NOD1/2 antagonist-1

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NOD1/2 antagonist-1 

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。

NOD1/2 antagonist-1

NOD1/2 antagonist-1 Chemical Structure

CAS No. : 2704623-69-6

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生物活性

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)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

Shanghai Jinpan Biotech Co Ltd 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%.

分子量

663.03

Formula

C32H28ClF5N4O4
CAS 号

2704623-69-6
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.
参考文献

  • [1]. Ma Y, Yang J, Wei X, et al. Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy. Eur J Med Chem. 2020;207:112723.

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