5.33718

NOD2 Signaling Inhibitor II, GSK717

• Synonym(s): NOD2 Signaling Inhibitor II, GSK717, N-(2-(1-(2-(2,3-Dihydro-1H-inden-5-ylamino)-2-oxoethyl)-1H-benzo[d]imidazol-2-yl)ethyl)-N-methylbenzamide, Nucleotide-binding Oligomerization Domain 2 Signaling Inhibitor II, MDP/NOD2-Mediated Signaling Inhibitor, GSK 717
• Empirical Formula (Hill Notation): C₂₈H₂₈N₄O₂
• CAS Number: 1595278-21-9
• Molecular Weight: 452.55
• MDL number: MFCD32671947
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
NOD2

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable