible paling of the spleen is the criterion for successful inoculation. After 10 min, the spleen is removed using a high-temperature cautery to avoid the possibility that the ectopic growth of pancreatic tumor cells in the spleen could be a confounding source of hematogenous liver metastatic cells. The abdominal wall is closed in one layer with wound clips. Treatment with 50 mg/kg LY2109761 twice a day p.o. (days 1-5 of each week after inoculation) is continued for one group of untreated mice inoculated with untreated cells.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2649 mL 11.3245 mL 22.6490 mL 56.6226 mL
    5 mM 0.4530 mL 2.2649 mL 4.5298 mL 11.3245 mL
    10 mM 0.2265 mL 1.1325 mL 2.2649 mL 5.6623 mL
    15 mM 0.1510 mL 0.7550 mL 1.5099 mL 3.7748 mL
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    LY2109761 Related Classifications

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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      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:

    LY2109761700874-71-1LY 2109761LY-2109761TGF-β ReceptorAutophagyTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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    製品名:
    LY2109761
    製品番号:
    HY-12075
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