NOD2 Signaling Inhibitor II, GSK717

A cell-permeable benzimidazole diamide compound that acts as a potent, selective, reversible and muramyl dipeptide (MDP)-induced NOD2 (MDP/nucleotide-binding oligomerization domain 2)-mediated signaling inhibitor (IC₅₀ = 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells). Does not affect NOD1, TNFR1, or TLR-2-mediated responses. Also shown to diminish synergy between NOD2 and TLR2. Reduces MDP-stimulated IL-8, IL-6, IL-1β, and TNFα release in primary human monocytes (~5 µM), but does not affect Pam₂CSK₄-stimulated IL-8 release. Due to a lack of typical activation loop/hinge-binding motif it is unlikely to act as a kinase inhibitor. NOD1 Inhibitor, Nodinitib-1 (>Cat. No. 488004) is also available.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
NOD2

Reversible: yes

Target IC₅₀: 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Rickard, D.J., et al. 2013. PLoS ONE.D408, e69619.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)