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    IMD 0354
    IMD 0354

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0752
    CAS #: 978-62-1Purity ≥98%

    Description: IMD-0354 is a novel, potent and selective IKKβ inhibitor and blocks IκBα phosphorylation in NFκB (nuclear factor-kappaB) pathway. IMD-0354 (< 5 μM), down-regulated the expression of NF-κB and blocked the translocation of NF-κB to the nucleus in HMC-1 cells. Study from HMC-1 cells also showed that IMD-0354 inhibited cell proliferation in a time and dose dependent manner. In addition, IMD-0354 was also reported to arrest the cell cycle at the G0/G1 phase and decreased the ratio of cells in S and G2/M phases in HMC-1 cells. IMD-0354 can be potentially used for the treatment of atopic dermatitis as it significantly reduces the accumulation of inflammation damage and oxidative lesions.

    References: Blood. 2005 Mar 15;105(6):2324-31; Biochem Biophys Res Commun. 2004 Oct 8;323(1):242-8. 

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    Molecular Weight (MW)383.67
    FormulaC15H8ClF6NO2
    CAS No.978-62-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mg/mL (26.1 mM) 
    Water: <1 mg/mL
    Ethanol: 77 mg/mL (200.7 mM)
    Solubility (In vivo)2% DMSO+5% Tween 80+0.5% CMC Na: 3 mg/mL  
    SynonymsIMD0354; IMD 0354; IMD-0354 

    Chemical Name: N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide

    InChi Key: CHILCFMQWMQVAL-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H8ClF6NO2/c16-9-1-2-12(24)11(6-9)13(25)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6,24H,(H,23,25)

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


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    In Vitro

    In vitro activity: IMD-0354 (at a concentration of < 5 μM) inhibits the expression of NF-κB as well as the translocation of NF-κB to the nucleus in HMC-1 cells. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner in HMC-1 cells. IMD-0354 (0.5 μM) almost inhibits the proliferation of IC-2G559 cells and IC-2V814 cells. IMD-0354 (0.5 μM) results in arrest of the cell cycle at the G0/G1 phase in HMC-1 cells. IMD-0354 (1 μM) increases the number of cells with hypodiploid DNA content in HMC-1 cells. IMD-0354 (<1 μM) decreases the ratio of cells in S and G2/M phases in HMC-1 cells. IMD-0354 (1 μM) downregulates Cyclin D3 expression as well as pRb phosphorylation level in a time-dependent manner in HMC-1 cells. IMD-0354 (< 10 μM) has no influence on the signals of STAT3 and STAT6, whereas the phosphorylation of STAT1 and STAT5 is very slightly suppressed at high concentrations in HMC-1 cells. IMD-0354 suppresses the translocation of NF-κB to the nucleus in CBhCMCs after 24 hours in a dose-dependent manner. IMD-0354 inhibits 98.5% of NF-κB activity at a concentration of 10 μg/ml in HepG2 cells. IMD-0354 (1 μM) ameliorates the TNFα-induced decrease in the adiponectin concentration in the media, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. IMD-0354 (1 μM) restores the phosphorylation of Akt down-regulated by the TNFα treatment, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. IMD-0354 (1 μM) inhibits phosphorylation of IκBα and nuclear translocation of nuclear factor-kappa B (NF-κB) induced by tumor necrosis factor-α (TNF-α) in cultured cardiomyocytes. IMD-0354 (1 μM) significantly reduces TNF-α-induced production of interleukin-1β and monocyte chemoattractant protein-1 from cultured cardiomyocytes.


    Kinase Assay: IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2±0.3 uM.


    Cell Assay: Cells (at the concentration of 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, 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 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) dissolves in PBS is added to each well. The reaction is stopped with the addition of 100 μL of 10% SDS in 0.01 N HCl. Absorbance is measured at 577 nm with ImmunoMini NJ-2300.

    In VivoIMD-0354 (5 mg/kg) significantly decreases NF-κB, but the magnitude of the decrease is lower than with 20 mg/kg IMD-0354 in lungs of OVA-sensitized mice. IMD-0354 (20 mg/kg) ameliorates airway hyperresponsiveness and reduces the numbers of bronchial eosinophils and mucus-producing cells in OVA-sensitized mice. IMD-0354 (20 mg/kg) also reduces the total numbers of cells and eosinophils in bronchoalveolar lavage fluid in OVA-sensitized mice. IMD-0354 (20 mg/kg) inhibits the production of Th2 cytokines such as interleukin (IL)-5 and IL-13 and eotaxin in the airways and/or lungs of OVA-sensitized mice, but it does not affect the restoration of Th1 cytokines such as IL-12 and interferon-gamma under the same experimental conditions. IMD-0354 (20 mg/kg) results in a partial decrease in serum IgE concentration in OVA-sensitized mice. IMD-0354 significantly decreases the plasma glucose levels in KKAy mice treated with and fed an HF diet in an dose-dependent manner without influence of body weight. IMD-0354 (10 mg/kg) results in a significant dose-dependent reduction of the infarction area/area at risk ratio and the preservation of fractional shortening ratio.
    Animal modelOvalbumin (OVA)-sensitized mice
    Formulation & DosageDissolved in  5% carboxymethylcellulose; 20 mg/kg; i.p. injection
    ReferencesBlood. 2005 Mar 15;105(6):2324-31; Biochem Biophys Res Commun. 2004 Oct 8;323(1):242-8.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    IMD 0354

     
    IMD 0354
    Inhibitory effect of IMD-0354 on cell proliferation of HMC-1 cells. Blood. 2005 Mar 15;105(6):2324-31.
     
    IMD 0354
    Inhibitory effect of IMD-0354 on proliferation of neoplastic mast cells. Blood. 2005 Mar 15;105(6):2324-31.
    IMD 0354
    Suppressive effect of IMD-0354 on cell cycle progression of HMC-1 cells. Blood. 2005 Mar 15;105(6):2324-31.
     
    IMD 0354
    Cyclin D3 expression in HMC-1 cells down-regulated by treatment with IMD-0354. Blood. 2005 Mar 15;105(6):2324-31.
     
    IMD 0354
    Signaling pathways involved in NF-κB activation in HMC-1 cells. Blood. 2005 Mar 15;105(6):2324-31.


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