PQA-18, Immunosuppressor

Product#: FDV-0009
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PQA-18, Immunosuppressor

Cat. No. FDV-0009
Chemical name 3-Methylbut-2-enyl 4,8-bis(3-methylbut-2-enyloxy)quinoline-2-carboxylate
Size 5 mg
Storage Store at -20℃. For reconstituted solution, store at +4℃. Protected from light
Reconstitution Reconstitute at 10 ~ 20 mM as stock solution in DMSO. ※In the case of poor solubility, vortex or heat it at 37℃.
CAS No. 1604678-82-1
Molecular formula C25H31NO4
Molecular weight 409.52
Solubility Soluble in DMSO
Purity  >=98%
License This product has been commercialized with a license from Tohoku University and Fukushima Medical University School of Medicine.
Warning Research use only. Not for use in humans.


Description

PQA-18 is a newly developed immunosuppressor. PQA-18 strongly inhibits p21-activated kinase 2 (PAK2), which is related to IL-2, IL-4, IL-6 and TNF-alpha production.

PQA-18 is the abbreviation of "Prenylated Quinolinecarboxylic Acid compound 18", and following effects are reported.

  • PAK2 activity is reduced in a dose-dependent manner, when PQA-18 is added to Jurkat cells.
  • IL-2, IL-4, IL-6 and TNF-alpha production are reduced, when PQA-18 is added to human peripheral lymphocytes stimulated for 24 hours by ConA (10 ug/ml).
  • Antigen specific immune reactions is inhibited when PQA-18 is intraperitoneally administered to mouse.
  • Nc/Nga mouse (13 weeks old), applied petrolatum ointment (100 mg) containing PQA-18 shows less skin irritation and blood IgE amount is reduced.
Product Background
PQA-18 is a novel small molecule which preserve prenylated quinolinecarboxylic acid (PQA) structure. PQA-18 exhibit suppression of IL2, IL4, IL6, and TNF-α production. Even in vivo, administration of PQA18 suppress the population of a subset of regulatory T cells and antigen-specific immune response in mice. Underlining mechanism of immunosuppressant effect of PQA-1 is through the inhibition of kinase activity of p21-activated kinase 2 (PAK2). PQA-18 may be safer immunosuppressant compound than others.

Features
  • Higher stability in blood compared to FK-506.
  • Compatible with in vivo and in vitro application.
  • CAS number : 1604678-82-1
  • Molecular Formula : C25H31NO4
  • Molecular Weight (Average) : 409.52
  • Purity : >98%
  • Solubility : DMSO *
* If you see insoluble, try vortex or heat at 37C. Recommended stock solution concentration is 10 - 20 mM.

Example Data
FDV-0009_1.jpg
PQA-18 is added to Jurkat cells. IL-2 production is reduced in a dose-dependent manner.

Reference
  • Ogura M, et al, Biochem Pharmacol, 105:55-65 (2016).
 
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