Endosidin 2
(Synonyms: ES2) 目录号 : GC19010Endosidin 2是一种选择性抑制剂，靶向保守的外囊复合体亚基EXO70。
Cas No.:1839524-44-5
Sample solution is provided at 25 µL, 10mM.
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Endosidin 2 is a selective inhibitor targeting the conserved exosome subunit EXO70[1]. Endosidin 2 binds to the C-terminal domain of EXO70, blocking its protein-protein interactions with other components of the outer capsule complex, thereby inhibiting exosomes and systemic circulation[2]. Endosidin 2 is commonly used in the study of endocytosis and recirculation mechanisms in plant and mammalian cells[3][4].
In vitro, treatment of peripheral blood mononuclear cells (PBMCs) with Endosidin 2 (40μM; 1-2h) significantly inhibited the translocation of ACE2 to the cell surface induced by R848 and LPS[5]. Treatment of skeletal myoblast cells with Endosidin 2(100μM; 30min) leads to impaired GLUT4 trafficking to the plasma membrane and hinders glucose uptake in response to an insulin stimulus[6].
In vivo, in the intraperitoneal transplantation model of ovarian cancer A2780CR cells, Endosidin 2 (6mg/kg every 6 days for 24 days; i.p.) significantly enhances the sensitivity of cisplatin in ovarian cancer cells by inhibiting the function of the Exo70 subunit of the outer capsule complex, overcomes cisplatin resistance in ovarian cancer cells, and thereby reduces tumor growth and metastasis[7].
References:
[1] Zhang C, Brown MQ, van de Ven W, et al. Endosidin2 targets conserved exocyst complex subunit EXO70 to inhibit exocytosis. Proc Natl Acad Sci U S A. 2016;113(1):E41-E50.
[2] Huang L, Li X, Li Y, et al. Endosidin2-14 Targets the Exocyst Complex in Plants and Fungal Pathogens to Inhibit Exocytosis. Plant Physiol. 2019;180(3):1756-1770.
[3] Huang L, Zhang C. Use Endosidin2 to Study Plant Exocytosis and Vacuolar Trafficking. Methods Mol Biol. 2018;1789:167-175.
[4] Ciampelli C, Galleri G, Puggioni S, et al. Inhibition of the Exocyst Complex Attenuates the LRRK2 Pathological Effects. Int J Mol Sci. 2023;24(16):12656.
[5] Yao Y, Subedi K, Liu T, et al. Surface translocation of ACE2 and TMPRSS2 upon TLR4/7/8 activation is required for SARS-CoV-2 infection in circulating monocytes. Cell Discov. 2022;8(1):89.
[6] Fujimoto BA, Young M, Carter L, et al. The exocyst complex regulates insulin-stimulated glucose uptake of skeletal muscle cells. Am J Physiol Endocrinol Metab. 2019;317(6):E957-E972.
[7] Zhao Y, Hong X, Chen X, et al. Deregulation of Exo70 Facilitates Innate and Acquired Cisplatin Resistance in Epithelial Ovarian Cancer by Promoting Cisplatin Efflux. Cancers (Basel). 2021;13(14):3467.
Endosidin 2是一种选择性抑制剂，靶向保守的外囊复合体亚基EXO70[1]。Endosidin 2结合EXO70的C端结构域，阻断其与其他外囊复合体组分的蛋白-蛋白相互作用，从而抑制外泌作用及内体循环[2]。Endosidin 2常用于植物及哺乳动物细胞内吞 - 再循环机制研究[3][4]。
在体外研究中，用Endosidin 2（40μM；1 - 2 小时）处理外周血单核细胞（PBMCs）显著抑制了由R848和LPS诱导的ACE2向细胞表面的转位[5]。在骨骼肌母细胞中，Endosidin 2（100μM；30分钟）处理导致胰岛素刺激下GLUT4向质膜的运输受损，进而阻碍了葡萄糖的摄取[6]。
在体内研究中，在卵巢癌A2780CR细胞腹腔移植肿瘤模型中，Endosidin 2（每6天6mg/kg; 24天；腹腔注射）通过抑制外囊复合体亚基Exo70的功能显著增强了顺铂在卵巢癌细胞中的敏感性，克服了卵巢癌细胞的顺铂耐药性，从而减少了肿瘤的生长和转移[7]。
| Cell experiment [1]: | |
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Cell lines |
Rat L6 myoblast cells |
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Preparation Method |
Rat L6 myoblast cells were cultured in complete Minimum Essential Medium- Alpha (MEM alpha) with nucleosides supplemented with 10% (v/v) fetal bovine serum (FBS), and 1% antibiotic-antimycotic solution (v/v) (100U/mL of penicillin and 100μg/mL of streptomycin). The stock solution of Endosidin 2 was 30mg/ml in DMSO. For inhibition experiments, cells were treated with 100μM Endosidin 2 simultaneously with insulin in KR Buffer with 0.1% BSA for 30 minutes. Untreated controls were exposed to equal amounts of DMSO. Cells were cultured to 80-90% confluence in complete medium, then collected for further analysis. |
|
Reaction Conditions |
100μM; 30min |
|
Applications |
Endosidin 2 leads to impaired GLUT4 trafficking to the plasma membrane and hinders glucose uptake in response to an insulin stimulus. |
| Animal experiment [2]: | |
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Animal models |
BALB/c nude mice |
|
Preparation Method |
A2780CR cells were intraperitoneally inoculated into 5-week old female Balb/c nude mice (3×106 cells in 100µL DMEM per mouse). Endosidin 2 (6mg/kg) was administered intraperitoneally every six days. After 24 days of treatment, mice were euthanized, and the peritoneal metastasic tumors were collected and measured. For in vivo bioluminescent imaging, mice were administrated with 150mg/kg D-luciferin and imaged by Caliper IVIS Lumina II Kinetic system, and the total photon flux was calculated by Living Image 4.4. |
|
Dosage form |
6mg/kg every 6 days for 24 days; i.p. |
|
Applications |
Endosidin 2 significantly enhances the sensitivity of cisplatin in ovarian cancer cells and reduces tumor growth and metastasis. |
|
References: |
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| Cas No. | 1839524-44-5 | SDF | |
| 别名 | ES2 | ||
| 化学名 | 3-fluoro-benzoic acid, (2E)-2-[(4-hydroxy-3-iodo-5-methoxyphenyl)methylene]hydrazide | ||
| Canonical SMILES | FC1=CC(C(N/N=C/C2=CC(I)=C(O)C(OC)=C2)=O)=CC=C1 | ||
| 分子式 | C15H12FIN2O3 | 分子量 | 414.2 |
| 溶解度 | 0.25mg/ml in ethanol; 30mg/ml in DMSO & DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4143 mL | 12.0715 mL | 24.1429 mL |
| 5 mM | 0.4829 mL | 2.4143 mL | 4.8286 mL |
| 10 mM | 0.2414 mL | 1.2071 mL | 2.4143 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet