For research use only.
Molecular Weight(MW): 383.67
IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.
Selleck's IMD 0354 has been cited by 17 publications
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(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.
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
|Description||IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.|
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.  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. 
|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.  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. |
|In vitro||Ethanol||77 mg/mL (200.69 mM)|
|DMSO||10 mg/mL (26.06 mM)|
|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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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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