525145
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
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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Julien Pothlichet et al.
Frontiers in immunology, 13, 824746-824746 (2022-04-09)
The origin of the impaired CD4 T-cell response and immunodeficiency of HIV-infected patients is still only partially understood. We recently demonstrated that PLA2G1B phospholipase synergizes with the HIV gp41 envelope protein in HIV viremic plasma to induce large abnormal membrane
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