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(-)-DHMEQ  (Synonyms: Dehydroxymethylepoxyquinomicin)

Cat. No.: HY-14645 Purity: 98.47%
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(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.

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

(-)-DHMEQ Chemical Structure

(-)-DHMEQ Chemical Structure

CAS No. : 287194-40-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 172 In-stock
Solution
10 mM * 1 mL in DMSO USD 172 In-stock
Solid
2 mg USD 120 In-stock
5 mg USD 200 In-stock
10 mg USD 300 In-stock
25 mg USD 550 In-stock
50 mg   Get quote  
100 mg   Get quote  

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

Customer Review

Based on 32 publication(s) in Google Scholar

Other Forms of (-)-DHMEQ:

Top Publications Citing Use of Products

    (-)-DHMEQ purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Jun;17(6):1303-1314.  [Abstract]

    Effects of NF-κB activation/inhibition on the expression of NF-κB and its downstream targets as well as AR in bladder cancer cells. Western blotting of NF-κB/p65, p-NF-κB/p65, and AR, using proteins extracted from UMUC3 cells cultured with ethanol (mock), TNF-α (20 ng/mL), or DHMEQ (15 µg/mL) for 6 hours.

    (-)-DHMEQ purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Jun;17(6):1303-1314.  [Abstract]

    Effects of TNF-α/DHMEQ on the expression of NF-κB and AR as well as neoplastic transformation of urothelial cells. Western blotting of NF-κB/p65, p-NF-κB/p65, and AR, using proteins extracted from SVHUC-AR cells cultured with ethanol, TNF-α(20 ng/mL), or DHMEQ (15 µg/mL) for 6 hours.

    (-)-DHMEQ purchased from MedChemExpress. Usage Cited in: Mol Cells. 2018 Dec 31;41(12):1008-1015.  [Abstract]

    NCI-H157 cells are pretreated with DHMEQ (10 or 20 μg/mL) for 2 h and then stimulated with PS-341 for 6 or 24 h. Nuclear proteins (6 h) and whole cell proteins (24 h) are isolated and subjected to Western blot analysis for p65, Lamin A/C, COX-2, and GAPDH.

    (-)-DHMEQ purchased from MedChemExpress. Usage Cited in: Biol Pharm Bull. 2017;40(10):1669-1677.  [Abstract]

    A549 transfectants stably expressing RelB (C144S) (B) are preincubated with various concentrations of (–)-DHMEQ for 1 h and then incubated with or without LTβ (25 ng/mL) for 2 h in the presence or absence of (−)-DHMEQ.

    (-)-DHMEQ purchased from MedChemExpress. Usage Cited in: Biol Pharm Bull. 2017;40(10):1669-1677.  [Abstract]

    A549 transfectants stably expressing RelB WT (A) are preincubated with various concentrations of (–)-DHMEQ for 1 h and then incubated with or without LTβ (25 ng/mL) for 2 h in the presence or absence of (−)-DHMEQ.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity[1][2][3].

    IC50 & Target[1]

    RelA

     

    RelB

     

    In Vitro

    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2-10 μg/mL; 12-48 hours) treatment significantly reduces the viability of all cell lines in a dose- and time-dependent manner, whereas the effect is not significant in a control cell line K562 without constitutive NF-κB activity[2].
    ? (-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1 and K562 cells) treatment significantly increases the Annexin V-positive cells in MT-1 and TL-Om1 cell lines[2].
    ? (-)-DHMEQ (10 μg/mL; 4-16 hours; MT-1 cells) treatment down-regulates Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53, and up-regulates proapoptotic genes such as caspase-3, -8, and-9[2].
    ? (-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ[2].
    ? (-)-DHMEQ binds to p65, cRel, RelB, and p50, but not to p52 at specific cysteine residues. (-)-DHMEQ inhibits not only DNA-binding of RelB, but also its interaction to importin. (-)-DHMEQ also induces instability of RelB[1].

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

    Cell Proliferation Assay[2]

    Cell Line: TL-Om1, MT-1, KK-1, ST-1 and K562 cells
    Concentration: 2 μg/mL, 5 μg/mL, 10 μg/mL
    Incubation Time: 12 hours, 24 hours, 48 hours
    Result: Significantly reduced the viability of all cell lines in a dose- and time-dependent manner.

    Apoptosis Analysis[2]

    Cell Line: TL-Om1, MT-1 and K562 cells
    Concentration: 10 μg/mL
    Incubation Time: 0 hours, 24 hours, 48 hours
    Result: Annexin V-positive cells were significantly increased after 24 to 48 hours.

    Western Blot Analysis[2]

    Cell Line: MT-1 cells
    Concentration: 10 μg/mL
    Incubation Time: 4 hours, 8 hours, 16 hours
    Result: Annexin V-positive cells were significantly increased after 24 to 48 hours.
    In Vivo

    (-)-DHMEQ (4 mg/kg or 12 mg/kg; intraperitoneal injection; on day 0 and 3 times a week; for one month; SCID mice) treatment shows a significant increase in the survival rate in mice[2].

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

    Animal Model: Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells[2]
    Dosage: 4 mg/kg or 12 mg/kg
    Administration: Intraperitoneal injection; on day 0 and 3 times a week; for one month
    Result: Showed a significant increase in the survival rate in mice.
    Molecular Weight

    261.23

    Formula

    C13H11NO5

    CAS No.
    Appearance

    Solid

    Color

    Off-white to gray

    SMILES

    O=C1[C@@H](O2)[C@@H]2[C@@H](O)C(NC(C3=C(O)C=CC=C3)=O)=C1

    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 : 95 mg/mL (363.66 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 3.8280 mL 19.1402 mL 38.2804 mL
    5 mM 0.7656 mL 3.8280 mL 7.6561 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: 5 mg/mL (19.14 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 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 (50.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    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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    %
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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

    Purity: 98.72%

    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 3.8280 mL 19.1402 mL 38.2804 mL 95.7011 mL
    5 mM 0.7656 mL 3.8280 mL 7.6561 mL 19.1402 mL
    10 mM 0.3828 mL 1.9140 mL 3.8280 mL 9.5701 mL
    15 mM 0.2552 mL 1.2760 mL 2.5520 mL 6.3801 mL
    20 mM 0.1914 mL 0.9570 mL 1.9140 mL 4.7851 mL
    25 mM 0.1531 mL 0.7656 mL 1.5312 mL 3.8280 mL
    30 mM 0.1276 mL 0.6380 mL 1.2760 mL 3.1900 mL
    40 mM 0.0957 mL 0.4785 mL 0.9570 mL 2.3925 mL
    50 mM 0.0766 mL 0.3828 mL 0.7656 mL 1.9140 mL
    60 mM 0.0638 mL 0.3190 mL 0.6380 mL 1.5950 mL
    80 mM 0.0479 mL 0.2393 mL 0.4785 mL 1.1963 mL
    100 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9570 mL
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    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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    Product Name:
    (-)-DHMEQ
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