IMD 0354

Catalog No.S2864 Batch:S286401

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Technical Data

Formula

C15H8ClF6NO2

Molecular Weight 383.67 CAS No. 978-62-1
Solubility (25°C)* In vitro Ethanol 77 mg/mL (200.69 mM)
DMSO 10 mg/mL (26.06 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]
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 (from reference)

Cell Assay:[1]
  • 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.

Animal Study:[2]
  • Animal Models

    ovalbumin (OVA)-sensitized mice

  • Dosages

    20 mg/kg

  • Administration

    Intraperitoneal

Customer Product Validation

Data from [Data independently produced by , , Int J Cancer, 2018, 144(1):200-209]

Data from [Data independently produced by , , Oncotarget, 2016, 7(20):29333-45]

Data from [Data independently produced by , , Oncotarget, 2016, 7(23):33796-808]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 471(4):576-81]

Selleck's IMD 0354 has been cited by 36 publications

Effects of tumor necrosis factor-α on glucose uptake in human granulosa cells under high androgen conditions [ Iran J Basic Med Sci, 2023, 26(8):912-918] PubMed: 37427330
Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] PubMed: 35704690
CD40×HER2 bispecific antibody overcomes the CCL2-induced trastuzumab resistance in HER2-positive gastric cancer [ J Immunother Cancer, 2022, 10(7)e005063] PubMed: 35851310
CD40×HER2 bispecific antibody overcomes the CCL2-induced trastuzumab resistance in HER2-positive gastric cancer [ J Immunother Cancer, 2022, 10(7)e005063] PubMed: 35851310
Norcantharidin overcomes vemurafenib resistance in melanoma by inhibiting pentose phosphate pathway and lipogenesis via downregulating the mTOR pathway [ Front Pharmacol, 2022, 13:906043] PubMed: 36034784
Norcantharidin overcomes vemurafenib resistance in melanoma by inhibiting pentose phosphate pathway and lipogenesis via downregulating the mTOR pathway [ Front Pharmacol, 2022, 13:906043] PubMed: 36034784
ACT001 suppressing M1 polarization against inflammation via NF-κB and STAT1 signaling pathways alleviates acute lung injury in mice [ Int Immunopharmacol, 2022, 110:108944] PubMed: 35728304
poly(I:C) synergizes with proteasome inhibitors to induce apoptosis in cervical cancer cells [ Transl Oncol, 2022, 18:101362] PubMed: 35151092
Manipulation of TAMs functions to facilitate the immune therapy effects of immune checkpoint antibodies [ J Control Release, 2021, 336:621-634] PubMed: 34246701
Novel Isoquinoline Alkaloid Litcubanine A - A Potential Anti-Inflammatory Candidate [ Front Immunol, 2021, 12:685556] PubMed: 34163484

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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