2704623-69-6
2704623-69-6 structure
- Name: NOD1/2 antagonist-1
- Chemical Name: NOD1/2 antagonist-1
- CAS Number: 2704623-69-6
- Molecular Formula: C32H28ClF5N4O4
- Molecular Weight: 663.03
- Catalog: Signaling Pathways Immunology/Inflammation NOD-like Receptor (NLR)
- Create Date: 2022-06-03 12:05:43
- Modify Date: 2024-01-12 10:04:03
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NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-bindingoligomerization 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].
| Name | NOD1/2 antagonist-1 |
|---|
| Description | NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-bindingoligomerization 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]. |
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| Related Catalog | |
| 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]. 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]. 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%. |
| References |
| Molecular Formula | C32H28ClF5N4O4 |
|---|---|
| Molecular Weight | 663.03 |