2. Immunology/Inflammation NF-κB Apoptosis
  3. Interleukin Related NF-κB AP-1 MDM-2/p53 Apoptosis
  4. Girolline

Girolline 是一种蛋白质合成抑制剂，也是 eIF5A 功能调节剂。Girolline 通过干扰 eIF5A 与核糖体结合引发核糖体停滞。Girolline 也能抑制 IL-6、IL-8 的产生，诱导肿瘤细胞细胞周期阻滞。Girolline 可用于炎症性疾病、实体瘤、白血病以及疟疾的相关研究。

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Girolline

Girolline Chemical Structure

CAS No. : 110883-46-0

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Girolline 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Girolline is a protein synthesis inhibitor and a functional modulator of eIF5A. Girolline induces ribosome stalling by interfering with the binding of eIF5A to ribosomes. Girolline also inhibits the production of IL-6 and IL-8, and induces cell cycle arrest in tumor cells. Girolline is applicable to research related to inflammatory diseases, solid tumors, leukemia and malaria[1][2][3][4].

IC50 & Target[1]

IL-6

 

IL-8

 

体外研究
(In Vitro)

Girolline (0.08-40000 ng/mL; 4.5 h) 可抑制鞭毛蛋白诱导的 CHO-K1-TLR5 细胞中 TLR5 NF-κB 荧光素酶报告基因活性[1]。
Girolline (2 μg/mL; 7 h) 可强效抑制鞭毛蛋白诱导的 THP1 来源巨噬细胞中 IL-8 的分泌以及 NF-κB/AP-1 的活性[1]。
Girolline (2 μg/mL; 7 h) 可阻断人外周血单个核细胞 (PBMCs) 中由鞭毛蛋白诱导的 IL-6 和 IL-8 分泌[1]。
Girolline (8-5000 ng/mL；7 h) 可在 HEK293 报告细胞中剂量依赖性地抑制由多种 TLR、IL-1β 及 TNF-α 诱导的 NF-κB/AP-1 活性，在浓度 ≥200 ng/mL 时可观察到显著抑制作用[1]。
Girolline (50 μM; 24 h) 可诱导 FL、HeLa 和 A549 肿瘤细胞系发生 G2/M 期细胞周期阻滞，其中在 FL 细胞中的作用效果最为显著[2]。
Girolline (5-50 μM; 24 h) 可在 FL 细胞中诱导多泛素化 p53 呈浓度依赖性累积[2]。
Girolline (0.1-1.0 μM; 1-4 days) 可在人 293 细胞中诱导呈剂量和时间依赖性的 G2 期阻滞，其中以 1.0 μM 作用 48 h 时 G2/M 期细胞的累积最为显著，而延长处理时间会导致凋亡细胞死亡增加[3]。
Girolline (10-300 μM; 1 h) 可在 HEK293T 细胞中剂量依赖性地抑制羟腐胺化 eIF5A 与核糖体之间的相互作用[4]。
Girolline (1-5 μM; 16 h) 可在 HEK293T 细胞中选择性抑制含 AAA 编码 Lys (而非 AAG 编码 Lys) 的序列的翻译过程，且 AAA 序列越长，抑制作用越强[4]。

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

Girolline 相关抗体:

Cell Cycle Analysis[2]

Cell Line: FL, HeLa, A549
Concentration: 50 μM
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest in FL cells.
Induced G2/M cell cycle arrest to a lesser extent in HeLa and A549 cells.

Cell Cycle Analysis[3]

Cell Line: human 293 cells
Concentration: 0.1 μM, 0.5 μM, 1.0 μM; 1 μM
Incubation Time: 1 day, 2 days, 3 days, 4 days
Result: Increased the percentage of cells in G2/M phase from 7.8% to 32.1% and decreased G0/G1 phase cells from 49.5% to 24.5% at 1.0 μM for 48 h, with S phase percentage unchanged.
Resulted in 27.1% of cells in G2/M phase at 1 μM for 2 days; this percentage decreased to 18.1% and 13.1% after 3 and 4 days, respectively.
Increased the pre-G0/G1 apoptotic cell population from 1.9% at day 1 to 18.1% at day 4 with 1 μM treatment.
体内研究
(In Vivo)

Girolline 在临床前毒理学研究中对犬和小鼠表现出低毒性作用[2]。

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

190.63

Formula

C6H11ClN4O
CAS 号
结构分类
初始来源

Cymbastela cantharella (Pseudaxinyssa cantharella)
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

Girolline 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Girolline110883-46-0RP 49532RP49532RP-49532Interleukin RelatedNF-κBAP-1MDM-2/p53ApoptosisILNuclear factor-κBNuclear factor-kappaBActivator Protein 1TLR2TLR7MyD88TLR5p53Toll-like receptorTLR3eukaryotic translation initiation factor 5Aelongation factor 2TLR4Inhibitorinhibitorinhibit

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