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| 5mg |
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| Targets |
EXO70 subunit of the exocyst complex. Endosidin-2 binds to the C-terminal domain of EXO70 with a Kd of 253 μM for the plant isoform EXO70A1. The exocyst complex is a highly conserved octameric protein complex that tethers secretory vesicles to the plasma membrane, a critical step in exocytosis. By binding to EXO70, Endosidin-2 disrupts the function of the exocyst, thereby inhibiting the fusion of vesicles with the plasma membrane and the release of their contents.
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| ln Vitro |
In vitro, Endosidin-2 has been shown to bind directly to the EXO70 subunit of the exocyst complex. Its binding affinity has been characterized using techniques such as isothermal titration calorimetry (ITC) or surface plasmon resonance (SPR). The compound inhibits exocytosis in plant and mammalian cell models, as demonstrated by the accumulation of post-Golgi vesicles and the inhibition of secretion of reporter proteins.
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| ln Vivo |
In vivo, Endosidin-2 is primarily used in plant research to study the role of exocytosis in various developmental and physiological processes, including polar growth, cell division, and stress responses. By inhibiting exocytosis, it can phenocopy the effects of mutations in exocyst subunits, providing insights into the function of this complex in living organisms.
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| Enzyme Assay |
The binding of Endosidin-2 to EXO70 can be assessed using in vitro binding assays. Recombinant EXO70 protein is incubated with varying concentrations of Endosidin-2, and the binding affinity is determined using isothermal titration calorimetry (ITC) or fluorescence polarization. A competition assay with a fluorescently labeled ligand can also be used.
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| Cell Assay |
To study its cellular effects, plant or mammalian cells are treated with Endosidin-2. The effect on exocytosis is assessed by monitoring the secretion of a reporter protein, such as a secreted alkaline phosphatase (SEAP), or by visualizing the accumulation of secretory vesicles using transmission electron microscopy or confocal microscopy with fluorescent markers.
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| Animal Protocol |
The in vivo efficacy of Endosidin-2 is typically evaluated in plant models, such as Arabidopsis thaliana. The compound is applied to seedlings or tissues, and its effects on growth, development, and cellular processes like root hair elongation, pollen tube growth, or cytokinesis are assessed.
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| ADME/Pharmacokinetics |
Endosidin-2 has a molecular weight of 414.17 g/mol and a molecular formula of C15H12FIN2O3. It is a cell-permeable small molecule. It is soluble in DMF (up to 35 mg/ml) and ethanol (up to 10 mg/ml). The compound is typically stored at -20°C. Specific pharmacokinetic data are not available, as it is not a drug candidate.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Endosidin-2 are not detailed, as it is a research compound. It is not intended for human or veterinary use. Standard laboratory safety precautions, including the use of personal protective equipment (PPE), should be followed when handling the compound.
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| References | |
| Additional Infomation |
The conserved subunit EXO70 in the exocytosis complex inhibits exocytosis.
Endosidin-2 is a valuable chemical probe for studying the exocyst complex and its role in membrane trafficking. It is one of a few small molecules that can specifically inhibit exocytosis, providing a unique tool for dissecting this fundamental cellular process. It has been used to study the dynamic regulation of membrane trafficking in plant cells, including polar growth and vesicle sorting. It is not an approved drug and is strictly for research purposes. |
| Molecular Formula |
C15H12FIN2O3
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|---|---|
| Molecular Weight |
414.17
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| Exact Mass |
413.987
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| CAS # |
1839524-44-5
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| PubChem CID |
135504490
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.631
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| LogP |
2.84
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
410
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C(=CC(=C1)/C=N/NC(=O)C2=CC(=CC=C2)F)I)O
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| InChi Key |
UIADDCURKKFTFW-QGMBQPNBSA-N
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| InChi Code |
InChI=1S/C15H12FIN2O3/c1-22-13-6-9(5-12(17)14(13)20)8-18-19-15(21)10-3-2-4-11(16)7-10/h2-8,20H,1H3,(H,19,21)/b18-8+
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| Chemical Name |
3-fluoro-N-[(E)-(4-hydroxy-3-iodo-5-methoxyphenyl)methylideneamino]benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (241.45 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4145 mL | 12.0723 mL | 24.1447 mL | |
| 5 mM | 0.4829 mL | 2.4145 mL | 4.8289 mL | |
| 10 mM | 0.2414 mL | 1.2072 mL | 2.4145 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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