Nodinitib-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 NOD1 抑制剂，IC50 为 0.56 uM。

A potent and selective NOD1 inhibitor with IC50 of 0.56 uM; no inhibition on NOD1, TNFα (IC50> 20 uM) and dIKKγ/NEMO, MYD88, FLIP, CARD6, APAF1 or NLRC4; inhibits IL-8 production induced by NOD1 ligand and γ-tri-DAP-induced expression of the prototypical NF-κB target gene IκBα at the mRNA level.

Nodinitib-1 selectively inhibits IL-8 production induced by NOD1 ligand. Nodinitib-1 also inhibits γ-tri-DAP-induced expression of the prototypical NF-κB target gene IκBα at the mRNA level. Nodinitib-1 inhibits γ-tri-DAP-dependent activation of NF-κB (IκBα 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-1β, IL-6 and TNFα elicited by γ-tri-DAP (but not by LPS), without causing cytoxicity. Nodinitib-1 is identified as NOD1-selective molecules from an HTS campaign involving ~290,000 compounds. Nodinitib-1 inhibits γ-tri-DAP-stimulated luciferase production in HEK 293T cells, which has endogenous NOD1 levels at submicromolar concentration as determined in a NF-κB-linked reporter assay.

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ML-130 | CID-1088438 | Nodinitib

NF-κB

NOD

NOD1|NOD2|TNF-α

Inflammation/Immunology

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799264-47-4

287.3369

C14H13N3O2S

>98% (HPLC)

DMSO: 20 mg/mL

NC1=NC2=CC=CC=C2N1S(=O)(C3=CC=C(C)C=C3)=OInChI=1S/C14H13N3O2S/c1-10-6-8-11(9-7-10)20(18,19)17-13-5-3-2-4-12(13)16-14(17)15/h2-9H,1H3,(H2,15,16)

1H-Benzimidazol-2-amine, 1-[(4-methylphenyl)sulfonyl]-

(-20℃)

With Ice Pack

≥ 2 years