1. NF-κB
  2. IKK
  3. IMD-0354

IMD-0354  (Synonyms: IKK2 Inhibitor V)

Cat. No.: HY-10172 Purity: 99.51%
SDS COA Handling Instructions

IMD-0354 (IKK2 Inhibitor V) est un inhibiteur sélectif de IKKβ qui inhibe l'activité NF-κB. IMD-0354 inhibe l'activité de transcription de NF-κB induite par le TNF-α avec un IC50 de 1,2 uM.

IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.

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

IMD-0354 Chemical Structure

IMD-0354 Chemical Structure

CAS No. : 978-62-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

    IMD-0354 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jun 12;11(6):455.  [Abstract]

    Phosphorylation of both p65 and IKKβ is efficiently suppressed after IMD0354 treatment, which shows no effectiveness upon NIK/IKKα.

    IMD-0354 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jun 12;11(6):455.  [Abstract]

    As illustrated in immunofluorescence, activation of IKKβ derived from CRYAB blockade is reversed by IMD0354 addition.

    View All IKK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity[1]. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM[2].

    IC50 & Target[1][2]

    IKKβ

     

    NF-κB

    1.2 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    1.27 μM
    Compound: IMD-0354
    Inhibition of NFkappaB (unknown origin) expressed in human A549 cells co-transfected with pNFkappaB-Luc vector assessed as reduction in TNFalpha-induced NFkappaB transcriptional activity co-incubated for 7 hrs in presence of TNFalpha by bright-glo lucifer
    Inhibition of NFkappaB (unknown origin) expressed in human A549 cells co-transfected with pNFkappaB-Luc vector assessed as reduction in TNFalpha-induced NFkappaB transcriptional activity co-incubated for 7 hrs in presence of TNFalpha by bright-glo lucifer
    [PMID: 31057738]
    A549 CC50
    4.1 μM
    Compound: 16
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay
    [PMID: 32045239]
    HepG2 IC50
    10.19 μM
    Compound: 3d
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTS assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTS assay
    [PMID: 28126437]
    HFF IC50
    16 nM
    Compound: 3j
    Antiapicomplexan activity against Toxoplasma gondii RH tachyzoites expressing yellow fluorescent protein infected in HFF cells after 72 hrs by fluorescence assay
    Antiapicomplexan activity against Toxoplasma gondii RH tachyzoites expressing yellow fluorescent protein infected in HFF cells after 72 hrs by fluorescence assay
    [PMID: 22970937]
    HL-60 IC50
    0.16 μM
    Compound: 65
    Cytotoxicity against human HL60 cells incubated for 3 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human HL60 cells incubated for 3 days by CellTiter-Glo luminescent assay
    [PMID: 31253529]
    Jurkat IC50
    0.48 μM
    Compound: 65
    Cytotoxicity against human Jurkat cells incubated for 3 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human Jurkat cells incubated for 3 days by CellTiter-Glo luminescent assay
    [PMID: 31253529]
    KG-1 IC50
    0.5 μM
    Compound: 65
    Cytotoxicity against human KG1 cells incubated for 3 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human KG1 cells incubated for 3 days by CellTiter-Glo luminescent assay
    [PMID: 31253529]
    Macrophage IC50
    5.2 μM
    Compound: 1, IMD-0354
    Cytotoxicity against mouse macrophage cell line J774.1 (ATCC TIB-67) for 3 days by Alamar Blue
    Cytotoxicity against mouse macrophage cell line J774.1 (ATCC TIB-67) for 3 days by Alamar Blue
    [PMID: 23211970]
    MDA-MB-231 IC50
    0.64 μM
    Compound: IMD-0354
    Antiproliferative activity against human MDA-MB-231 cells assessed as DNA content after 72 hrs by Hoechst 33258 staining based fluorescence assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as DNA content after 72 hrs by Hoechst 33258 staining based fluorescence assay
    [PMID: 30108896]
    MDA-MB-231 IC50
    0.85 μM
    Compound: IMD-0354
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTox green assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTox green assay
    [PMID: 30108896]
    MG-63 IC50
    48.72 μM
    Compound: IMD-0354
    Cytotoxicity against human MG-63 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human MG-63 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33530028]
    NALM-6 IC50
    0.63 μM
    Compound: 65
    Cytotoxicity against human NALM6 cells incubated for 3 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human NALM6 cells incubated for 3 days by CellTiter-Glo luminescent assay
    [PMID: 31253529]
    Platelet IC50
    0.57 μM
    Compound: 1; IMD-0354
    Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of collagen-induced platelet aggregation pre-incubated for 30 mins before collagen stimulation by aggregometry
    Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of collagen-induced platelet aggregation pre-incubated for 30 mins before collagen stimulation by aggregometry
    [PMID: 32345019]
    Platelet IC50
    3.64 μM
    Compound: 1; IMD-0354
    Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of TRAP6-induced platelet aggregation pre-incubated for 30 mins before TRAP6 stimulation by aggregometry
    Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of TRAP6-induced platelet aggregation pre-incubated for 30 mins before TRAP6 stimulation by aggregometry
    [PMID: 32345019]
    Platelet IC50
    4.73 μM
    Compound: 1; IMD-0354
    Antagonist activity P2X1 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation pre-incubated for 30 mins before ADP stimulation by aggregometry
    Antagonist activity P2X1 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation pre-incubated for 30 mins before ADP stimulation by aggregometry
    [PMID: 32345019]
    U2OS IC50
    50.91 μM
    Compound: IMD-0354
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 33530028]
    In Vitro

    IMD-0354 inhibits NF-κB activity in HMC-1 cells, resulting in complete repression of growth factor-independent proliferation of mast cells. When the DNA-binding activity of NF-κB is inhibited by treatment with IMD-0354, cell proliferation is completely suppressed. HMC-1 cells are incubated with increasing concentrations of IMD-0354 or STI571 for 24, 48, and 72 hours, and numbers and viability of cells are determined by a dye exclusion test and an MTT assay. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner. The inhibitory effect of IMD-0354 is remarkable, even at lower concentrations, when compared with that of STI571[1].
    IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM[2].

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

    In Vivo

    Daily administration with 5 mg/kg IMD-0354 significantly suppresses tumor expansion in nude mice implanted with established MDA-MB-231 tumors. In mice treated with IMD-0354, tumor progression is restrained[3]. The number of infiltrating cells in aqueous humor is 53.6±9.8×105, 72.5±17.0×105, 127.25±32.0×105, and 132.0±25.0×105 cells/mL in rats treated with 30, 10, 3, or 0 mg/kg of IMD-0354, respectively. The total protein concentrations of aqueous humor are 92.6±3.1 mg/mL, 101.5±6.8 mg/mL, 112.6±1.9 mg/mL, and 117.33±1.8 mg/mL in rats treated with 30, 10, 3, and 0 mg/kg of IMD-0354, respectively[4].

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

    Molecular Weight

    383.67

    Formula

    C15H8ClF6NO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)C2=CC(Cl)=CC=C2O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : ≥ 100 mg/mL (260.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6064 mL 13.0320 mL 26.0641 mL
    5 mM 0.5213 mL 2.6064 mL 5.2128 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

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    Concentration (final)

    C2

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    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: ≥ 2.5 mg/mL (6.52 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 (6.52 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (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
    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
    References
    Cell Assay
    [1]

    HMC-1 cells (2×105 cells/mL) are incubated with various concentrations of IMD-0354 (0.1, 0.5, 1, 5 and 10 uM), STI571, or pyrrolidine dithiocarbamate (PDTC) for the indicated hours, and viable cell numbers are calculated with the use of the trypan blue dye exclusion test at each time point. Cells (2×105 cells/mL) are incubated in phenol red free α-MEM containing 10% FCS (for HMC-1 and IC-2 cells) or 5% FCS (for CBhCMCs), and antibiotics with or without various concentrations of IMD-0354 (0.1, 0.5, 1, 5 and 10 uM), STI571, or PDTC. IC-2WT cells and CBhCMCs are incubated in the presence of 100 ng/mL recombinant rat or recombinant human SCF. One hundred microliters of cell suspension is applied to each well of 96-well culture plates and are incubated for 24, 48, and 72 hours. Before 4 hours from the end of the culture, 10 μL of 5 mg/mL MTT dissolved in PBS is added to each well. The reaction is stopped with the addition of 100 μLof 10% SDS in 0.01 N HCl. Absorbance is measured at 577 nm with ImmunoMini NJ-2300[1].

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

    Animal Administration
    [3][4]

    Mice[3]
    MDA-MB-231 cells are suspended in PBS (5×106 cells/100 μL mouse) and s.c. injected to the back of female BALB/c nude mice at the age of 4 to 5 weeks. After growth, the tumor is removed surgically and 100 mg of each established tumor is transplanted to the back of other female nude mice at the age of 4 weeks under ether anesthesia. IMD-0354 is suspended in saline and 5 mg/kg body weight IMD-0354 (suspended in 100 μL/mouse) is given to each mouse by i.p. injection once a day for 28 days after the implantation. Saline is injected in nude mice as a control. Estimated tumor volume (mm3) and tumor weight (mg) are calculated.
    Rats[4]
    Eight-week-old male Lewis rats (180-220 g) are used. Endotoxin-induced uveitis (EIU) is induced with subcutaneous injection with 200 μg LPS from Escherichia coli that has been diluted in 200 μL PBS. At the same time, the rats are injected intraperitoneally with 30, 10, or 3 mg/kg of IMD-0354, diluted in 500 μL of 0.5% CMC. Control EIU rats are intraperitoneally administered 500 μL of CMC alone. Naïve rats are used as controls. All experiments are performed in triplicate with five animals in each group.

    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, 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 2.6064 mL 13.0320 mL 26.0641 mL 65.1602 mL
    5 mM 0.5213 mL 2.6064 mL 5.2128 mL 13.0320 mL
    10 mM 0.2606 mL 1.3032 mL 2.6064 mL 6.5160 mL
    15 mM 0.1738 mL 0.8688 mL 1.7376 mL 4.3440 mL
    20 mM 0.1303 mL 0.6516 mL 1.3032 mL 3.2580 mL
    25 mM 0.1043 mL 0.5213 mL 1.0426 mL 2.6064 mL
    30 mM 0.0869 mL 0.4344 mL 0.8688 mL 2.1720 mL
    40 mM 0.0652 mL 0.3258 mL 0.6516 mL 1.6290 mL
    50 mM 0.0521 mL 0.2606 mL 0.5213 mL 1.3032 mL
    60 mM 0.0434 mL 0.2172 mL 0.4344 mL 1.0860 mL
    80 mM 0.0326 mL 0.1629 mL 0.3258 mL 0.8145 mL
    100 mM 0.0261 mL 0.1303 mL 0.2606 mL 0.6516 mL
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    IMD-0354 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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