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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
AEBSF HCl (known also as AEBSF Hydrochloride) is a novel, broad spectrum, covalently/irreversibly inhibitor of serine proteases, such as chymotrypsin, plasmin, thrombin, and trypsin. Different cell lines were found to produce less Aβ when exposed to AEBSF. AEBSF demonstrated a dose-dependent decrease of Aβ with an IC50 value of roughly 1 mM in K293 cells transfected with APP695 (K695sw). AEBSF exhibited an inhibitory effect with an IC50 value of approximately 300 μM in HS695 and SKN695 cells transfected with wild-type APP695.
| Targets |
serine protease
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|---|---|
| ln Vitro |
AEBSF directly inhibits β-secretase in five distinct human cell lines, both neural and nonneural, to prevent the constitutive synthesis of Aβ[1].
AEBSF, as a serine protease inhibitor that prevents human macrophages from lysing leukemic cells, but it does not stop macrophages from secreting TNF-α and IL-1β[2]. AEBSF also modifies the pattern of protein secretion, which prevents HeLa cells from adhering to HUVECs and interferes with the growth of blastocysts on endometrial cells[4]. |
| ln Vivo |
AEBSF (76.8 mg/kg daily, i.p.) results in prolongation of the survival of mice that have been given a lethal T. gondii infection[3]. AEBSF also lowers the cockroach allergen-induced murine model's airway response and underlying inflammation[4].
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| Cell Assay |
HeLa cells suspended in RPMI-1640 medium with 10% FCS are plated into a 96-well microplate, with 5×103 cells/200 μL allocated to each well. The cells are treated with varying doses of AEBSF (0, 25, 50, and 100 μg/mL) for 48 hours following a 24-hour incubation period at 37°C. Subsequently, each well receives 20 μL of fresh 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-diphenytetrazoliumromide (MTT) reagent (5 μg/μL), and the cells are cultured for an additional 4 hours at 37°C in 5% CO2. After carefully discarding the media, add 150 μL of DMSO. On a microplate reader, absorbance is measured at two different wavelengths: 540 and 620 nm.
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| Animal Protocol |
Mice that receive a 2.5×103 parasite injection are randomly allocated to one of the following treatment groups: vehicle alone (control group), pyrimethamine alone at various doses, LY311727 alone at various doses, AEBSF alone at various doses, or AEBSF 76.8 mg/kg plus pyrimethamine 10 mg/kg. Each treatment group has ten animals in it. After the parasite inoculation, treatment is started 24 hours later and lasts for seven days in a row. In live mice, mouse survival is tracked every day for 15 days after infection. Every experiment is run three times, and the results displayed are the total of those runs.
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| References |
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| Molecular Formula |
C8H11CLFNO2S
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|---|---|---|
| Molecular Weight |
239.69
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| Exact Mass |
239.018
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| Elemental Analysis |
C, 40.09; H, 4.63; Cl, 14.79; F, 7.93; N, 5.84; O, 13.35; S, 13.38
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| CAS # |
30827-99-7
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| Related CAS # |
34284-75-8;30827-99-7 (HCl);
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| PubChem CID |
186136
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| Appearance |
White to off-white solid powder
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| Boiling Point |
292.5ºC at 760 mmHg
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| Melting Point |
175-177 °C
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| Flash Point |
130.7ºC
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| LogP |
3.429
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
239
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C1=CC=C(CCN)C=C1)(F)=O.[H]Cl
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| InChi Key |
WRDABNWSWOHGMS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H10FNO2S.ClH/c9-13(11,12)8-3-1-7(2-4-8)5-6-10;/h1-4H,5-6,10H2;1H
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| Chemical Name |
4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride
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| Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (417.21 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 5: 100 mg/mL (417.21 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1721 mL | 20.8603 mL | 41.7206 mL | |
| 5 mM | 0.8344 mL | 4.1721 mL | 8.3441 mL | |
| 10 mM | 0.4172 mL | 2.0860 mL | 4.1721 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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