PQA-18 is a unique PAK2 inhibitor (IC50: 10 nM). PQA-18 has immunosuppressive activity and can inhibit the production of IL2, IL4, IL6 and TNFα. PQA-18 can inhibit the number of regulatory T cell subsets and the production of immunoglobulins (Ig) against T cell-dependent antigens in mice, and can alleviate dermatitis symptoms in mice.

Physicochemical Properties

Molecular Formula	C25H31NO4
Molecular Weight	409.52
CAS #	1604678-82-1
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	PAK2 10 nM (IC50); IL-6 IL4 IL-2
ln Vitro	PQA-18 (0.1-20 μM, 6-24 h) inhibits ConA-induced production of IL2, IL4, IL6, and TNFα in human peripheral lymphocytes (IC50 of 450, 650, 580, and 460 nM, respectively) and IL2 protein and mRNA production in Jurkat cells (IC50: 400 nM)[1]. PQA-18 (10 μM) attenuates phosphorylation of cofilin-1 and histone H4 by inhibiting the corresponding kinases[1]. PQA-18 inhibits PAK2 activity by autophosphorylation at Ser141[1]. PQA-18 (0.1 nM-1 μM) inhibits PAK2 kinase activity in a non-competitive and concentration-dependent manner by autophosphorylation at Ser141 (IC50 of 10 nM, Km of 2.1 μM)[1].
ln Vivo	PQA-18 (0.5 mg/kg, intraperitoneal injection, three times a week) showed immunosuppressive activity in NP-CGG-immunized C57BL/6J mice, inhibiting the number of regulatory T cell subsets and the production of immunoglobulins (Ig) against T cell-dependent antigens [1]. PQA-18 ointment (100 mg/mouse, containing 0.05%-0.1% PQA-18, three times a week, 17 weeks) can improve dermatitis and IgE levels in Nc/Nga mice [1]. QA-18 (1 mg/kg, 6 weeks) had no significant effect on the liver and kidneys of mice [1].
Cell Assay	Real Time qPCR[1] Cell Types: Jurkat cells cultured with ConA Tested Tested Concentrations: 1, 10, 20 μM Incubation Duration: 6 h Experimental Results: Suppressed IL2 mRNA level in ConA-stimulated Jurkat cells. Affected ∼50% of IL2 transcripts at a high dose (10 μM).
Animal Protocol	Animal/Disease Models: Male C57BL/6J mice (10 weeks old) immunized by intraperitoneal injection of 50 μg NP-CGG[1] Doses: 0.5 mg/kg Route of Administration: Intraperitoneal injection (i.p.); three times a week Experimental Results: Suppressed the NP-specific responses (IgM, IgG1, and IgG3) in peripheral blood. Significantly suppressed the number of Foxp3+CD4+CD25+ cells in spleens.
References	[1]. Prenylated quinolinecarboxylic acid derivative suppresses immune response through inhibition of PAK2. Biochem Pharmacol. 2016 Apr 1;105:55-65.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4419 mL	12.2094 mL	24.4188 mL
	5 mM	0.4884 mL	2.4419 mL	4.8838 mL
	10 mM	0.2442 mL	1.2209 mL	2.4419 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.