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苄磺酰氟

苄磺酰氟用途

PMSF是通常用于制备细胞裂解物的不可逆的丝氨酸/半胱氨酸蛋白酶抑制剂。

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苄磺酰氟名称

[ CAS 号 ]:
329-98-6

[ 中文名 ]:
苯甲基磺酰氟

[ 英文名 ]:
PMSF

[中文别名 ]:

[英文别名 ]:

α-Toluenesulfonyl fluoride
Benzenemethanesulfonyl fluoride
Phenylmethanesulfonyl fluoride (PMSF)
Phenylmethylsulfonyl fluoride
Phenylmethanesulfonyl fluoride
Phenylmethanesulphonyl fluoride
Fluoride, Phenylmethanesulfonyl
phenyl methane sulfonyl fluoride
phenylmethyl-sulfonyl fluoride
PMSF

苄磺酰氟生物活性

[ 描述 ]:

PMSF是通常用于制备细胞裂解物的不可逆的丝氨酸/半胱氨酸蛋白酶抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 组织蛋白酶

研究领域 >> 其他

[体外研究]

PMSF(2mM)在Li +存在下抑制卡巴胆碱刺激的肌醇磷酸累积仅15％-19％。 PMSF对磷酸肌醇转换的抑制是由于磷酸肌醇分解后的一个或多个步骤[1]。 PMSF抑制T.brucei的血流中GPI中间体的肌醇残基的酰化。 PMSF抑制糖脂C的形成但不抑制体外脂肪酸重塑。 PMSF抑制了在procyclic锥虫中添加GPI酰化和乙醇胺磷酸酶,但在Hela细胞中没有[2]。

[体内研究]

PMSF(0.1mL/10g b.wt,ip)产生抗伤害感受,如甩尾潜伏期评估中％MPE的剂量响应性增加所示,但未能产生明确的剂量反应性运动抑制。接受腹膜内注射PMSF的小鼠表现出大麻素效应,包括抗伤害感受,体温过低和不动,ED50值分别为86,224和206mg/kg。 PMSF(30 mg/kg)预处理增强了anandamide对甩尾反应(抗伤害感受),自发活动和活动性的影响,分别为5倍,10倍和8倍[3]。

[动物实验]

在测定中使用重18至25g的雄性ICR小鼠。将PMSF溶解在芝麻油中，并以0.1mL / 10g b.wt的体积腹膜内施用。在静脉注射anandamide或载体注射前10分钟始终给予PMSF。使小鼠适应评估室过夜而不中断食物或水。在静脉注射anandamide或载体给药后，如下评价每只动物：5分钟的甩尾潜伏期（抗伤害感受）反应和5至15分钟的自发（运动）活动;或核心（直肠）温度5分钟和环固定（僵住症）5至10分钟。

[参考文献]

[1]. Sekar, M.C. and B.D. Roufogalis, Differential effects of phenylmethanesulfonyl fluoride (PMSF) on carbachol and potassium stimulated phosphoinositide turnover and contraction in longitudinal smooth muscle of guinea pig ileum. Cell Calcium, 1984. 5(3): p.

[2]. Guther, M.L., W.J. Masterson, and M.A. Ferguson, The effects of phenylmethylsulfonyl fluoride on inositol-acylation and fatty acid remodeling in African trypanosomes. J Biol Chem, 1994. 269(28): p. 18694-701.

[3]. Compton, D.R. and B.R. Martin, The effect of the enzyme inhibitor phenylmethylsulfonyl fluoride on the pharmacological effect of anandamide in the mouse model of cannabimimetic activity. J Pharmacol Exp Ther, 1997. 283(3): p. 1138-43.

[相关活性小分子]

苄磺酰氟物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
285.7±19.0 °C at 760 mmHg

[ 熔点 ]:
92-95 °C

[ 分子式 ]:
C₇H₇FO₂S

[ 分子量 ]:
174.193

[ 闪点 ]:
126.6±21.5 °C

[ 精确质量 ]:
174.015076

[ PSA ]:
42.52000

[ LogP ]:
2.33

[ 外观性状 ]:
白色至奶油色固体

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.522

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
hydrolysis

苄磺酰氟MSDS

详细MSDS(安全技术说明书)

苄磺酰氟毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XT8040000

CHEMICAL NAME :: alpha-Toluenesulfonyl fluoride

CAS REGISTRY NUMBER :: 329-98-6

BEILSTEIN REFERENCE NO. :: 2088311

LAST UPDATED :: 199701

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C7-H7-F-O2-S

MOLECULAR WEIGHT :: 174.20

WISWESSER LINE NOTATION :: WSF1R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 173,33,1954

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 39,265,1976

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 215 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: LIFSAK Life Sciences. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1-8, 1962-69; V.14- 1974- Volume(issue)/page/year: 31,1193,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4865 No. of Facilities: 104 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 2391 (estimated) No. of Female Employees: 1942 (estimated)

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苄磺酰氟安全信息

[ 符号 ]:

GHS05, GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H314

[ 警示性声明 ]:
P280-P305 + P351 + P338-P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P2 (EN 143) respirator cartridges;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R25;R34

[ 安全声明 (欧洲) ]:
S7-S16-S45-S36/37/39-S28A-S26

[ 危险品运输编码 ]:
UN 3261 8/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
XT8050000

[ 包装等级 ]:
III

[ 危险类别 ]:
8

[ 海关编码 ]:
2904909090

苄磺酰氟合成路线

详细合成路线

苄磺酰氟上下游产品

苄磺酰氟上游产品

苄磺酰氟下游产品

苄磺酰氟海关

[ 海关编码 ]: 2904909090

[ 中文概述 ]:
2904909090 其他烃的磺化、硝化、亚硝化衍生物（不论是否卤化）. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:5.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
HS:2904909090 sulphonated, nitrated or nitrosated derivatives of hydrocarbons, whether or not halogenated VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:5.5% General tariff:30.0%

苄磺酰氟文献

Immunomodulation by the Pseudomonas syringae HopZ type III effector family in Arabidopsis.

PLoS ONE 9(12) , e116152, (2014)

Pseudomonas syringae employs a type III secretion system to inject 20-30 different type III effector (T3SE) proteins into plant host cells. A major role of T3SEs is to suppress plant immune responses ...

Assembly and structure of Lys33-linked polyubiquitin reveals distinct conformations.

Biochem. J. 467(2) , 345-52, (2015)

Ubiquitylation regulates a multitude of biological processes and this versatility stems from the ability of ubiquitin (Ub) to form topologically different polymers of eight different linkage types. Wh...

A survey of the interactome of Kaposi's sarcoma-associated herpesvirus ORF45 revealed its binding to viral ORF33 and cellular USP7, resulting in stabilization of ORF33 that is required for production of progeny viruses.

J. Virol. 89(9) , 4918-31, (2015)

The ORF45 protein of Kaposi's sarcoma-associated herpesvirus (KSHV) is a gammaherpesvirus-specific immediate-early tegument protein. Our previous studies have revealed its crucial roles in both early ...

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