Bioactivity:

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 _M) inhibits the release of IL-8, IL-6, TNF_ and IL-1_ in primary human monocytes stimulated with MDP[1]. [1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

CAS nr:

1595278-21-9

Purity:

98%

Molecular Weight:

452,55

SMILES:

O=C(NC1=CC=C2C(CCC2)=C1)CN3C4=CC=CC=C4N=C3CCN(C)C(C5=CC=CC=C5)=O

Formula:

C28H28N4O2

Pathway:

Immunology/Inflammation,NF-_b,Immunology/Inflammation

Target:

NOD,NOD,IL Receptor