IMD 0354

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Description: Inhibitor of IKKβ; also exhibits antibacterial activity
Chemical Name: N-[3,5-Bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (6)
Reviews (1)

Biological Activity for IMD 0354

IMD 0354 is an inhibitor of IκB kinase-β (IKKβ) that blocks NF-κB nuclear translocation. Attenuates myocardial ischemia/reperfusion injury by decreasing expression of adhesion molecules ICAM-1 and P-selectin and inhibiting cytokine and chemokine production in cardiomyocytes. Induces G0/G1 cell cycle arrest and apoptosis in HMC-1 and breast cancer cells. Antagonist at P2X1, P2X4 and P2X7 receptors (IC50 values are 19, 156 and 175 nM respectively). Inhibits platelet aggregation induced by collagen in vitro. Exhibits potent antibacterial activity against MRSA in C. elegans model (MIC = 0.06 μg/mL). Selective aquaporin 4 inhibitor (IC50 values are 210 nM, 390 nM and 420 nM at rat, mouse and human receptors, respectively).

Technical Data for IMD 0354

M. Wt 383.67
Formula C15H8ClF6NO2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 978-62-1
PubChem ID 5081913
InChI Key CHILCFMQWMQVAL-UHFFFAOYSA-N
Smiles OC1=C(C=C(Cl)C=C1)C(=O)NC1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for IMD 0354

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.36 100
ethanol 38.36 100

Preparing Stock Solutions for IMD 0354

The following data is based on the product molecular weight 383.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.61 mL 13.03 mL 26.06 mL
5 mM 0.52 mL 2.61 mL 5.21 mL
10 mM 0.26 mL 1.3 mL 2.61 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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References for IMD 0354

References are publications that support the biological activity of the product.

Onai et al (2004) Inhibition of IκB phosphorylation in cardiomyocytes attenuates myocardial ischemia/reperfusion injury. Cardiovasc.Res. 63 51 PMID: 15194461

Tanaka et al (2006) A new IκB kinase β inhibitor prevents human breast cancer progression through negative regulation of cell cycle transition. Cancer Res. 66 419 PMID: 16397257

Tanaka et al (2005) A novel NF-κB inhibitor, IMD-0354, supresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors. Hematopoiesis 105 2324

Escobar et al (2020) New antimicrobial bioactivity against multidrug resistant gram-positive bacteria of kinase inhibitor IMD0354. Antibiotics 9 665 PMID: 33019726


If you know of a relevant reference for IMD 0354, please let us know.

View Related Products by Product Action

View all IκB Kinase Inhibitors

Keywords: IMD 0354, IMD 0354 supplier, inhibitors, inhibits, IKK-2, IKK, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, NF-κB, NF-kappaB, NF-kB, Cytokine, Signaling, Signalling, Transcription, Factors, IMD0354, AER270, IkB, Kinase, NF-kB/IkB, P2X, Receptors, Antibiotics, Aquaporins, 2611, Tocris Bioscience

6 Citations for IMD 0354

Citations are publications that use Tocris products. Selected citations for IMD 0354 include:

Zhang et al (2018) Tumor-Stroma IL1β-IRAK4 Feedforward Circuitry Drives Tumor Fibrosis, Chemoresistance, and Poor Prognosis in Pancreatic Cancer. Cancer Res 78 1700 PMID: 29363544

Chen et al (2015) Pentoxifylline Attenuates Proteinuria in Anti-Thy1 Glomerulonephritis via Downregulation of Nuclear Factor-κB and Smad2/3 Signaling. J Mol Neurosci 21 276 PMID: 25879629

Escobar et al (2020) New antimicrobial bioactivity against multidrug resistant gram-positive bacteria of kinase inhibitor IMD0354. Antibiotics 9 665 PMID: 33019726

Zwicker et al (2015) Interleukin 34: a new modulator of human and experimental inflammatory bowel disease. Clin Sci (Lond) 129 281 PMID: 25896238


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Reviews for IMD 0354

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IMD 0354 ameliorates LPS-induced TNFa production.
By Anonymous on 12/11/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Macrophages

RAW macrophages were incubated with 5 μM IMD 0354 for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with IMD 0354.

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