AEBSF HCl

Alias:
Cat No.:V0711 Purity: ≥98%
AEBSF HCl (known also as AEBSF Hydrochloride) is a novel, broad spectrum, covalently/irreversible inhibitor of serine protease including trypsin, chymotrypsin, plasmin and thrombin.
AEBSF HCl Chemical Structure CAS No.: 30827-99-7
Product category: Serine Protease
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
serine protease
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].
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.
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.
References

[1]. Inhibition of amyloid beta-protein production in neural cells by the serine protease inhibitor AEBSF. Neuron. 1996 Jul;17(1):171-9.

[2]. Lysis of leukemic cells by human macrophages: inhibition by 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), a serine protease inhibitor. J Leukoc Biol. 1996 Sep;60(3):328-36.

[3]. Evaluation of two inhibitors of invasion: LY311727 [3-(3-acetamide-1-benzyl-2-ethyl-indolyl-5-oxy)propane phosphonic acid] and AEBSF [4-(2-aminoethyl)-benzenesulphonyl fluoride] in acute murine toxoplasmosis. J Antimicrob Chemother.

[4]. Serine protease inhibitor 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (AEBSF) inhibits the rat embryo implantation in vivo and interferes with cell adhesion in vitro. Contraception. 2011 Dec;84(6):642-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C8H11CLFNO2S
Molecular Weight
239.69
Exact Mass
239.02
Elemental Analysis
C, 40.09; H, 4.63; Cl, 14.79; F, 7.93; N, 5.84; O, 13.35; S, 13.38
CAS #
30827-99-7
Related CAS #
34284-75-8;30827-99-7 (HCl);
Appearance
Solid powder
SMILES
C1=CC(=CC=C1CCN)S(=O)(=O)F.Cl
InChi Key
WRDABNWSWOHGMS-UHFFFAOYSA-N
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
Chemical Name
4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride
Synonyms

AEBSF HCl; AEBSF hydrochloride

HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: ~47 mg/mL (~196.1 mM)
Water: ~20 mg/mL (~83.4 mM)
Ethanol: ~47 mg/mL (~196.1 mM)
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.

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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.
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Biological Data
  • AEBSF Stabilizes Full-Length βAPP. Neuron . 1996 Jul;17(1):171-9.
  • AEBSF Increases α-Secretion. Neuron . 1996 Jul;17(1):171-9.
  • AEBSF Increases Aβ Production in the Cell Lines F690P and D597Δ. Neuron . 1996 Jul;17(1):171-9.
  • Radiosequencing of Aβ Proteins Secreted by the Cell Lines F690P and D597Δ with and without AEBSF Treatment. Neuron . 1996 Jul;17(1):171-9.
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