AEBSF.HCl (Synonyms: Pefabloc SC) |
| Katalog-Nr.GC14502 |
AEBSF.HCl is a broad-spectrum, irreversible inhibitor of serine proteases, capable of inhibiting trypsin, kallikrein, plasmin, thrombin, chymotrypsin, and related thrombolytic enzymes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 30827-99-7
Sample solution is provided at 25 µL, 10mM.
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AEBSF.HCl is a broad-spectrum, irreversible inhibitor of serine proteases, capable of inhibiting trypsin, kallikrein, plasmin, thrombin, chymotrypsin, and related thrombolytic enzymes. The mechanism of action of AEBSF.HCl involves covalent binding to serine residues, blocking the active center of the protease, thereby inhibiting its activity [1].
In vitro, AEBSF.HCl inhibits the production of Aβ in various cell lines. AEBSF.HCl demonstrates a dose-dependent reduction of Aβ in K293 cells transfected with K695 sw, with an IC50 value of about 1 mM, and shows a dose-dependent inhibitory effect in HS 695 and SKN 695 cells transfected with wild-type APP 695, with an IC50 value of about 300 μM. AEBSF.HCl also increases α-cleavage while inhibiting β-cleavage [1]. Additionally, as a protease inhibitor, AEBSF.HCl (150 μM) incubated with macrophages for 6 hours can block the lysis of leukemia cells by monocyte-derived macrophages [2].
In vivo, AEBSF.HCl (5 mg or 10 mg; i.v.) inhibits rat embryo implantation, with a visible reduction in the number of implanted embryos on day 8 of pregnancy [3]. AEBSF.HCl (76.8 mg/kg/d, i.p.) extends the survival time of mice given a lethal infection of Toxoplasma gondii [4].
References:
[1] Citron M, Diehl T S, Capell A, et al. Inhibition of amyloid β-protein production in neural cells by the serine protease inhibitor AEBSF. Neuron, 1996, 17(1): 171-179.
[2] Nakabo Y, Pabst M J. Lysis of leukemic cells by human macrophages: inhibition by 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), a serine protease inhibitor. Journal of leukocyte biology, 1996, 60(3): 328-336.
[3] Jiang YH, Shi Y, He YP, Du J, Li RS, Shi HJ, Sun ZG, Wang J. 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.
[4] Buitrago-Rey R, et al. 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. 2002 May;49(5):871-4
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Cell experiment [1]: |
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Cell lines |
K695sw, HS695 and SKN695 cells |
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Preparation method |
Aβ inhibition assay was performed with 0, 0.1, 0.3, 0.6, 0.8, 1.0 and 1.2 mM AEBSF.HCl for 20 min. |
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Reaction Conditions |
0, 0.1, 0.3, 0.6, 0.8, 1.0 and 1.2 mM; 20 mins |
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Applications |
AEBSF.HCl was found to inhibit Aβ production in various cell lines. In K293 cells transfected with K695sw, AEBSF.HCl showed dose-dependent reduction of Aβ with the IC50 value of about 1 mM. In HS695 and SKN695 cells transfected with wild-type APP695, AEBSF.HCl showed inhibition effect with IC50 value of about 300 μM. |
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Animal experiment [2]: |
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Animal models |
SD rats |
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Preparation method |
Intrauterine (5 mg or 10 mg AEBSF.HCl per injection) or tail vein (10 mg AEBSF.HCl per rat) administration on day 3 of pregnancy |
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Dosage form |
5 mg or 10 mg；i.v. |
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Applications |
According to the number of visible implanted embryos on day 8 of pregnancy, it was shown that AEBSF.HCl inhibited embryo implantation in rat. |
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References: [1] Citron M, Diehl T S, Capell A, et al. Inhibition of amyloid β-protein production in neural cells by the serine protease inhibitor AEBSF. Neuron, 1996, 17(1): 171-179. [2] Jiang YH, Shi Y, He YP, Du J, Li RS, Shi HJ, Sun ZG, Wang J. 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. |
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| Cas No. | 30827-99-7 | SDF | |
| Überlieferungen | Pefabloc SC | ||
| Chemical Name | 4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride | ||
| Canonical SMILES | C1=CC(=CC=C1CCN)S(=O)(=O)F.Cl | ||
| Formula | C8H10FNO2S.HCl | M.Wt | 239.69 |
| Löslichkeit | ≥ 12 mg/mL in DMSO, ≥ 15.73 mg/mL in Water, ≥ 23.8 mg/mL in EtOH with gentle warming | Storage | Desiccate 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 | 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 | 2.086 mL | 4.1721 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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