IMD 0354

Biological Activity

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

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.

Background References

1. Inhibition of IκB phosphorylation in cardiomyocytes attenuates myocardial ischemia/reperfusion injury.
   Onai et al.
   Cardiovasc.Res., 2004;63:51
2. A new IκB kinase β inhibitor prevents human breast cancer progression through negative regulation of cell cycle transition.
   Tanaka et al.
   Cancer Res., 2006;66:419
3. A novel NF-κB inhibitor, IMD-0354, supresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors.
   Tanaka et al.
   Hematopoiesis, 2005;105:2324
4. New antimicrobial bioactivity against multidrug resistant gram-positive bacteria of kinase inhibitor IMD0354.
   Escobar et al.
   Antibiotics, 2020;9:665

Product Datasheets