AEBSF.HCl
(Synonyms: 4-(2-氨乙基)苯磺酰氟盐酸盐,AEBSF.HCl,AEBSF Hydrochloride) 目录号 : GC14502
AEBSF.HCl是丝氨酸蛋白酶广谱的不可逆的抑制剂，可抑制胰凝乳蛋白酶，激肽释放酶，纤溶酶，凝血酶，胰蛋白酶和相关的溶栓酶等。
Cas No.:30827-99-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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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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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
AEBSF.HCl是丝氨酸蛋白酶广谱的不可逆的抑制剂，可抑制胰凝乳蛋白酶，激肽释放酶，纤溶酶，凝血酶，胰蛋白酶和相关的溶栓酶等。AEBSF.HCl的作用机制是通过与丝氨酸残基共价结合，阻断蛋白酶的活性中心，从而抑制蛋白酶的活性[1]。
在体外，AEBSF.HCl抑制多种细胞系中的Aβ产生。AEBSF.HCl在转染K695 sw的K293细胞中呈剂量依赖性降低Aβ，IC50值约为1 mM，在转染野生型APP 695的HS 695和SKN 695细胞中呈剂量依赖性抑制作用，IC50值约为300 μM。AEBSF.HCl还能增加α-裂解，抑制β-裂解[1]。此外，作为蛋白酶抑制剂，AEBSF.HCl（150 μM）与巨噬细胞孵育6小时可以阻止单核细胞衍生的巨噬细胞裂解白血病细胞[2]。
在体内，AEBSF.HCl(5 mg or 10 mg；i.v.)对大鼠胚胎着床有抑制作用，在妊娠第8天可见着床胚胎数[3]。AEBSF.HCl（76.8 mg/kg/d，i. p.）延长了被给予致死性刚地弓形虫(Toxoplasma gondii)感染的小鼠生存时间[4]。
| Cas No. | 30827-99-7 | SDF | |
| 别名 | 4-(2-氨乙基)苯磺酰氟盐酸盐,AEBSF.HCl,AEBSF Hydrochloride | ||
| 化学名 | 4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride | ||
| Canonical SMILES | C1=CC(=CC=C1CCN)S(=O)(=O)F.Cl | ||
| 分子式 | C8H10FNO2S.HCl | 分子量 | 239.69 |
| 溶解度 | ≥ 12 mg/mL in DMSO, ≥ 15.73 mg/mL in Water, ≥ 23.8 mg/mL in EtOH with gentle warming | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。