Non-competitive
Puromycin-Sensitive Aminopeptidase (PSA) Inhibitor
PAQ-22
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Wako Catalog No. 165-23581 (10mg) for Cellbiology, Keep at RT
Puromycin-sensitive aminopeptidase (PSA), which is a neutral
aminopeptidase with a substrate specificity similar to that of
aminopeptidase N (APN), is distributed mainly in the brain and neurons.
Although PSA regarded as an enkephalin-degrading enzyme, the physical
roles/functions of PSA remain unclear.
PSA is possibly related to cell division and Apoptosis. PSA was reported
as a potent modifier of tau-induced pathology and was suggested as a
possible tau-degrading enzyme in an unknown mechanism in Alzheimer’s
disease.
PSA activity is inhibited by Puromycin but Puromycin also inhibits APN.
Wako has launched a non-peptide, small-molecular, non-competitive PSA
Inhibitor, PAQ-22 and the structurally modified fluorescent bioprobe,
DAMPAQ-22 (for detailed information, please see below).
Line weaver-Burk plot analysis of PSA inhibition by PAQ-22 and Puromycin
Using living human monocytic cell MOLT-4, which is known to express PSA, PSA inhibitory activity of
PAQ-22 and Puromycin was determined with an indicator, which is fluorescence generated from a fluorescent
substrate Ala-MCA broken down by PSA. Lineweaver-Burk plot indicated that PAQ-22 acts as specific
non-competitive inhibitor. On the other hand, Puromycin acts a competitive inhibitor. In addition, PAQ-22 and
DAMPAQ-22 are easily incorporated into MOLT-4 under the general cell culture conditions.
APN-Inhibitory Activity of PAQ-22 and Puromycin
PAQ-22
DAMPAQ-22
Puromycin
PSA IC50(µmol/L)
3.8
4.6
0.6
APN IC50(µmol/L)
>100
N/A
4.8
PSA- and APN-inhibitory activities were
assayed by the use of L-Ala-MCA with
MOLT-4. PAQ-22 is inactive toward
APN, indicating that PAQ-22 is specific
to PSA.
(These data were provided by Dr. Yuichi Hashimoto, Institute of Molecular and Cellular Biosciences, The University of Tokyo)
Fluorescent Bioprobe
for Visualization of PSA in Living Cells
DAMPAQ-22
Wako Catalog No. 049-30761 (2mg) for Cellbiology, Keep at RT
Wako has launched a non-peptide, small-molecular, non-competitive
PSA Inhibitor, PAQ-22(See above) and the structurally
modified fluorescent bioprobe, DAMPAQ-22. The cellular
localization of PSA within the living body could be specifically
visualized by the use of DAMPAQ-222)
IC50 : PSA 4.6 µmol/L (Please see the above table.)
No APN-inhibitory activity toward APN and LAP.
Visualization of PSA with DAMPAQ-22 in MOLT-4 cells
Fluorescent microscopic images of MOLT-4 cells treated with 10 µmol/L DAMPAQ-22 for
10 minutes.
(These data were provided by Dr. Yuichi Hashimoto, Institute of Molecular and Cellular Biosciences, The University of Tokyo)
References
1) Kakuta H, Tanatani A, Nagasawa K, Hashimoto Y.: "(1H,3H)-quinazolinedione skeleton", Chem. pharm. Bull, 51,
1273-82 (2003).
2) Kakuta, H., Koiso, Y., Nagasawa, K., Hashimoto, Y., "Fluorescent Bioprobes for Visualization of Puromycin-
Sensitive Aminopeptidase in Living Cells" Bioorg. Med. Chemd. Lett., 13, 83-6 (2003)
3) Bukowska A, Tadje J, Arndt M, Wolke C, Kähne T, Bartsch J, Faust J, Neubert K, Hashimoto Y, Lendeckel U.:
"Transcriptional regulation of cytosol and membrane alanyl-aminopeptidase in human T cell subsets", Biol
Chem., 384, 657-65 (2003)
4) Sànchez-Moràn, E., Jones, G.H., Franklin, F.C. and Santos, J.L. : Plant Cell, 16,2895 (2004)
5) Thielitz, A., Bukowska, A., Wolke, C., Vetter, R., Lendeckel, U., Wrenger, S., Hashimoto, Y., Ansorge, S.,Gollnick,
H. and Reinhold, D. : Biochem. Biophys. Res. Commun., 321, 795 (2004)
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