2. Cell Cycle/DNA Damage
  3. PERK
  4. MK-28

MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.

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CAS 番号 : 864388-65-8

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 330 在庫あり
Solution
10 mM * 1 mL in DMSO USD 330 在庫あり
Solid
5 mg $300 在庫あり
10 mg $480 在庫あり
25 mg $930 在庫あり
50 mg $1400 在庫あり
100 mg $2100 在庫あり
1 g $4900 在庫あり
5 g   お問い合わせ  
10 g   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 9 publication(s) in Google Scholar

MK-28 関連抗体

Top Publications Citing Use of Products

    MK-28 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Jun;4(6):839-853.  [Abstract]

    Representative images of UCP1 immunofluorescence staining. SVF cells isolated from iWAT of 2-month-old male mice were pre-treated with either vehicle, E2 (10 nM), or three different activators of ER stress MK-28, IXA4, AA147 (10 μM) before differentiating into beige adipocytes.

    MK-28 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Jun;4(6):839-853.  [Abstract]

    Western blot analysis of PERK and PERK phosphorylation in iWAT from vehicle and MK-28 (10 μM).

    MK-28 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Jun;4(6):839-853.  [Abstract]

    qPCR analysis of thermogenic gene expression treated with MK-28 (10 μM).

    MK-28 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Jun;4(6):839-853.  [Abstract]

    Representative images of H&E staining in the middle part of iWAT treated with MK-28 (1 mg/kg, i.p.).

    MK-28 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Jun;4(6):839-853.  [Abstract]

    The blood glucose levels of the vehicle or MK28 (1 mg/kg, i.p.) treated group in 2-month-old male mice after intraperitoneal injection of glucose tolerance test and Area under curve (AUC) analysis by one way-ANOVA followed by Tukey’s post-hoc test.

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    製品説明

    MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1].

    体外実験

    MK-28 (0-100 μM) shows PERK selectivity in vitro on a 391-kinase panel and rescues cells (but not PERK / cells) from ER stress-induced apoptosis[1].
    ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ111/111 cells at high MK-28 concentration. CHOP and GADD34 mRNA levels show a signifcant increase in both cell types, up to 10- and 5-fold respectively[1].
    MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2)[1].

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

    MK-28 関連抗体

    Apoptosis Analysis[1].

    Cell Line: STHdhQ111/111 cells.
    Concentration: 0-100 μM.
    Incubation Time: 48 h.
    Result: Rescued cells from ER stress-induced apoptosis.
    体内実験

    MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (Cmax) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection[1].
    MK-28 (1 mg/kg, IP, daily for 28 days) improves systemic function and survival in R6/2 mice and induces increased levels of eIF2α-P in the mouse brain striatum[1].
    MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity[1].

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

    Animal Model: R6/2 mice[1].
    Dosage: 1 mg/kg.
    Administration: IP, daily for 28 days.
    Result: Incerased the survival.
    分子量

    396.44

    分子式

    C24H20N4O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OC1=CC=C(C=C1O)/C=N/N(C2=NC(C3=CC=CC=C3)=CC(C4=CC=CC=C4)=N2)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 : 12.5 mg/mL (31.53 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 2.5224 mL 12.6122 mL 25.2245 mL
    5 mM 0.5045 mL 2.5224 mL 5.0449 mL
    10 mM 0.2522 mL 1.2612 mL 2.5224 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    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）

    C1

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    体積 （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: 1.25 mg/mL (3.15 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.25 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 (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.
    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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    +
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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

    純度: 99.88%

    COA (248 KB) HNMR (231 KB) LCMS (98 KB)

    取扱説明書 (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5224 mL 12.6122 mL 25.2245 mL 63.0612 mL
    5 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
    10 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
    15 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
    20 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 mL
    25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
    30 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
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    MK-28 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    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:

    MK-28864388-65-8MK28MK 28PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseHuntingtonER-stressInhibitorinhibitorinhibit

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    製品名:
    MK-28
    製品番号:
    HY-137207
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