AEBSF.HCl
AEBSF.HCl (CAS 30827-99-7) is an irreversible serine protease inhibitor that covalently binds and inhibits several proteases, including trypsin, chymotrypsin, plasmin, and thrombin. It has been applied in cellular research to study amyloid-beta (Aβ) production mechanisms. In APP695 (K695sw)-transfected K293 cells, AEBSF dose-dependently reduces Aβ formation with an IC50 around 1 mM, while in wild-type APP695-transfected HS695 and SKN695 cells, it shows inhibitory effects with an IC50 of approximately 300 μM. Besides suppressing β-cleavage, AEBSF promotes α-cleavage of APP. In macrophage-mediated leukemic cell lysis assays, incubation with AEBSF at 150 μM for 6 hours achieves near-maximal protease inhibition, thus impeding cell lysis.
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.
- 1. Shuzhen Liu, Preston Perez, et al. "MLKL polymerization-induced lysosomal membrane permeabilization promotes necroptosis." Cell Death Differ. 2023 Nov 23. PMID: 37996483
- 2. Zhijun Liu, Himani Nailwal, et al. "A class of viral inducer of degradation of the necroptosis adaptor RIPK3 regulates virus-induced inflammation." Immunity. 2021 Feb 9;54(2):247-258.e7. PMID: 33444549
- 3. Brodie NI, Popov KI, et al."Conformational ensemble of native α-synuclein in solution as determined by short-distance crosslinking constraint-guided discrete molecular dynamics simulations." PLoS Comput Biol. 2019 Mar 27;15(3):e1006859. PMID: 30917118
| Storage | Desiccate at -20°C |
| M.Wt | 239.69 |
| Cas No. | 30827-99-7 |
| Formula | C8H10FNO2S·HCl |
| Synonyms | AEBSF.HCl,AEBSF Hydrochloride |
| Solubility | ≥12 mg/mL in DMSO; ≥15.73 mg/mL in H2O; ≥23.8 mg/mL in EtOH with gentle warming |
| Chemical Name | 4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1CCN)S(=O)(=O)F.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
K695sw, HS695 and SKN695 cells |
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Preparation method |
The solubility of this compound in DMSO is ≥798.97mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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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 was found to inhibit Aβ production in various cell lines. In K293 cells transfected with βAPP695 (K695sw), AEBSF 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 showed inhibition effect with IC50 value of about 300 μM. AEBSF was also found to increase α-cleavege and inhibit β- cleavage. |
| Animal experiment [2]: | |
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Animal models |
SD rats |
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Dosage form |
Intrauterine (5 mg or 10 mg AEBSF per injection) or tail vein (10 mg AEBSF per rat) administration on day 3 of pregnancy |
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Applications |
According to the number of visible implanted embryos on day 8 of pregnancy, it was shown that AEBSF inhibited embryo implantation in rat. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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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| Description | AEBSF.HCl is an irreversible broad spectrum inhibitor of serine protease. | |||||
| Targets | serine protease | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
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