IMD 0354

Catalog No.S2864 Batch:S286402

Technical Data

Formula

C₁₅H₈ClF₆NO₂

Molecular Weight

383.67

CAS No.

978-62-1

Solubility (25°C)*

In vitro

DMSO

76 mg/mL (198.08 mM)

Ethanol

76 mg/mL (198.08 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	1.9mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 38 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.9mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 38 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.)

Preparing Stock Solutions

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-2^G559 cells and IC-2^V814 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-2^WT 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

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-2^WT 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

References

[4] Onai Y, et al. Cardiovasc Res, 2004, 63(1), 51-59.

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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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