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(Synonyms: 苯甲基磺酰氟; Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride) 目录号 : GC10477

PMSF (苯甲基磺酰氟)是一种不可逆的丝氨酸蛋白酶抑制剂,常在细胞或组织裂解之前加入裂解液中以预防蛋白的降解。

PMSF Chemical Structure

Cas No.:329-98-6

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10mM (in 1mL DMSO)
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Sample solution is provided at 25 µL, 10mM.

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Description

PMSF is an irreversible serine protease inhibitor that is often added to the lysis buffer before cell or tissue lysis to prevent protein degradation[1,2]. PMSF can effectively inhibit chymotrypsin, trypsin, thrombin, etc. The principle of action of PMSF is that it can specifically recognize and sulfonate the serine residue active site that determines enzyme activity. PMSF is also an inhibitor of fatty acid amide hydrolase (FAAH), cysteine proteases (such as papain, the inhibitory activity of which is reversed by DTT), and acetylcholinesterase of mammalian origin[3]. The inhibitory effect of PMSF on papain can be reversed by DTT (Dithiothreitol).

The deactivation of PMSF increases with increasing pH and temperature. The half-lives of the inhibitors are approximately 110, 55, and 35 minutes at 25°C and pH 7.0, 7.5, and 8.0, respectively. At pH 8, 100μM PMSF is almost completely inactivated within 1 hour at 25°C or 22 hours at 4°C. PMSF stock solutions prepared using 100% isopropyl alcohol are stable for months or longer at 25°C. Within 1 week at 25°C and pH 7.0, chymotrypsin inhibited by PMSF did not reactivate[4].

In animal experiments, PMSF had significant analgesic effects at doses of 120 and 300 mg/kg. Sub-analgesic doses (60 mg/kg, i.p.) of PMSF can reduce tolerance resulting from acute and chronic administration of opioids[3].

PMSF can be used alone or often mixed with other protease inhibitors such as aprotinin A or phosphatase inhibitors such as sodium orthovanadate.

PMSF is poorly soluble in water and has poor stability in aqueous solutions. It is recommended to add it to lysis buffer or other aqueous solutions before use. PMSF powder can be dissolved in methanol, ethanol or isopropyl alcohol to prepare a storage solution. The recommended concentration is 100-200mM. The effective working concentration of PMSF is 0.1-1mM.

PMSF (苯甲基磺酰氟)是一种不可逆的丝氨酸蛋白酶抑制剂,常在细胞或组织裂解之前加入裂解液中以预防蛋白的降解[1,2]PMSF能够有效抑制胰凝乳蛋白酶、胰蛋白酶、凝血酶等。PMSF的作用原理是能够特异性识别并磺化决定酶活性的丝氨酸残基活性位点。PMSF也是脂肪酸酰胺水解酶 (FAAH) 、半胱氨酸蛋白酶(如木瓜蛋白酶,DTT逆转其抑制活性)和哺乳动物来源的乙酰胆碱酯酶的抑制剂[3]PMSF对木瓜蛋白酶的抑制效果可被DTTDithiothreitol,二硫苏糖醇)逆转。

PMSF的失活随着pH值和温度的升高而增加。在25°CpH 7.07.58.0时,抑制剂的半衰期分别约为1105535分钟。在pH 8时,100μM PMSF25°C1小时内或在4°C22小时几乎完全失活。使用100%异丙醇制备的PMSF储备溶液在25°C下可稳定保存数月甚至更长。在25°CpH 7.0的条件下1周内,PMSF抑制的胰凝乳蛋白酶没有发生再激活[4]

在动物实验中,PMSF在剂量为120300mg/kg时具有显着的镇痛作用。亚镇痛剂量 (60 mg/kg, i.p.) PMSF可以降低阿片类药物的急性和慢性给药导致的耐受性[3]

PMSF可以单独使用,也常与其他蛋白酶抑制剂如胃抑肽酶A或者磷酸酶抑制剂如正钒酸钠混合使用。

PMSF难溶于水,且在水溶液中的稳定性很差,建议在使用前加入裂解液或其他水溶液中。PMSF粉末可用甲醇,乙醇或者异丙醇溶解配置储存液,推荐浓度100-200 mMPMSF的有效工作浓度为0.1-1 mM

实验参考方法

Animal experiment [1]:

Animal models

Adult male mice

Preparation Method

This assay measures analgesic activity. All animals were placed on a 55 ± 1 °C hot plate, and the latency time to either jumping or licking was recorded. The cut-off time was set as 15 s to protect mice from any damage. The antinociceptive effects of a single dose of morphine (10 mg/kg s.c.) and PMSF (60, 120, and 300 mg/kg) were determined.

Dosage form

60, 120, and 300 mg/kg, i.p.

Applications

The results suggest that the administration of the PMSF doses (120 and 300 mg/kg, i.p.) led to significant changes in the analgesic latency time, while administration with PMSF (60 mg/kg i.p.) had no significant difference.

References:

[1]: Akbarabadi E A, Vardanjani H R, Molavinia S, et al. PMSF Attenuates Morphine Antinociceptive Tolerance and Dependence in Mice: Its Association with the Oxidative Stress Suppression[J]. Iranian Journal of Pharmaceutical Research: IJPR, 2021, 20(3): 300.

化学性质

Cas No. 329-98-6 SDF
别名 苯甲基磺酰氟; Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride
化学名 phenylmethanesulfonyl fluoride
Canonical SMILES C1=CC=C(C=C1)CS(=O)(=O)F
分子式 C7H7FO2S 分子量 174.2
溶解度 ≥ 17.4mg/mL in DMSO 储存条件 Store at RT
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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 5.7405 mL 28.7026 mL 57.4053 mL
5 mM 1.1481 mL 5.7405 mL 11.4811 mL
10 mM 0.5741 mL 2.8703 mL 5.7405 mL
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