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PMSF

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Chemical Structure| 329-98-6 同义名 : 苯甲基磺酰氟 ;NSC 88499;Benzylsulfonyl fluoride;Phenylmethylsulfonyl fluoride
CAS号 : 329-98-6
货号 : A767839
分子式 : C7H7FO2S
纯度 : 95%
分子量 : 174.193
MDL号 : MFCD00007424
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(1435.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Cysteine Protease
描述 Phenylmethanesulfonyl fluoride (PMSF) is an irreversible serine/cysteine protease inhibitor used in protein extraction experiment. It is also a putative inhibitor of phosphatidylinositol-specific phospholipase C, almost completely inhibited carbachol-stimulated inositol incorporation into phosphatidylinositol (PI) of longitudinal smooth muscle of guinea pig ileum, while it had no effect on potassium-stimulated inositol incorporation. PMSF (2 mM) inhibited carbachol-stimulated inositol phosphate accumulation in the presence of Li+ by only 15% - 19%[3]. Mice receiving i.p. injections of PMSF exhibited cannabinoid effects that included antinociception, hypothermia and immobility with ED50 values of 86, 224 and 206 mg/kg, respectively. Spontaneous activity was reduced at doses greater than 100 mg/kg. On the other hand, pretreatment with an inactive dose of PMSF (30 mg/kg) potentiated the effects of anandamide on tail-flick response (antinociception), spontaneous activity and mobility by 5-, 10- and 8-fold, respectively. PMSF did not alter anandamide's hypothermic effects[4]. PMSF inhibits the acylation of the inositol residue of GPI intermediates in bloodstream form T. brucei. PMSF inhihits the formntion of glycolipid C but does not inhibit fatty acid remodeling in vitro. PMSF inhihits GPI acylation and ethanolamine phosphatp addition in procyclic trypanosomes but not in Hela cells[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.74mL

1.15mL

0.57mL

28.70mL

5.74mL

2.87mL

57.41mL

11.48mL

5.74mL
参考文献

[1]Estevez J, Barril J, et al. Kinetics of inhibition of soluble peripheral nerve esterases by PMSF: a non-stable compound that potentiates the organophosphorus-induced delayed neurotoxicity. Arch Toxicol. 2012 May;86(5):767-77.

[2]Sheth AR, Gunjikar AN, et al. The presence of progressive motility sustaining factor (PMSF) in human epididymis. Andrologia. 1981 Mar-Apr;13(2):142-6.

[3]Sekar MC, Roufogalis BD. 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):191-203

[4]Compton DR, Martin BR. 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):1138-1143

[5]Güther ML, Masterson WJ, Ferguson MA. The effects of phenylmethylsulfonyl fluoride on inositol-acylation and fatty acid remodeling in African trypanosomes. J Biol Chem. 1994;269(28):18694-18701