| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| 5g | |||
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| Targets |
ES9-17 targets the clathrin heavy chain (CHC). By binding to the N-terminal domain of CHC, it inhibits clathrin-mediated endocytosis (CME) in both plant (Arabidopsis) and human cells. This inhibition blocks the internalization of various CME cargoes.
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| ln Vitro |
At an EC50 of 13 μM, ES9-17 (0-100 μM; 30 minutes) inhibits the absorption of the lipophilic phenyl endocytic tracer (FM4-64) [1]. In HeLa cells, ES9-17 (30 μM; 30 min) and ES9-17 (30 μM; 30 min) also lessen transferrin's nutritional availability [1]. In addition to not causing cytoplasmic acidification, ES9-17 inhibits CHC and controls the inner membrane transport pathway [2].
In vitro, ES9-17 inhibits the uptake of FM4-64 and several CME cargos in Arabidopsis. It also inhibits transferrin uptake in human cells. The compound is a potent inhibitor of CME in both plant and mammalian systems. |
| ln Vivo |
In vivo, ES9-17 inhibits root growth in Arabidopsis seedlings. This phenotypic effect is a readout of CME inhibition in plants. The compound's activity has been characterized in both plant and human cellular systems.
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| Enzyme Assay |
The binding of ES9-17 to the N-terminal domain of clathrin heavy chain (CHC) is assessed using binding assays. CME inhibition is measured by assessing the uptake of fluorescent endocytic cargoes such as FM4-64 or transferrin.
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| Cell Assay |
Cellular activity of ES9-17 is evaluated in cell lines such as HeLa cells or plant systems like Arabidopsis. Cells are treated with ES9-17, and the uptake of fluorescently labeled cargo is measured by flow cytometry or fluorescence microscopy.
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| Animal Protocol |
In vivo efficacy of ES9-17 is evaluated in Arabidopsis seedlings. Seedlings are grown in the presence of the compound, and root growth inhibition is measured as a phenotypic readout of CME inhibition.
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| ADME/Pharmacokinetics |
ES9-17 has a molecular formula of C10H8BrNO2S2 and a molecular weight of 318.21. Its chemical name is 5-bromo-N-phenylthiophene-2-sulfonamide. The compound is stored as a powder at -20°C for up to 3 years. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Toxicological data for ES9-17 are limited. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
ES9-17 is a potent and selective inhibitor of clathrin-mediated endocytosis (CME). It is an improved analog of Endosidin9 (ES9). It is a valuable tool for studying endocytosis in both plant and animal systems and has potential applications in cancer research.
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| Molecular Formula |
C10H8BRNO2S2
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|---|---|
| Molecular Weight |
318.203
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| Exact Mass |
316.917
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| Elemental Analysis |
C, 37.75; H, 2.53; Br, 25.11; N, 4.40; O, 10.06; S, 20.15
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| CAS # |
55854-43-8
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| PubChem CID |
893416
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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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| Boiling Point |
435.4±55.0 °C at 760 mmHg
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| Flash Point |
217.1±31.5 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.682
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
322
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C1=CC=C(Br)S1)(NC2=CC=CC=C2)=O
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| InChi Key |
AIZXCKZVUXCHAP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8BrNO2S2/c11-9-6-7-10(15-9)16(13,14)12-8-4-2-1-3-5-8/h1-7,12H
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| Chemical Name |
5-Bromo-N-phenylthiophene-2-sulfonamide
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| Synonyms |
ES9-17; ES9 17; ES917
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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 : ~125 mg/mL (~392.82 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 | 3.1427 mL | 15.7134 mL | 31.4268 mL | |
| 5 mM | 0.6285 mL | 3.1427 mL | 6.2854 mL | |
| 10 mM | 0.3143 mL | 1.5713 mL | 3.1427 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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