2. Apoptosis Immunology/Inflammation Metabolic Enzyme/Protease
  3. TNF Receptor Interleukin Related Arginase PD-1/PD-L1
  4. Naamidine J

Naamidine J 是一种在海绵中发现的咪唑类生物碱。Naamidine J 通过与蛋白 CSE1L (KD = 5.41 μM) 结合来抑制炎症。Namidine J 显著抑制促炎因子 (TNF-α、IL-1β 和 IL-6) 的表达，并上调抗炎因子 (CD206 和 Arg-1)。Namidine J 抑制 PD-L1 并展示出抗癌活性。Namidine J 显著减轻小鼠肺组织水肿、炎症细胞浸润和细胞因子风暴。Naamidine J 可用于急性肺损伤和肿瘤的免疫微环境的研究。

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Naamidine J

Naamidine J Chemical Structure

CAS No. : 2227550-73-2

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Naamidine J 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Naamidine J is an imidazole-type alkaloids discovered in a sponge. Naamidine J inhibits inflammation by binding to the protein CSE1L (KD = 5.41 μM). Namidine J significantly inhibits the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and upregulates anti-inflammatory factors such as CD206 and Arg-1. Namidine J inhibits PD-L1 and shows antitumor activity. Namidine J significantly reduces pulmonary tissue edema, inflammatory cell infiltration and cytokine storm in mice. Namidine J can be used for the research on the immune microenvironment of acute lung injury and tumors[1][2].

IC50 & Target[2]

IL-1β

 

IL-6

 

体外研究
(In Vitro)

Naamidine J (5 μM, 24 小时) 对 K562 细胞具有细胞毒性，IC50 为 11.3 μM，但对巨噬细胞和 RKO 细胞无毒性 (IC50 > 40 μM)[1][2]。
Naamidine J (10 μM，24 小时) 可降低 RKO 细胞和 PDAC 细胞中的 PD-L1 表达[1][3]。
Naamidine J (1-5 μM, 5 小时) 可抑制 LPS (HY-D1056) 诱导的 RAW264.7 巨噬细胞中的炎症反应[2]。
Naamidine J (5 μM, 5 小时) 可抑制 CSE1L 介导的转录因子 SP1 核易位。 LPS诱导的巨噬细胞[2]。
Naamidine J (10 μM，24 小时) 可恢复 CD8+ T 细胞的细胞毒性，并显著降低 PDAC 细胞 (MIA-PaCa2、BxPC-3) 的存活率[3]。

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

Naamidine J 相关抗体:

Western Blot Analysis[1]

Cell Line: RKO cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Had a certain inhibitory effect on PD-L1 expression.

ELISA Assay[1]

Cell Line: RAW264.7 cells
Concentration: 1, 2 and 5 μM
Incubation Time: Pre-treatment for 3 hours, followed by co-stimulation with LPS for 2 hours
Result: Exhibited concentration-dependent inhibition of TNF-α release.

RT-PCR[1]

Cell Line: RAW264.7 cells
Concentration: 1, 2 and 5 μM
Incubation Time: Pre-treatment for 3 hours, followed by co-stimulation with LPS for 2 hours
Result: Inhibited pro-inflammatory factors (TNF-α, IL-1β, IL-6), and promoted anti-inflammatory factors (CD206, Arg-1).

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 5 μM
Incubation Time: Pre-treatment for 3 hours, followed by co-stimulation with LPS for 2 hours
Result: Resulted in the accumulation of SP1 in the cytoplasm.
Enhanced the interaction between CSE1L and SP1.
体内研究
(In Vivo)

Naamidine J (10-20 mg/kg，腹腔注射，每日一次，连续3天) 显著减轻小鼠 LPS 诱发的急性肺损伤，并减轻肺水肿[2]。
Naamidine J (30 mg/kg，腹腔注射，每三天一次，共 28 天) 在 NAT10 高表达的荷瘤小鼠中，显著提高 CD8+T 细胞亚群比例，降低 CD8+Th 细胞亚群比例[3]。

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

Animal Model: Acute lung injury model established in mice[2]
Dosage: 10 and 20 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 3 days
Result: Significantly reduced the increase in lung organ coefficient induced by LPS and alleviate pulmonary edema.
Significantly improved the pathological damage of lung tissue and reduce the infiltration of inflammatory cells.
Significantly reduced the protein levels of TNF-α in serum and lung tissue, as well as the mRNA expression of various inflammatory factors.
Reduced the proportion of pro-inflammatory M1-type macrophages in the lung tissue and increased the proportion of anti-inflammatory M2-type macrophages.
Animal Model: PanO2 xenograft model established in four-week-old female C57BL/6 mice (18 to 20 g)[3]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.), once every three days for 28 days
Result: Significantly inhibited tumor growth in the Nat10-OE group.
Reversed T cell exhaustion and restores anti-tumor function.
Increased the infiltration of CD8+ T cells, reduced the PD-1 with IFNγ and exhausted phenotype, and increased the PD-1-IFNγ+ cytotoxic phenotype.
分子量

477.51

Formula

C25H27N5O5
CAS 号
结构分类
初始来源

Pericharax heteroraphis
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.
纯度 & 产品资料
参考文献

Naamidine J 相关分类

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  • 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:

Naamidine J2227550-73-2TNF ReceptorInterleukin RelatedArginasePD-1/PD-L1Tumor Necrosis Factor ReceptorTNFRILPD-1/Programmed death-ligand 1Imidazole-type alkaloidsacute Lung Injurymice modelMacrophage-mediated InflammationInhibitorinhibitorinhibit

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