Endosidin 2 (Synonyms: ES2) |
Catalog No.GC19010
One-Click Copy Product Info
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Endosidin 2 is a selective inhibitor targeting the conserved exosome subunit EXO70.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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. |
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Reaction Conditions |
100μM; 30min |
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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 |
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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. |
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Dosage form |
6mg/kg every 6 days for 24 days; i.p. |
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Applications |
Endosidin 2 significantly enhances the sensitivity of cisplatin in ovarian cancer cells and reduces tumor growth and metastasis. |
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References: |
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| Cas No. | 1839524-44-5 | SDF | |
| Synonyms | ES2 | ||
| Chemical Name | 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 | ||
| Formula | C15H12FIN2O3 | M.Wt | 414.2 |
| Solubility | 0.25mg/ml in ethanol; 30mg/ml in DMSO & DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4143 mL | 12.0715 mL | 24.1429 mL |
| 5 mM | 482.9 μL | 2.4143 mL | 4.8286 mL |
| 10 mM | 241.4 μL | 1.2071 mL | 2.4143 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)