| Description | AEBSF hydrochloride (Pefabloc SC) is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, thrombin, plasmin, and trypsin. |
| In vitro | 在蟑螂诱发的小鼠过敏模型中,AEBSF能够减少其呼吸道反应和潜在的炎症.在小鼠中注射致死量的弓形虫,每天腹腔注射76.8 mg/kg AEBSF,能够延长其生存期. |
| In vivo | AEBSF是一种丝氨酸蛋白酶抑制剂,它能够抑制巨噬细胞裂解白血病细胞,并且不会抑制巨噬细胞分泌TNF-α和IL-1β。在5种不同人细胞系中,AEBSF通过抑制神经和非神经中的β分泌,从而抑制组成Aβ的产物。AEBSF能够扰乱子宫内膜中囊胚的生长,还能够改变蛋白分泌机制从而抑制在人脐静脉内皮细胞中HeLa细胞的粘附。 |
| Cell experiments | The HeLa cells suspended in RPMI-1640 media containing 10% FCS are plated into each well of a 96-well microplate (5×103 cells/200 μL/well). After incubation for 24 h at 37°C, cells are treated with different doses of AEBSF (0, 25, 50, 100 μg/mL) for 48 h. Then, 20 μL fresh 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-diphenytetrazoliumromide (MTT) reagent (5 μg/μL) is added into each well, and cells are cultured at 37°C in 5% CO2 for another 4 h. The media are discarded carefully, and 150 μL DMSO is added. Absorbance is read on a microplate reader at dual wavelengths of 540 and 620 nm. |
| Synonyms | AEBSF HCl, Pefabloc SC |
| molecular weight | 239.69 |
| Molecular formula | C8H11ClFNO2S |
| CAS | 30827-99-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 24 mg/mL (100 mM) DMSO: 60 mg/mL (250.32 mM) |
| References | 1. Citron M, et al. Neuron. 1996, 17(1), 171-179. 2. Nakabo Y, et al. J Leukoc Biol. 1996, 60(3), 328-336. 3. Buitrago-Rey R. et al. J Antimicrob Chemother. 2002, 49(5), 871-874. 4. Jiang YH, et al. Contraception. 2011, 84(6), 642-648. 5. Saw S, et al. Inflammation. 2014. DOI 10.12007/s10753-2014-19976-0. 6. Jiang T Y, Feng X F, Fang Z, et al. PTEN deficiency facilitates the therapeutic vulnerability to proteasome inhibitor bortezomib in gallbladder cancer[J]. Cancer Letters. 2020 7. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562). |
| Citations | 1. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma. Science Translational Medicine. 2020, 12(562). 2. Jiang T Y, Feng X F, Fang Z, et al. PTEN deficiency facilitates the therapeutic vulnerability to proteasome inhibitor bortezomib in gallbladder cancer. Cancer Letters. 2021, 501: 187-199. |