2. MAPK/ERK Pathway
  3. MAP4K
  4. GNE-495

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.

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CAS 番号 : 1449277-10-4

容量 価格（税別） 在庫状況 数量
1 mg $43 在庫あり
5 mg $100 在庫あり
10 mg $180 在庫あり
25 mg $320 在庫あり
50 mg $450 在庫あり
100 mg $750 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of GNE-495:

GNE-495 関連抗体

Top Publications Citing Use of Products

    GNE-495 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2026 Feb 16:218336.

    GNE-495 (3 mg/kg; i.p.; once daily for 3 weeks) reduced tumor burden in KPC (Pdx1-Cre x LSL-KRASG12D x LSL-TP53R172H) mice.

    GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671.  [Abstract]

    GNE-495 (0.2-10 µM; 24 h) dramatically diminished the expression of MAP4K4 in Huh7 and PLC/PRF/5 cells.

    GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671.  [Abstract]

    GNE-495 (2 µM; 24 h). Representative images and quantification of the Huh7 and PLC/PRF/5 cells in the wound-healing migration assays.

    GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671.  [Abstract]

    GNE-495 (2 µM; 24 h). Representative images and quantification of the migration and invasion of the Huh7 and PLC/PRF/5 cells in the Transwell assays.

    GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671.  [Abstract]

    Protein expression of EMT‐associated proteins in HCC and PLC/PRF/5 cells treated with GNE-495 (2 µM; 24 h).

    MAP4K 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
    MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.

    IC50 & Target[1]

    MAP4K4

    3.7 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HUVEC IC50
    0.057 nM
    Compound: 13, GNE-495
    Anti-angiogenesis activity in HUVEC assessed as inhibition of cell migration
    Anti-angiogenesis activity in HUVEC assessed as inhibition of cell migration
    		[PMID: 26288693]
    体外実験

    GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency[1].

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

    GNE-495 関連抗体
    体内実験

    GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows good in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%)[1].

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

    405.42

    分子式

    C22H20FN5O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=C2C=CC(C3=CC=CC(F)=C3)=NC2=C(N)N=C1)NC4CN(C(C5CC5)=O)C4
    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 : 2.17 mg/mL (5.35 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 2.4666 mL 12.3329 mL 24.6658 mL
    5 mM 0.4933 mL 2.4666 mL 4.9332 mL
    10 mM --- --- ---
    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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    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）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    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:  2% DMSO    40% PEG300    5% Tween-80    53% PBS

      Solubility: 1 mg/mL (2.47 mM); Suspended solution; Need ultrasonic

    • Protocol 2

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

      Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.22 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.2 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.
    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 +
    % 
    +
    %
    Tween-80 +
    %
    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: 99.49%

    COA (252 KB) LCMS (96 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [1]

    Rats, Mice and Pups [1]
    For the brain cassette study, three male Sprague-Dawley (SD) rats are dosed with intravenous (IV) bolus of six test compounds (e.g., GNE-495; 0.5 mg/kg). For the mouse PK study, female CD-1 mice are administered IV bolus doses of GNE-495 (1 mg/kg). In addition, female CD-1 mice are administered GNE-495 (5 mg/kg) via oral (PO) gavage. A dosing volume of 2 mL/kg is used for the rat brain cassette PK and 5 mL/kg is used for all other dosing. Animals are not fasted prior to dose administration, and water and food are available ad libitum. Following administration of the compound of interest, three blood samples (~60 μL) are collected at each time point from individual mice up to either 9 or 24 hours post-dose using a serial sampling approach. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice or in a chilled Kryorack prior to centrifugation to obtain plasma. Within 1 hr of collection, blood samples are centrifuged at approximately 1000-2000× g for 10-15 min at 4°C, and plasma is harvested. The plasma samples are stored at -70 to -80°C until analysis. For neonate PK, 3-day old CD1 pups are injected with 25 mg/kg and 50 mg/kg GNE-495 intraperitoneally, blood samples are collected at the time points indicated, retinas are collected one hour post-dose and snap frozen in liquid nitrogen and stored at -80°C until analysis. Plasma and retinal lysate concentrations are determined by LC/MS/MS.

    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 2.4666 mL 12.3329 mL 24.6658 mL 61.6644 mL
    5 mM 0.4933 mL 2.4666 mL 4.9332 mL 12.3329 mL
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    GNE-495 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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.

    Keywords:

    GNE-4951449277-10-4GNE495GNE 495MAP4KMAPK Kinase Kinase KinaseInhibitorinhibitorinhibit

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    製品名:
    GNE-495
    製品番号:
    HY-100343
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