1. MAPK/ERK Pathway
  2. MAP4K MAP3K
  3. NG25

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

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CAS 番号 : 1315355-93-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 177 在庫あり
Solution
10 mM * 1 mL in DMSO USD 177 在庫あり
Solid
1 mg $98 在庫あり
5 mg $150 在庫あり
10 mg $248 在庫あり
25 mg $540 在庫あり
50 mg $846 在庫あり
100 mg $1180 在庫あり
500 mg $2380 在庫あり
1 g $3800 在庫あり
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10 g   お問い合わせ  

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カスタマーレビュー

Based on 24 publication(s) in Google Scholar

Other Forms of NG25:

Top Publications Citing Use of Products

    NG25 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2018 Jul 10;11(538). pii: eaan5850.  [Abstract]

    A549 cells are treated for 30 min with either 5z-7-oxozeanol or NG-25 to inhibit TAK1 and immunoblotted with the indicated antibodies.

    NG25 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2018 Jan;17(1):1710-1716.  [Abstract]

    Expression level of p TAK1 and downstream targets following NG25 treatment. Western blot detection of p TAK1 and TAK1 expression levels in the sham group, and samples from HI, DMSO treated and NG25 treated rat brain cortexes.

    NG25 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2017 Oct;19(10):1248-1259.  [Abstract]

    Immortalized RIPK1 +/+ fetal liver mouse macrophages were infected with YopP-negative Ye-ΔyopP in presence of inhibitors for TAK1 (NP, NG25), IKKβ, IKK, p38, MK2, JNK, or MEK1/ERK. The phosphorylation of RIPK1 is analyzed by immunoblotting in cell lysates prepared after 75 min of infection.

    NG25 purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 Oct 5;36(40):5620-5630.  [Abstract]

    C3-TAg cells are starved and stimulated for 0, 15 and 30 min with ephrin-A1-Fc (EphA2 ligand; 1 μg/mL) in the presence or absence of ALW-II-41-27 or NG-25 control. EphA2 is immunoprecipitated and products probed for tyrosine phosphorylation and EphA2. ALW-II-41-27 significantly reduces basal and ephrin-A1-Fc induced tyrosine phosphorylation.

    NG25 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 1;8(61):104330-104346.  [Abstract]

    MC38-CT or -CC1-L cells are treated with 1 μM of DMSO, or the non-specific NG-25 or specific ALW-II-41-27 EPHA2 receptor inhibitor for indicated periods of time, followed by stimulation with EFNA1-Fc (2 μg/mL) in the last 15 min of treatments. Protein lysates are prepared and subjected to immunoblotting using antibodies to determine the effect of kinase inhibitors on EPHA2 activation.

    NG25 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2016 Sep 7;6:32737.  [Abstract]

    TAK1 inhibition inhibits Dox-induced p38 activation and IκBα degradation. Breast cancer cell lines T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549 are treated with Dox (20 μM) alone or combined with NG25 (2 μM) for 0, 2 h, 4 h or 6 h. The protein extracts are subjected to SDS-PAGE and immunoblotted with the antibodies against p-p38, p38, and IκBα. β-actin are detected as loading controls for whole cell extracts.

    NG25 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2014 Oct 10;453(1):106-11.  [Abstract]

    786-O/A489 RCC cells are treated with LYTAK1 (100 nM), 5Z-7-oxozeanol (5Z, 0.25 lM) or NG-25 (NG-25, 2.5 lM) for 24 h, Western blots are applied to tested list proteins.
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    製品説明

    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.

    IC50 & Target[1]

    MAP4K2

    21.7 nM (IC50)

    TAK1

    149 nM (IC50)

    LYN

    12.9 nM (IC50)

    GSK

    56.4 nM (IC50)

    ABL,ARG

    75.2 nM (IC50)

    FER

    82.3 nM (IC50)

    SRC

    113 nM (IC50)

    Eph B2

    672 nM (IC50)

    ZAK

    698 nM (IC50)

    Eph A2

    773 nM (IC50)

    Eph B4

    999 nM (IC50)

    ZC1/HGK

    3250 nM (IC50)

    RAF1

    7590 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    BaF3 IC50
    0.018 μM
    Compound: 1
    Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
    Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
    [PMID: 25075558]
    BaF3 IC50
    7.722 μM
    Compound: 1
    Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
    Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
    [PMID: 25075558]
    体外実験

    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. NG25 also potently suppresses several kinases such as LYN, CSK, FER, p38α, ABL,ARG and SRC, with IC50s of 12.9, 56.4, 82.3, 102, 75.2, and 113 nM, respectively[1]. NG25 is very potent suppressor of CpG B- or CpG A-stimulated secretion of IFNα and CL097-stimulated secretion of IFNβ, with complete inhibition by 400 nM[2]. NG25 treatment reduces cell viability of all tested breast cancer cell lines in a dose dependent manner. NG25 (2?μM) enhances the cytotoxic effect of Dox on breast cancer cells[3].

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

    分子量

    537.58

    分子式

    C29H30F3N5O2

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC(C(F)(F)F)=C(CN(CC2)CCN2CC)C=C1)C3=CC(OC4=C5C(NC=C5)=NC=C4)=C(C)C=C3

    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 : 13.46 mg/mL (25.04 mM; Need ultrasonic; 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 1.8602 mL 9.3009 mL 18.6019 mL
    5 mM 0.3720 mL 1.8602 mL 3.7204 mL
    10 mM 0.1860 mL 0.9301 mL 1.8602 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.

    • Molarity Calculator

    • Dilution Calculator

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

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    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)

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    体内:

    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: ≥ 2.5 mg/mL (4.65 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
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    %
    Saline
    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.
    純度とドキュメンテーション

    純度: 98.68%

    参考文献
    キナーゼ実験
    [2]

    IRF7 is expressed in Escherichia coli as a glutathione S-transferase (GST) fusion protein with a PreScission proteinase cleavage site between the GST and the IRF7. The GST-IRF7 is captured on glutathione-Sepharose and IRF7 released from GST and glutathione-Sepharose by digestion with PreScission proteinase. His6-tagged IKKβ and TBK1 are expressed in their active phosphorylated forms in insect Sf21 cells and purified by affinity chromatography on nickel nitrilotriacetate-agarose. Active GST-IKKα is purchased from Millipore and assayed.

    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。

    細胞実験
    [2]

    3.5×105 Gen2.2 cells or Flt3-DCs are incubated for 1 h in 96-well plates without or with the indicated concentrations of inhibitor, then stimulated with 1 μM CpG (type A or B) or 1 μg/mL of CL097 or R848. After 5 or 12 h the cell culture supernatants are collected, clarified by centrifugation, and frozen at −80°C until cytokine levels are analyzed. For cell viability assays, unstimulated cells are incubated for 12 h in the absence or presence of inhibitors. Cells are then fixed and the percentage of live cells analyzed by flow cytometry.

    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, 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 1.8602 mL 9.3009 mL 18.6019 mL 46.5047 mL
    5 mM 0.3720 mL 1.8602 mL 3.7204 mL 9.3009 mL
    10 mM 0.1860 mL 0.9301 mL 1.8602 mL 4.6505 mL
    15 mM 0.1240 mL 0.6201 mL 1.2401 mL 3.1003 mL
    20 mM 0.0930 mL 0.4650 mL 0.9301 mL 2.3252 mL
    25 mM 0.0744 mL 0.3720 mL 0.7441 mL 1.8602 mL
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    • Molarity Calculator

    • Dilution Calculator

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

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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
    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.

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    Inquiry Information

    製品名:
    NG25
    製品番号:
    HY-15434
    数量:
    MCE 日本正規代理店: