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525145

Sigma-Aldrich

sPLA2-IIA Inhibitor I

The sPLA₂-IIA Inhibitor I controls the biological activity of sPLA₂-IIA. This small molecule/inhibitor is primarily used for Cell Signaling applications.

Synonym(s):

sPLA2-IIA Inhibitor I, c(2NapA)LS(2NapA)R, TFA

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About This Item

Empirical Formula (Hill Notation):
C41H50N8O6 · xC2HF3O2
Molecular Weight:
750.89 (free base basis)
UNSPSC Code:
41106300
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

lyophilized solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)

color

white

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

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.

Biochem/physiol Actions

Cell permeable: no
Primary Target
sPLA2-IIA (human type IIA secreted phospholipase A2
Product does not compete with ATP.
Reversible: no
Target IC50: 12.8 µM against sPLA2-IIA (human type IIA secreted phospholipase A2

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

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

Other Notes

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

Legal Information

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

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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