Inhibitor SourceBook™ Second Edition

Lipid Signaling
Phospholipase Inhibitors, continued
Product Cat. No. Comments Size Price
MJ33 475865 [1-Hexadecyl-3-(trifluoroethyl)-sn-glycero-2-phosphomethanol, Li]
A novel, active-site directed, specific, competitive, and reversible inhibitor
of PLA 2 . Shows high specificity for type I (pancreatic) and bee venom PLA 2 ,
but has relatively poor affinity for the type II human synovial PLA 2 . MJ33 has
shown inhibitory activity against a low pH calcium-independent enzyme, as
well as against the PLA 2 activity, which is responsible for permeability barrier
homeostasis or esophagitis.
Neomycin Sulfate 4801 An inhibitor of inositol phospholipid turnover. A non-specific PLC inhibitor. Also
inhibits phophatidylcholine-PLD activity (IC 50 = 65 mM).
Neomycin Sulfate,
g-Irradiated, Tissue Culture
Grade
480100 An inhibitor of inositol phospholipid turnover. A non-specific PLC inhibitor.
Also inhibits phophatidylcholine-PLD activity (IC 50 = 65 mM).
PACOCF 3 506274 (Palmitoyl Trifluoromethyl Ketone)
A novel Ca 2+ -independent PLA 2 inhibitor (IC 50 = 3.8 mM). May also inhibit
Ca 2+ -dependent PLA 2 at higher concentrations (IC 50 = 45 mM).
cPLA2a Inhibitor 525143 {N-{(2S,4R)-4-(Biphenyl-2-ylmethyl-isobutyl-amino)-1-[2-(2,4-difluorobenzoyl)benzoyl]-pyrrolidin-2-ylmethyl}-3-[4-(2,4-dioxothiazolidin-5-ylidenemethyl)phenyl]acrylamide,
HCl}
A cell-permeable, highly specific, potent inhibitor of cytosolic PLA2a
(IC 50 = .8 nM). Exhibits ~230-fold greater potency in enzyme assays and
~3900-fold greater potency in cellular assays compared to AACOCF 3
(Cat. No. 00 09).
sPLA 2 -IIA Inhibitor I 525145 [c(2NapA)LS(2NapA)R, TFA]
A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a
potent inhibitor of human type IIA secreted PLA 2 (IC 50 = 2.8 mM). Reported
to effectively block sPLA 2 -IIA-induced PGE 2 production at 00 nM in human
rheumatoid synoviocytes and is non-toxic at doses up to 0 mM. Does not affect
the activities of porcine sPLA 2 -IB, Naja naja sPLA 2 -IB, or Crotalus durissus
sPLA 2 -IIA even at 0 mM.
Quercetin, Dihydrate 551600 (3,3´,4´,5,7-Pentahydroxyflavone)
An inhibitor of PI 3-kinase (IC 50 = 3.8 mM) and phospholipase A2 (IC 50 = 2 mM).
Also inhibits mitochondrial ATPase, phosphodiesterases, and PKC.
Quinacrine, Dihydrochloride 551850 (Mepacrine)
A phospholipase A 2 inhibitor that also inhibits the activity of monoamine
oxidase.
Spermine,
Tetrahydrochloride
D-erythro-Sphingosine,
Dihydro-
5677 Polyamine that plays an important role in the regulation of cellular proliferation
and differentiation. Acts as an inhibitor of PLC-a and an activator of PLC-d.
300230 (Sphinganine)
Biosynthetic precursor of sphingosine. Inhibits PKC in Chinese hamster ovary
cells (IC 50 = 2.9 mM).
ST638 567790 [a-Cyano-(3-ethoxy-4-hydroxy-5-phenylthiomethyl)cinnamide]
A protein tyrosine kinase inhibitor (IC 50 = 370 nM) that also inhibits PLD activity
in human neutrophils.
U-73 22 662035 {1-[6-((17b-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione}
Inhibits agonist-induced PLC activation (IC 50 = .0–2. mM) in human platelets
and neutrophils.
U-73343 662041 {1-[6-((17b-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-2,5-pyrrolidinedione}
Analog of U-73 22 (Cat. No. 662035) that acts as a very weak inhibitor of PLC.
Suitable as a negative control.
5 mg $89
25 g $32
20 ml $55
5 mg $43
500 mg $ 73
mg $ 03
00 mg $33
00 mg $34
5 g $ 45
0 mg $79
5 mg $ 28
5 mg $95
5 mg $95
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