IMD 0354

Catalog No.S2864

IMD 0354 Chemical Structure

Molecular Weight(MW): 383.67

IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 90 In stock
USD 110 In stock
USD 470 In stock
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Cited by 8 Publications

5 Customer Reviews

  • (B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, **P < 0.01 and ***P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.

    Int J Cancer, 2018, 144(1):200-209. IMD 0354 purchased from Selleck.

    (C) ELISA showed that the elevated IL-8 was significantly inhibited in HUVEC-shCD109 when pretreated with SB525334, LY294002, or IMD 0354. GAPDH served as a loading control for WB. Data shown as mean ± SD were from triplicates of three independent experiments. **P < 0.01 by t test. CM, conditioned media; NC, negative control.

    Oncotarget, 2016, 7(20):29333-45. IMD 0354 purchased from Selleck.

  • E. MΦ-THP-1 cells were pretreated with IMD 0354 (3μM) for 30 minutes, then incubated with core protein for 3 and 6 hours, cell lysates were analyzed by immunoblotting to examine the A20 expression.

    Oncotarget, 2016, 7(23):33796-808. IMD 0354 purchased from Selleck.

    Dystrophic muscle fibroblasts treated with 5 μM IMD-0354 or vehicle were incubated in serum-deprived medium (1% FBS) with (+) or without (−) TGF-β1 (10 ng/ml) for 24 h. Cells containing EdU incorporated into the nucleus were scored as EdU-positive (D, up panel), and the percentage of EdU-positive cells was calculated (D, down panel). The scale bar is 50 μm. Values are expressed as the mean ± SD, n = 3. #P < 0.05 versus cells in grow medium (10% FBS); *P < 0.05 versus cells under serum deprivation without TGF-β1 and IMD-0354 treatments; **P < 0.05.

    Biochem Biophys Res Commun, 2016, 471(4):576-81. IMD 0354 purchased from Selleck.

  • IMD-0354 attenuates TGF-β1-mediated survival and proliferation in dystrophic muscle fibroblasts. (A) Dystrophic muscle fibroblasts were cultured in culture medium or serum-deprived medium with (+) or without (−) TGF-β1 (10 ng/ml) and various concentrations of IMD-0354 as indicated for 24 h. Cell viability was determined by CCK-8 assay. (B) Dystrophic muscle fibroblasts were cultured as described in A. Western blot analysis was applied to determine the protein abundance of cleaved caspase-3, cleaved PARP and Bcl-2. (C) Dystrophic muscle fibroblasts were cultured in culture medium or serum-deprived medium (1% FBS) with (+) or without (−) TGF-β1 (10 ng/ml) and various concentrations of IMD-0354 as indicated for 24 h. The protein abundance of cyclin D1 and PCNA was determined by Western blot. (D) Dystrophic muscle fibroblasts treated with 5 μM IMD-0354 or vehicle were incubated in serum-deprived medium (1% FBS) with (+) or without (−) TGF-β1 (10 ng/ml) for 24 h. Cells containing EdU incorporated into the nucleus were scored as EdU-positive (D, up panel), and the percentage of EdU-positive cells was calculated (D, down panel). The scale bar is 50 μm. Values are expressed as the mean ± SD, n = 3. #P < 0.05 versus cells in grow medium (10% FBS); *P < 0.05 versus cells under serum deprivation without TGF-β1 and IMD-0354 treatments; **P < 0.05.

    Biochem Biophys Res Commun, 2016, 471(4):576-81.. IMD 0354 purchased from Selleck.

Purity & Quality Control

Choose Selective IκB/IKK Inhibitors

Biological Activity

Description IMD-0354 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 MmrQSpVv[3Srb36gZZN{[Xl? MYi3NkBp MVzBcpRq[XCrY3;tdIxmgGGwIHHjeIl3cXS7IHHnZYlve3RiVH;4c5Bt[XOvYTDnc45lcWliUligeIFkcHm8b3n0[ZMh\XiycnXzd4lv\yC7ZXzsc5ch\my3b4Lld4NmdnRicILveIVqdiCrbn\lZ5Rm\CCrbjDISmYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OD1yLkCxOkDPxE1? NIDjPI4zOjl5MEmzOy=>

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • Animal Models: ovalbumin (OVA)-sensitized mice
  • Formulation: 5% carboxymethylcellulose
  • Dosages: 20 mg/kg
  • Administration: Intraperitoneal
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 77 mg/mL (200.69 mM)
DMSO 10 mg/mL (26.06 mM)
Water Insoluble
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 N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID