sPLA2-IIA Inhibitor I

Biochem/physiol Actions

Cell permeable: no

Reversible: no

Target IC₅₀: 12.8 µM against sPLA2-IIA (human type IIA secreted phospholipase A2

Primary TargetsPLA2-IIA (human type IIA secreted phospholipase A2

Product does not compete with ATP.

General description

A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a potent inhibitor of human type IIA secreted phospholipase A₂ (sPLA₂-IIA) (IC₅₀ = 12.8 µM). Reported to effectively block sPLA₂-IIA-induced PGE₂ production at 100 nM in human rheumatoid synoviocytes and is non-toxic at doses up to 10 µM. Does not have any significant effect on the activities of porcine sPLA₂-IB, Naja naja sPLA₂-IB, or Crotalus durissus sPLA₂-IIA at 10 µM.

A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a potent inhibitor of sPLA₂-IIA (human type IIA secreted phospholipase A₂; IC₅₀ = 12.8 µM). Shown to effectively block sPLA₂-IIA-induced PGE₂ production at 100 nM in human rheumatoid synoviocytes and is non-toxic at doses up to 10 µM. Does not have any significant effect on the activities of porcine sPLA₂-IB, Naja naja sPLA₂-IB, or Crotalus durissus sPLA₂-IIA even at 10 µM concentration.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Church, W.B., et al. 2001. J. Biol. Chem.276, 33156.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Sequence

cyclic(2-NaphthylAla-Leu-Ser-2-NaphthylAla-Arg)•TFA

Warning

Toxicity: Standard Handling (A)