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AEBSF.HCl

现货
Catalog No.
A2573
丝氨酸蛋白酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
100mg
¥ 600.00
现货
500mg
¥ 2,000.00
Ship with 10-15 days

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Background

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.

文献引用

1. 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

Chemical Properties

StorageDesiccate at -20°C
M.Wt239.69
Cas No.30827-99-7
FormulaC8H10FNO2S.HCl
SynonymsAEBSF.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 Name4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride
SDFDownload SDF
Canonical SMILESC1=CC(=CC=C1CCN)S(=O)(=O)F.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

K695sw、HS695和SKN695细胞

制备方法

在DMSO中的溶解度≥798.97mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

0、0.1、0.3、0.6、0.8、1.0和1.2 mM;20分钟

实验结果

据发现,在各种细胞系中,AEBSF抑制Aβ生成。在转染了βAPP695(K695sw)的K293细胞中,AEBSF呈剂量依赖性地减少Aβ,其IC50值约为1 mM。在转染了野生型APP695的HS695和SKN695细胞中,AEBSF显示出抑制作用,其IC50值约为300 μM。此外,AEBSF增加α裂解并抑制β裂解。

动物实验 [2]:

动物模型

SD大鼠

给药剂量

于妊娠第3天,子宫内(每次注射5 mg或10 mg AEBSF)或尾静脉注射(给予每只大鼠10 mg AEBSF)给药

实验结果

于妊娠第8天,统计可见的植入胚胎数,结果表明,AEBSF抑制大鼠胚胎植入。

其他注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

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.

生物活性

描述 AEBSF.HCl是一种不可逆的、广谱性丝氨酸蛋白酶抑制剂。
靶点 serine protease          
IC50            

质量控制

质量控制和MSDS

批次:

化学结构

AEBSF.HCl

相关生物数据

AEBSF.HCl

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AEBSF.HCl

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AEBSF.HCl