1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. LMK-235

LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.

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

LMK-235 Chemical Structure

LMK-235 Chemical Structure

CAS No. : 1418033-25-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 96 In-stock
50 mg USD 300 In-stock
100 mg USD 540 In-stock
200 mg USD 960 In-stock
500 mg   Get quote  
1 g   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

    LMK-235 purchased from MedChemExpress. Usage Cited in: Life Sci. 2018 Aug 15;207:386-394.  [Abstract]

    The protein levels of HDAC4, HDAC5, HO-1, histone 3 acetylation, histone 4 acetylation and Smad7 in CCRF-SB cells are detected by Western blot after LMK-235 treatment at 0.25, 0.5, 1, 2 and 4 μM for 24 h. β-Actin is used as internal reference.

    LMK-235 purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2018;19(9):825-834.  [Abstract]

    OCILY10 cells are treated with different concentration of LMK-235 (0.5, 1.0, 1.5, 2.0 and 2.5 μM) for 24 hours,24 hours, 36 hours and 48 hours, and HDAC4 and HDAC5 protein levels are examined by Western blot .All experiments are conducted three times.

    LMK-235 purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2018;19(9):825-834.  [Abstract]

    OCI-LY3 cells are treated with different concentration of LMK-235 (0.5, 1.0, 1.5, 2.0 and 2.5 μM) for 24 hours,24 hours, 36 hours and 48 hours, and HDAC4 and HDAC5 protein levels are examined by Western blot .All experiments are conducted three times.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.

    IC50 & Target[1]

    HDAC5

    4.22 nM (IC50)

    HDAC4

    11.9 nM (IC50)

    HDAC6

    55.7 nM (IC50)

    HDAC1

    320 nM (IC50)

    HDAC11

    852 nM (IC50)

    HDAC2

    881 nM (IC50)

    HDAC8

    1278 nM (IC50)

    In Vitro

    LMK-235 shows cytotoxic activity against human ovarian cancer cell lines A2780 and A2780 CisR, with IC50s of 0.49 μM and 0.32 μM, respectively. LMK-235 inhibits HDAC in A2780 and A2780 CisR cell lines, with IC50s of 0.65 μM and 0.32 μM, respectively. LMK-235 produces a higher reduction in cell viability in comparison to the combination of cisplatin and vorinostat in all cell lines[1]. LMK-235 (0, 0.625, 1.25, 2.5, 5, 10, and 20 μM) reduces the proliferation of BC cells in a dose- and time-dependent manner. LMK-235 (0-800 nM) also inhibits the growth of BC cells. Moreover, LMK-235 synergizes with bortezomib in BC cell lines[2]. LMK235 (2, 20?nM) decreases in HDAC4 nuclear accumulation in Cdkl5 -/Y NPCs, completely restores the reduced number of neurons generated from Cdkl5 -/Y NPCs. LMK235 also restores histone 3 acetylation in Cdkl5 -/Y NPCs. LMK235 causes a notable increase in the isoform IV, but does not affect BDNF isoforms I or II[3].

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

    In Vivo

    LMK235 (5 and 20?mg/kg) restores survival and maturation of postmitotic granule neurons in Cdkl5 -/Y mice. LMK235 also restores synapse development in the dentate gyrus and hippocampus of Cdkl5 -/Y mice. Furthermore, LMK235 restores hippocampus-dependent learning and memory in Cdkl5 -/Y mice[3].

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

    Molecular Weight

    294.35

    Formula

    C15H22N2O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NOCCCCCC(NO)=O)C1=CC(C)=CC(C)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (101.92 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 3.3973 mL 16.9866 mL 33.9732 mL
    5 mM 0.6795 mL 3.3973 mL 6.7946 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.

    • 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.08 mg/mL (7.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
    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.
    Purity & Documentation

    Purity: 99.61%

    References
    Cell Assay
    [1]

    The rate of cell survival under the action of test substances is evaluated by an improved MTT assay. The assay is based on the ability of viable cells to metabolize yellow 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to violet formazan that can be detected spectrophotometrically. In brief, A2780, Cal27, Kyse510, and MDA-MB-231 cell lines are seeded at a density of 5000, 7000, 8000, and 10 000 cells/well in 96-well plates. After 24 h, cells are exposed to increased concentrations of the test compounds. Incubation is ended after 72 h, and cell survival is determined by addition of MTT solution (5 mg/mL in phosphate buffered saline). The formazan precipitate is dissolved in DMSO. Absorbance is measured at 544 and 690 nm in a FLUOstar microplate reader[1].

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

    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. 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 3.3973 mL 16.9866 mL 33.9732 mL 84.9329 mL
    5 mM 0.6795 mL 3.3973 mL 6.7946 mL 16.9866 mL
    10 mM 0.3397 mL 1.6987 mL 3.3973 mL 8.4933 mL
    15 mM 0.2265 mL 1.1324 mL 2.2649 mL 5.6622 mL
    20 mM 0.1699 mL 0.8493 mL 1.6987 mL 4.2466 mL
    25 mM 0.1359 mL 0.6795 mL 1.3589 mL 3.3973 mL
    30 mM 0.1132 mL 0.5662 mL 1.1324 mL 2.8311 mL
    40 mM 0.0849 mL 0.4247 mL 0.8493 mL 2.1233 mL
    50 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
    60 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4155 mL
    80 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
    100 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8493 mL
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    LMK-235 Related Classifications

    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.

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