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Submit ReviewIMD 0354
Description: Inhibitor of IKKβ; also exhibits antibacterial activity
Chemical Name: N-[3,5-Bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide
Purity: ≥99% (HPLC)
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.
| 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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Product Datasheets for IMD 0354
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.
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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:
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
Kong et al (2015) Tumor-suppressive microRNA-497 targets IKKβ to regulate NF-κB signaling pathway in human prostate cancer cells. Am J Cancer Res 5 1795 PMID: 26175947
Cataldi et al (2015) Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1. Virology 485 340 PMID: 26331681
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
Do you know of a great paper that uses IMD 0354 from Tocris? Please let us know.
Reviews for IMD 0354
Average Rating: 5 (Based on 1 Review.)
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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.
