PMSF

Synonyms: Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride

PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.

PMSF  Chemical Structure

PMSF Chemical Structure

CAS No. 329-98-6

Purity & Quality Control

PMSF Related Products

Biological Activity

Description PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
Targets
cysteine protease [1] chymotrypsin [1]
In vitro
In vitro Although human trypsin is less susceptible to inhibition by PMSF, PMSF rapidly inactivates purified chymotrypsin from human pancreas. PMSF also rapidly inhibits acetylcholinesterase from human red cells. [1] As an inhibitor of phosphatidylinositol-specific phospholipase C, PMSF treatment at 2 mM almost completely inhibits carbachol-stimulated inositol incorporation into phosphatidylinositol (PI) of longitudinal smooth muscle of guinea pig ileum, while it has no effect on potassium-stimulated inositol incorporation. In contrast to its specific inhibition of carbachol-stimulated phosphoinositide turnover, PMSF produces a transient inhibition of contraction by both carbachol and potassium. [3] PMSF has been shown to inhibit the addition of ethanolamine phosphate to glycosylphosphatidylinositol (GPI) intermediates in Trypanosoma brucei. PMSF also inhibits the acylation of the inositol residue of GPI intermediates in bloodstream form T. brucei. PMSF inhibits ethanolamine phosphate addition and inositol acylation for procyclic forms of T. brucei but not for mammalian HeLa cells. [4] PMSF is the more reactive inactivator of mouse acetylcholinesterase (AChE), as the 8-fold higher BSF concentration is necessary to achieve even a 6-fold slower inactivation than that using PMSF. [7]
In Vivo
In vivo Intraperitoneal injection of PMSF produces dose-dependent analgesia in Sprague-Dawley rats. PMSF significantly enhances the analgesic effect of beta-endorphin (END) in rats. [2] Mice receiving i.p. injections of PMSF exhibit cannabinoid effects that include antinociception, hypothermia and immobility with ED50 of 86 mg/kg, 224 mg/kg and 206 mg/kg, respectively. Pretreatment with an inactive dose of PMSF (30 mg/kg) enhances the effects of anandamide on tail-flick response (antinociception), spontaneous activity and mobility by 5-, 10- and 8-fold, respectively. [5] Administration of PMSF 12 hours prior to PSP causes complete protection in organophosphorus ester-induced delayed neuropathy (OPIDN) in hens, but PMSF administered 4 hours after PSP potentiates its neurotoxic effects. [6] Pretreatment with PMSF (30 mg/kg, i.p.) prior to an injection of 1 or 10 mg/kg 3H-anandamide results 5 minutes later in enhanced brain levels of anandamide compared to those obtained with 3H-anandamide plus vehicle injection. [8] Pretreatment with PMSF inhibits tri-ortho-cresyl phosphate (TOCP)-induced neurofilament (NF) degradation, and protects hens against the development of organophosphate-induced delayed neuropathy (OPIDN). [9] Administration of PMSF enhances the characteristic cannabimimetic effects of Δ(9)-tetrahydrocannabinol (THC) or anandamide (AEA) in ICR mice, by inhibiting the enzyme fatty acid amide hydrolase. [10]
Animal Research Animal Models Male ICR mice subjected to anandamide injection
Dosages ~1000 mg/kg
Administration Administered i.p. 10 minutes before i.v. anandamide injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04062786 Unknown status
Scheduled Heart Surgery|Valve Replacement|Coronary Artery Bypass
University Hospital Strasbourg France
February 21 2019 --
NCT03300323 Unknown status
Peri-operative Fluid Management
St George''s Healthcare NHS Trust
October 2017 Not Applicable
NCT02569008 Completed
Post Cardiac Surgery
St George''s University of London
January 2014 Not Applicable

Chemical Information & Solubility

Molecular Weight 174.19 Formula

C7H7FO2S

CAS No. 329-98-6 SDF Download PMSF SDF
Smiles C1=CC=C(C=C1)CS(=O)(=O)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 35 mg/mL ( (200.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 35 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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