Nodinitib-1

799264-47-4

C14H13N3O2S

DMSO : 20 mg/mL (69.60 mM; Need ultrasonic and warming)

Immunology/Inflammation

Nodinitib-1 (ML130; CID-1088438) is a NOD1 inhibitor with an IC₅₀ of 0.56 uM. IC50 & Target: IC50: 0.56 uM (NOD1)^[1] In Vitro: Nodinitib-1 selectively inhibits IL-8 production induced by NOD1 ligand. Nodinitib-1 also inhibits gamma-tri-DAP-induced expression of the prototypical NF-kappaB target gene IkappaBalpha at the mRNA level. Nodinitib-1 inhibits gamma-tri-DAP-dependent activation of NF-kappaB (IkappaBalpha phosphorylation and degradation) and MAPK (p38 phosphorylation) signalings, without affecting Akt survival pathway. Nodinitib-1 selectively inhibits responses of primary dendritic cells to NOD1 ligand. Nodinitib-1 reduces cell surface expression of co-stimulatory molecules CD83, CD86 and HLA-DR and also inhibits expression of IL-1beta, IL-6 and TNFalpha elicited by gamma-tri-DAP (but not by LPS), without causing cytoxicity^[1]. Nodinitib-1 is identified as NOD1-selective molecules from an HTS campaign involving ca.290, 000 compounds. Nodinitib-1 inhibits gamma-tri-DAP-stimulated luciferase production in HEK 293T cells, which has endogenous NOD1 levels at submicromolar concentration as determined in a NF-kappaB-linked reporter assay^[2].