2. MAPK/ERK Pathway
  3. KLF
  4. ML264

ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.

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CAS 番号 : 1550008-55-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 93 在庫あり
Solution
10 mM * 1 mL in DMSO USD 93 在庫あり
Solid
1 mg $36 在庫あり
5 mg $85 在庫あり
10 mg $140 在庫あり
25 mg $280 在庫あり
50 mg $440 在庫あり
100 mg $660 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 15 publication(s) in Google Scholar

ML264 関連抗体

Top Publications Citing Use of Products

    ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 May 23:pwae032.  [Abstract]

    ML264 (20 mg/kg; i.p.; every other day for 4-6 weeks) significantly alleviated the HCM phenotypes, as shown by a marked reduction in LVPWd thickness in the treated HCM mice compared to that in the untreated HCM (hypertrophic cardiomyopathy) mice.

    ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 May 23:pwae032.  [Abstract]

    ML264 (20 mg/kg; i.p.; every other day) significantly decreased the cardiomyocyte cross-sectional area in HCM (hypertrophic cardiomyopathy) mice.

    ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 May 23:pwae032.  [Abstract]

    ML264 (20 mg/kg; i.p.; every other day) significantly reduced myocardial fibrosis in HCM (hypertrophic cardiomyopathy) mice.

    ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 May 23:pwae032.  [Abstract]

    The transcriptomes of the HCM (hypertrophic cardiomyopathy) mice treated with ML264 (20 mg/kg; i.p.; every other day) were more similar to those of the WT mice than those of the untreated mutants.

    ML264 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2024 May 23:pwae032.  [Abstract]

    ML264 (20 mg/kg; i.p.; every other day) reversed 74 of 88 (84%) co-upregulated DEGs and 217 of 275 (79%) co-downregulated DEGs in HCM (hypertrophic cardiomyopathy) mice.

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    製品説明

    ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.

    IC50 & Target

    KLF5[1]
    体外実験

    ML264 is highly active (IC50=29 nM is a cell-based assay for proliferation of DLD-1 cells, IC50=81 nM in a cell-based luciferase assay). ML264 lacks cytotoxicity in the IEC-6 control cell line (IC50>50 μM, <50% inhibition is observed at 100 μM). Robust activity is also seen in several other KLF5-expressing cell types as well (e.g., HCT116, IC50=560 nM; HT29, IC50=130 nM; SW620, IC50=430 nM). Western blot analysis shows that ML264 significantly reduces KLF5 expression[1]. The effects of ML264 are tested on the rate of cell proliferation of colon cancer cells lines DLD-1 and HCT116 over 72 hours. ML264 efficiently inhibits the rate of proliferation of both cell lines. A significant decrease in proliferation is evident within 24 hours of treatment and by 72 hours the live cell numbers of ML264-treated and vehicle-treated cells differed by 15- to 30- fold. An MTS assay that allows the quantification of metabolically active cells is performed. ML264 treatment significantly reduces the number of cells undergoing mitosis in DLD-1 cells at 24, 48 and 72 hours[2].

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

    ML264 関連抗体
    体内実験

    Single daily injections of ML264 at 10 mg/kg do not significantly affect tumor growth. However, twice daily injections of ML264 at 10 mg/kg or 25 mg/kg result in significant reductions in tumor growth, and this effect can be detected as early as two days after the first injection. The data also show that there is a concentration-dependent effect of ML264 on the tumor volume. Statistical analysis of tumor growth reveals significant tumor size reduction in mice treated twice daily with ML264 compared to those receiving only vehicle at day 5 and 10[2].

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

    384.88

    分子式

    C17H21ClN2O4S
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NCC(N(C)C(CC1)CCS1(=O)=O)=O)/C=C/C2=CC=CC(Cl)=C2
    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 : ≥ 100 mg/mL (259.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5982 mL 12.9911 mL 25.9821 mL
    5 mM 0.5196 mL 2.5982 mL 5.1964 mL
    10 mM 0.2598 mL 1.2991 mL 2.5982 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

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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    90% Corn Oil

      Solubility: ≥ 3.25 mg/mL (8.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.25 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 (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (25.98 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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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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    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
    細胞実験
    [2]

    For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10 μM ML264 or with vehicle (DMSO). Live cells are collected at 24, 48 and 72 hours post treatment and their numbers are determined by counting using a Coulter counter. Each experiment is done in triplicate. In MTS assay, DLD-1 and HCT116 cells are treated with 10 μM ML264 or with vehicle (DMSO). After 24, 48, and 72 hours of incubations, 20 μL of MTS solution is added to each well and an analysis is performed. The measurement of the control (cells with medium and DMSO) is defined as 100% and the results from other measurements are calculated accordingly. Each experiment is done in sextuplicate. A cell cycle progression assay is performed. Each experiment is done in triplicate. The apoptosis rate is determined using the Alexa Fluor 488 Annexin V/Dead Cell Apoptosis Kit with analysis by flow cytometry. Each experiment is done in triplicate[2].

    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
    [2]

    Mice[2]
    Nude mice are housed under specific pathogen-free conditions in ventilated and filtered cages under positive pressure. Xenograft tumors are generated by injecting subcutaneously 5×106 DLD-1 human colorectal cells into the right flank of 6-7 week old male nude mice. Tumor volume is determined by caliper measurement and calculated by established methods. When tumors reach a volume of about 100 mm6, mice are treated intraperitoneally (i.p.) with varying doses of ML264: 10 mg/kg daily, 10 mg/kg twice per day and 25 mg/kg twice per day, with each treatment regimen lasting for a duration of 10 days. The vehicle solution is used as the control treatment. Mice are monitored and weighed every two days. Experiments are terminated when the tumor’s greatest measurement reaches 2 cm. Tumors are excised and retained for further analyses[2].

    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 2.5982 mL 12.9911 mL 25.9821 mL 64.9553 mL
    5 mM 0.5196 mL 2.5982 mL 5.1964 mL 12.9911 mL
    10 mM 0.2598 mL 1.2991 mL 2.5982 mL 6.4955 mL
    15 mM 0.1732 mL 0.8661 mL 1.7321 mL 4.3304 mL
    20 mM 0.1299 mL 0.6496 mL 1.2991 mL 3.2478 mL
    25 mM 0.1039 mL 0.5196 mL 1.0393 mL 2.5982 mL
    30 mM 0.0866 mL 0.4330 mL 0.8661 mL 2.1652 mL
    40 mM 0.0650 mL 0.3248 mL 0.6496 mL 1.6239 mL
    50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2991 mL
    60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0826 mL
    80 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8119 mL
    100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6496 mL
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    ML264 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
    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:

    ML2641550008-55-3ML 264ML-264KLFKrüppel-like factorInhibitorinhibitorinhibit

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    製品番号:
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