2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. NOD1/2 antagonist-1

NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).

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NOD1/2 antagonist-1 Chemical Structure

NOD1/2 antagonist-1 Chemical Structure

CAS No. : 2704623-69-6

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NOD1/2 antagonist-1 Related Antibodies

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Description

NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX)[1].

IC50 & Target

NOD1

1.13 μM (IC50)

NOD2

0.77 μM (IC50)

In Vitro

NOD1/2 antagonist-1 (compound 36b) (0-10 μM, 3 h) inhibits C12-iE-DAP-induced or MDP-induced NF-κB activation[1].
NOD1/2 antagonist-1 (0-10 μM, 1 h) suppresses inflammation via NOD1 and NOD2 activation[1].
NOD1/2 antagonist-1 (0-10 μM, 1 h) consistently and dose-dependently reduces the transcription of IL-6, TNF-α and IL-8, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NOD1/2 antagonist-1 Related Antibodies

Cell Viability Assay

Cell Line: HEK-Blue hNOD1 and HEK-Blue hNOD2 cells[1]
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 3 h
Result: Inhibited C12-iE-DAP-induced or MDP-induced NF-κB activation, and had no or little effect on cell growth.

Western Blot Analysis

Cell Line: THP-1 cells[1]
Concentration: 1, 10 μM
Incubation Time: 1 h
Result: Prevented the increases in p-RIP2, p-IKKα/β, p-p65, p-p38, and p-JNK and the degradation of IκBα in a dose-dependent manner, and blocked NOD1-and NOD2-mediated inflammatory cytokine secretion in THP-1 cells.

RT-PCR

Cell Line: THP-1 cells[1]
Concentration: 1, 10 μM
Incubation Time: 1 h
Result: Consistently and dose-dependently reduced the transcription of IL-6, TNF-α and IL-8 stimulated by C12-iE-DAP or MDP, respectively.
In Vivo

NOD1/2 antagonist-1 (compound 36b) (50 mg/kg, IV, once every other day, for 16 days) improves the antitumor efficacy of PTX in B16 tumor-bearing model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (6-8 weeks old, male, B16 tumor-bearing model, 4 groups, n = 7 each group)[1]
Dosage: 50 mg/kg (36b), 50 mg/kg (36b) + 12 mg/kg (PTX) (formulated in DMSO/Cremophor EL/saline at 5:5:90(v:v:v))
Administration: IV, once every other day (36b), once every 4 days (PTX), for 16 days
Result: Significantly reduced tumor growth compared with PTX treatment alone, and the tumor weight inhibitory rate increased from 64.07% to 85.46%.
Molecular Weight

663.03

Formula

C32H28ClF5N4O4
CAS No.
SMILES

O=C(C1=C(C=C2C(N(C=NC2=C1)CC(N3CCCC(F)(C3)F)=O)=O)C4=CC(Cl)=CC=C4)NCCCOC5=CC=C(C=C5)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NOD1/2 antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NOD1/2 antagonist-12704623-69-6NOD-like Receptor (NLR)B16 tumorAntitumor efficacyTHP-1 cellsInhibitorinhibitorinhibit

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