IMD 0354

For research use only.

Catalog No.S2864 Synonyms: IKK2 Inhibitor V

21 publications

IMD 0354 Chemical Structure

CAS No. 978-62-1

IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

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Selleck's IMD 0354 has been cited by 21 publications

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Biological Activity

Description IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.
Targets
IKKβ [1]
In vitro

IMD-0354 (< 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. [1] IMD-0354 inhibits 98.5% of NF-κB activity at a concentration of 10 μg/ml in HepG2 cells. [2] 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. [3] 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. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HFF cells NUTQfWlGTnWwY4Tpc44h[XO|YYm= MXq3NkBp NEHDc5NCdnSrYYDpZ49ueGyneHHuJIFkfGm4aYT5JIFo[Wmwc4SgWI95d3CuYYPtZUBod26maXmgVmghfGGlaIn6c4l1\XNiZYjwdoV{e2mwZzD5[Yxtd3diZnz1c5Jme2OnboSgdJJwfGWrbjDpcoZm[3SnZDDpckBJTkZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME2wMlAyPiEQvF2= MlnqNlI6PzB7M{e=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin D1 / Cyclin D2 / Cyclin D3 / Cyclin E / Bcl-2 ; 

PubMed: 24510578     


The expression of cyclins D1, D2, and D3 was suppressed in MSTO-211H cells and that of cyclin D3 was decreased in NCI-H28 and NCI-H2052 cells by treatment with IMD-0354 (1 μmol/L) for 24 h. In NCI-H2052 cells, Bcl-2 expression was suppressed by IMD-0354 treatment (representative of three different experiments).

p-IκBα / IκBα ; 

PubMed: 24531845     


Involvement of constitutive NF-κB activation in tumorigenic proliferation was examined using 2 different cell lines, namely, ER-positive MCF-7 and ER-negative HMC1-8 cells. After serum starvation, the cells were incubated in complete culture media with the indicated concentrations of IMD-0354 for 16 h; whole cell lysates were obtained to detect the IκB phosphorylation responsible for NF-κB activation by Western blot analysis. The constitutive phosphorylation of IκB and the downregulation of the phosphorylated form by IMD-0354 were detected in both cells. Concerning the expression of IκBα, 2 immunoreactive bands were identified in lysates from the HMC1-8 cells. The upper band was estimated as intact IκBα and the lower one was its partial proteolytic product.

24510578 24531845
Immunofluorescence
NF-κB p65 ; 

PubMed: 29332242     


Effect of IMD0354 treatment on NF-κB nuclear translocation and phospho-IκBα expression on 24 h serum-starved HUVEC. Inhibitory effect of IMD0354 (10 ng/ml) on NF-κB (red) nuclear translocation (pink).

VEGFA; 

PubMed: 29332242     


Immunofluorescent detection of VEGF-A (green) in HUVEC treated with IMD0354 (10, 5, 2.5 ng/ml). Cell nuclei visualized with DAPI staining (blue).

29332242
Growth inhibition assay
Cell viability; 

PubMed: 24014113     


Viability of MDA-MB-231 cells was assessed by MTT assay after treatment with IMD-0354 for 24 h (A), 48 h (B) and 72 h (C). Viability of 4T1 cells was assessed by MTT assay after treatment with IMD-0354 for 24 h (E), 48 h (F) and 72 h (G). Data are shown as mean ± SEM.

24014113
In vivo IMD-0354 at 5 mg/kg also 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. [2] 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. [3] 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. [4]

Protocol

Cell Research:[1]
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  • Cell lines: HMC-1, IC-2, CBhCMCs cells
  • Concentrations: 10 μM
  • Incubation Time: 72 hours
  • Method: 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, 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.
    (Only for Reference)
Animal Research:[2]
- Collapse
  • Animal Models: ovalbumin (OVA)-sensitized mice
  • Dosages: 20 mg/kg
  • Administration: Intraperitoneal
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (26.06 mM)
Water Insoluble
Ethanol '77 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+5% Tween 80+0.5% CMC Na
For best results, use promptly after mixing.
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.67
Formula

C15H8ClF6NO2

CAS No. 978-62-1
Storage powder
in solvent
Synonyms IKK2 Inhibitor V
Smiles C1=CC(=C(C=C1Cl)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)C(F)(F)F)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID