PMSF

Biological Activity

PMSF (Phenylmethyl sulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. PMSF rapidly inactivates purified chymotrypsin from human pancreas, although human trypsin is less susceptible to inhibition by PMSF. C14-labeled PMSF penetrates human red cells rapidly and inhibits acetylcholinesterase in situ. PMSF is known as phospholipase C inhibitor and also as acetylcholine esterase inhibitor. PMSF inhibits arachidonic acid release during first 4 minutes of ischemia. PMSF inhibits acetylcholine esterase activity in the early stage of complete cerebral ischemia, and induces an inhibition of increase of extracellular glutamate level. PMSF inhibits 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 is capable of altering the actions of anandamide in vitro by blocking its metabolism. Administration of PMSF in vivo produces cannabinoid effects by altering endogenous levels of anandamide and potentiates the effects of exogenously administered anandamide. ^[4] Administration of PMSF can induce both promotion and protection in organophosphorus ester-induced delayed neuropathy (OPIDN) in hens. Pretreatment with PMSF results in a leftward shift of the anandamide dose effect curves for antinociception and hypothermia in male mice. Acetylcholinesterase (AChE), a serine hydrolase, is potentially susceptible to inactivation by PMSF. Pretreatment with PMSF protects against the degradation of neurofilaments in tri-ortho-cresyl phosphate (TOCP) induced delayed neuropathy in hens. PMSF treatment enhances the behavioral effects of endogenous and exogenous cannabinoid agonists in mice or rats.

Product Citations

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  Cell Death Differ. 2022 Jul;29(7):1395-1408.

  SARS-CoV-2 membrane protein causes the mitochondrial apoptosis and pulmonary edema via targeting BOK
  PMSF purchased from AbMole

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  Front Pharmacol . 2022 Jul 18;13:943111.

  (±)-5-bromo-2-(5-fluoro-1-hydroxyamyl) Benzoate Protects Against Oxidative Stress Injury in PC12 Cells Exposed to H 2 O 2 Through Activation of Nrf2 Pathway
  PMSF purchased from AbMole

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  J Cell Mol Med. 2022 Jul;26(14):4048-4060.

  BRAF V600E protect from cell death via inhibition of the mitochondrial permeability transition in papillary and anaplastic thyroid cancers
  PMSF purchased from AbMole

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  Arch Virol. 2021 Aug;166(8):2173-2185.

  Interplay of the ubiquitin proteasome system and the innate immune response is essential for the replication of infectious bronchitis virus
  PMSF purchased from AbMole

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  Int J Mol Med. 2021 May;47(5):70.

  circNRIP1 facilitates keloid progression via FXR1‑mediated upregulation of miR‑503‑3p and miR‑503‑5p
  PMSF purchased from AbMole

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  Lipids Health Dis. 2021 Apr 26;20(1):40.

  Elucidation of SIRT-1/PGC-1α-associated mitochondrial dysfunction and autophagy in nonalcoholic fatty liver disease
  PMSF purchased from AbMole

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  Cells. 2021 Feb 18;10(2):430.

  Knockdown of AKT3 Activates HER2 and DDR Kinases in Bone-Seeking Breast Cancer Cells, Promotes Metastasis In Vivo and Attenuates the TGFβ/CTGF Axis
  PMSF purchased from AbMole

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  Mar Drυgs. 2020 Oct 28;18(11):538.

  Immunostimulatory Effects of Polysaccharides from Spirulina platensis In Vivo and Vitro and Their Activation Mechanism on RAW246.7 Macrophages
  PMSF purchased from AbMole

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  Mol Cell. 2020 Nov 19;80(4):607-620.e12.

  Paradoxical Mitophagy Regulation by PINK1 and TUFm
  PMSF purchased from AbMole

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  Drug Chem Toxicol. 2016 Oct;39(4):392-9.

  Effects of 2,4-dichlorophenoxyacetic acid on the ventral prostate of rats during the peri-pubertal, pubertal and adult stage
  PMSF purchased from AbMole

Chemical Information

Molecular Weight	174.19
Formula	C7H7FO2S
CAS Number	329-98-6
Solubility (25°C)	DMSO ≥ 40 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ehsan Asadi Akbarabadi, et al. PMSF Attenuates Morphine Antinociceptive Tolerance and Dependence in Mice: Its Association with the Oxidative Stress Suppression

[2] Gabriel S Santos, et al. Prolyl Endopeptidase-Like Facilitates the α-Synuclein Aggregation Seeding, and This Effect Is Reverted by Serine Peptidase Inhibitor PMSF

[3] T Irie, et al. Evaluation of phenylmethanesulfonyl fluoride (PMSF) as a tracer candidate mapping acetylcholinesterase in vivo

[4] C Pinsky, et al. Phenylmethylsulfonyl fluoride (PMSF) given systemically produces naloxone-reversible analgesia and potentiates effects of beta-endorphin given centrally

[5] M C Sekar, et al. Differential effects of phenylmethanesulfonyl fluoride (PMSF) on carbachol and potassium stimulated phosphoinositide turnover and contraction in longitudinal smooth muscle of guinea pig ileum