NOD1/2 antagonist-1 (compound 36b) 是一种有效的NOD1/2双拮抗剂，其IC50值分别为 1.13 (NOD1) 和 0.77 μM (NOD2)。NOD1/2 antagonist-1 有可接受的 T1/2(67.6 min)。NOD1/2 antagonist-1 (compound 36b) 可提高紫杉醇 (PTX) 的抗肿瘤作用。
| 生物活性 | NOD1/2 antagonist-1 (compound 36b) is a potentNOD1/2(nucleotide-binding
oligomerization domain-like receptor 1/2) dual antagonist, withIC50values 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) |
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体外研究
(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. |
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体内研究
(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%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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