Cell lines

K695sw, HS695 and SKN695 cells

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.

Reaction Conditions

0, 0.1, 0.3, 0.6, 0.8, 1.0 and 1.2 mM; 20 mins

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 models

SD rats

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

Applications

According to the number of visible implanted embryos on day 8 of pregnancy, it was shown that AEBSF inhibited embryo implantation in rat.

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.

AEBSF is a broad spectrum, irreversible inhibitor of serine proteases [1].

AEBSF is a covalently binding inhibitor of proteases, including trypsin, chymotrypsin, plasmin and thrombin. AEBSF was found to inhibit Aβ production in various cell lines. In K293 cells transfected with APP695 (K695sw), AEBSF showed does-dependent reduction of Aβ with IC50 value of about 1mM. 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. Besides that, as a protease inhibitor, AEBSF was reported to prevent monocyte-derived macrophages from lysing the leukemic cells. Incubation of macrophages with 150 μM AEBSF for 6 hours resulted in nearly maximum inhibition [1, 2].

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.