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  3. WEHI-345

WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.

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CAS 番号 : 1354825-58-3

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 在庫あり
Solution
10 mM * 1 mL in DMSO USD 145 在庫あり
Solid
5 mg $132 在庫あり
10 mg $209 在庫あり
25 mg $400 在庫あり
50 mg $650 在庫あり
100 mg $950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    WEHI-345 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2018 Feb 15;69(4):551-565.e7.  [Abstract]

    THP1 cells are treated with muramyl dipeptide (MDP) for 30 min in the presence or absence of indicated kinase inhibitors (1 mM; added 1 hr prior) followed by lysis in 6 M urea buffer. Lysates are immunoprecipitated with K63 and linear ubiquitin chain antibodies, and precipitates and lysates are examined by western blotting using indicated antibodies.

    WEHI-345 purchased from MedChemExpress. Usage Cited in: J Immunol. 2017 May 1;198(9):3729-3736.  [Abstract]

    Confocal images of lysozyme and procryptdin in cultured WT crypt organoids treated with GSK583 (5 μM) or mock-treated (A), or WEHI-345 (2.5 μM) or mock-treated (B) for 16 hours.

    RIP kinase アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 純度とドキュメンテーション

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    製品説明

    WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation[1].

    IC50 & Target

    RIPK2

     

    Cellular Effect
    Cell Line Type Value Description References
    H9c2 IC50
    13.07 3
    Compound: WEHI-345
    Toxicity in rat H9c2 cells assessed as inhibitory rate
    Toxicity in rat H9c2 cells assessed as inhibitory rate
    [PMID: 35709396]
    BMDM IC50
    57.7 1
    Compound: WEHI-345
    Inhibition of LPS/MDP-stimulated TNFalpha production in C57BL/6J mouse BMDM cells by ELISA relative to control
    Inhibition of LPS/MDP-stimulated TNFalpha production in C57BL/6J mouse BMDM cells by ELISA relative to control
    [PMID: 35709396]
    BMDM IC50
    57.7 1
    Compound: WEHI-345
    Inhibition of LPS/MDP-stimulated TNFalpha production in C57BL/6J mouse BMDM cells by ELISA relative to control
    Inhibition of LPS/MDP-stimulated TNFalpha production in C57BL/6J mouse BMDM cells by ELISA relative to control
    [PMID: 35709396]
    BMDM IC50
    57.7 1
    Compound: WEHI-345
    Inhibition of LPS/MDP-stimulated TNFalpha production in C57BL/6J mouse BMDM cells by ELISA relative to control
    Inhibition of LPS/MDP-stimulated TNFalpha production in C57BL/6J mouse BMDM cells by ELISA relative to control
    [PMID: 35709396]
    H9c2 IC50
    13.07 3
    Compound: WEHI-345
    Toxicity in rat H9c2 cells assessed as inhibitory rate
    Toxicity in rat H9c2 cells assessed as inhibitory rate
    [PMID: 35709396]
    体外実験

    WEHI-345 (500 nM; Raw 267.4 cells) is able to inhibit MDP-induced autophosphorylation activity of RIPK2 in cells[1].
    WEHI-345 (500 nM; 0 hour, 2 hours, 4 hours, 8 hours; BMDMs or THP-1 cells) potently blocks MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in bone marrow-derived macrophages (BMDMs). In THP-1 cells, WEHI-345 reduces mRNA levels of NF-kB targets such as TNF, IL-8, IL-1b and A20[1].

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

    Western Blot Analysis[1]

    Cell Line: Raw 267.4 cells
    Concentration: 500 nM
    Incubation Time:
    Result: Inhibited MDP-induced autophosphorylation activity of RIPK2 in cells.

    RT-PCR[1]

    Cell Line: BMDMs or THP-1 cells
    Concentration: 500 nM
    Incubation Time: 0 hour, 2 hours, 4 hours, 8 hours
    Result: Blocked MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in BMDMs. And reduced mRNA levels of NF-kB targets in THP-1 cells.
    体内実験

    WEHI-345 (20 mg/kg; intraperitoneal injection; twice daily; for 6 days; C57BL/6 male mice) treatment reduces disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improves body weight and reduces cytokine and chemokine levels, indicating an overall improvement of the condition in experimental autoimmune encephalomyelitis (EAE)-induced wild-type C57Bl/6 mice[1].

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

    Animal Model: C57BL/6 male mice (8-week-old)[1]
    Dosage: 20 mg/kg
    Administration: Intraperitoneal injection; twice daily; for 6 days
    Result: Reduced disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improved body weight and reduced cytokine and chemokine levels.
    分子量

    401.46

    分子式

    C22H23N7O

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=NC=C1)NCC(C)(N2N=C(C3=CC=C(C)C=C3)C4=C(N)N=CN=C42)C

    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 : 25 mg/mL (62.27 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 2.4909 mL 12.4545 mL 24.9091 mL
    5 mM 0.4982 mL 2.4909 mL 4.9818 mL
    10 mM 0.2491 mL 1.2455 mL 2.4909 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.

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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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.23 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 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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.
    純度とドキュメンテーション
    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 2.4909 mL 12.4545 mL 24.9091 mL 62.2727 mL
    5 mM 0.4982 mL 2.4909 mL 4.9818 mL 12.4545 mL
    10 mM 0.2491 mL 1.2455 mL 2.4909 mL 6.2273 mL
    15 mM 0.1661 mL 0.8303 mL 1.6606 mL 4.1515 mL
    20 mM 0.1245 mL 0.6227 mL 1.2455 mL 3.1136 mL
    25 mM 0.0996 mL 0.4982 mL 0.9964 mL 2.4909 mL
    30 mM 0.0830 mL 0.4152 mL 0.8303 mL 2.0758 mL
    40 mM 0.0623 mL 0.3114 mL 0.6227 mL 1.5568 mL
    50 mM 0.0498 mL 0.2491 mL 0.4982 mL 1.2455 mL
    60 mM 0.0415 mL 0.2076 mL 0.4152 mL 1.0379 mL
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    一般には略語で表示されます:C1V1 = C2V2

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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.

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    Inquiry Information

    製品名:
    WEHI-345
    製品番号:
    HY-18937
    数量:
    MCE 日本正規代理店: