1. Epigenetics
  2. Histone Demethylase
  3. KDM5-C70

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.

For research use only. We do not sell to patients.

CAS No. : 1596348-32-1

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Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    KDM5-C70 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Feb 13;15(1):5409.  [Abstract]

    NSCs treated with 0.1% DMSO (Upper row) or 25 µM KDM5-C70 (Lower row) in the absence of EGF and FGF2 for 4 days. (a) nuclei stained with DAPI (blue), (b) astrocytes immuno-stained with GFAP (red), (c) neurons immuno-stained with TuJ1 (green), and (d) merged images.

    KDM5-C70 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Feb 13;15(1):5409.  [Abstract]

    Real-time RT-PCR was performed to quantify the mRNA levels of Gfap. Total RNA was extracted from NSCs treated with 0.1% DMSO or 25 µM KDM5-C70 in the absence of EGF and FGF2 for 3 days. Gapdh was used as an internal control.

    KDM5-C70 purchased from MedChemExpress. Usage Cited in: Cell Res. 2023 May;33(5):403-406.  [Abstract]

    Western blotting was performed in mRBBP5-dTAG mESCs treated with dTAG and/or pan-KDM5 inhibitor KDM5-C70 for 12 h. The results showed that supplementation with KDM5-C70 reversed the reduction of global H3K4me2/3 induced by 12 h dTAG treatment.

    KDM5-C70 purchased from MedChemExpress. Usage Cited in: Cell Res. 2023 May;33(5):403-406.  [Abstract]

    Western blotting of dTAG treatment with or without pan-KDM5 inhibition by KDM5-C70 (12 h) in mRBBP5-dTAG mESCs. The results showed that treatment with the pan-KDM5 inhibitor KDM5-C70 restored H3K4me3 levels, indicating that KDM5 demethylases are mainly responsible for RBBP5 degradation-induced rapid H3K4me3 depletion.

    KDM5-C70 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Apr 7;9(14):eadd8343.  [Abstract]

    The treatment of pan-Kdm5 histone demethylase inhibitor KDM5-C70 partially rescued the mushroom morphology of te×ls embryos. The te×ls embryos were treated with KDM5-C70 (20 μM) from stage 3, and images were captured at stage 11.

    KDM5-C70 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Apr 7;9(14):eadd8343.  [Abstract]

    The H3K4me3 and Mdm2 protein levels in te×ls embryos upon KDM5-C70 (10-20 μM) treatment were detected by western blot around stage 11. The results showed that elevations of H3K4me3 and Mdm2 were observed in KDM5-C70–treated te×ls embryos.

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    Description

    KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2].

    IC50 & Target

    KDM5

     

    Cellular Effect
    Cell Line Type Value Description References
    MCF7 IC50
    <1 μM
    Compound: 130
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay
    [PMID: 26710088]
    MM1.S EC50
    3.1 μM
    Compound: 14
    Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
    Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
    [PMID: 34555614]
    U2OS IC50
    <1 μM
    Compound: 130
    Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
    Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
    [PMID: 26710088]
    U2OS IC50
    <1 μM
    Compound: 130
    Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
    Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
    [PMID: 26710088]
    In Vitro

    KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM)[1].
    KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression[1].
    Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations[1].

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

    Cell Viability Assay[1]

    Cell Line: MM.1S myeloma cells
    Concentration: 10-9-10-5 M
    Incubation Time: 7 days
    Result: Showed antiproliferative effects after 7 days of treatment at elevated concentrations.

    Western Blot Analysis[1]

    Cell Line: MM.1S myeloma cells
    Concentration: 50 μM
    Incubation Time: 7 days
    Result: Decreased the level of phosphorylation of retinoblastoma protein (Rb).
    Molecular Weight

    336.43

    Formula

    C17H28N4O3

    CAS No.
    Appearance

    Liquid (Density: 1.099 g/cm3)

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OCC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (297.24 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 2.9724 mL 14.8619 mL 29.7239 mL
    5 mM 0.5945 mL 2.9724 mL 5.9448 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 (stored under nitrogen). 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)

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    In Vivo:

    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 (7.43 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 (7.43 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    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.
    Purity & Documentation
    References

    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 (stored under nitrogen). 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 2.9724 mL 14.8619 mL 29.7239 mL 74.3097 mL
    5 mM 0.5945 mL 2.9724 mL 5.9448 mL 14.8619 mL
    10 mM 0.2972 mL 1.4862 mL 2.9724 mL 7.4310 mL
    15 mM 0.1982 mL 0.9908 mL 1.9816 mL 4.9540 mL
    20 mM 0.1486 mL 0.7431 mL 1.4862 mL 3.7155 mL
    25 mM 0.1189 mL 0.5945 mL 1.1890 mL 2.9724 mL
    30 mM 0.0991 mL 0.4954 mL 0.9908 mL 2.4770 mL
    40 mM 0.0743 mL 0.3715 mL 0.7431 mL 1.8577 mL
    50 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
    60 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2385 mL
    80 mM 0.0372 mL 0.1858 mL 0.3715 mL 0.9289 mL
    100 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7431 mL
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    • 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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