PQA-18 is an inhibitor of p21-activated kinase 2 (PAK2; IC50 = 10 nM), an immunosuppressant, and a derivative of Ppc-1.1 It inhibits the production of IL-2 induced by concanavalin A in Jurkat T cells (IC50 = 400 nM). Topical application of PQA-18 (0.1%) decreases disease severity, serum IgE levels, and skin thickness in the NC/Nga mouse model of atopic dermatitis. It also reduces cutaneous nerve fiber density in NC/Nga mice when applied topically at 0.05%.2 PQA-18 (4 mg/kg) increases graft survival rate in a rat model of small intestine transplant.3
References:
[1]. Ogura, M., Kikuchi, H., Suzuki, T., et al.Prenylated quinolinecarboxylic acid derivative suppresses immune response through inhibition of PAK2Biochem Pharmacol.10555-65(2016).
[2]. Ogura, M., Endo, K., Suzuki, T., et al.Prenylated quinolinecarboxylic acid compound-18 prevents sensory nerve fiber outgrowth through inhibition of the interleukin-31 pathwayPLoS One16(2)e0246630(2021).
[3]. Kodama, T., Maeda, A., Lo, P.-C., et al.The effect of a novel immunosuppressive drug, a PAK-2 inhibitor, on macrophage differentiation/polarization in a rat small intestinal transplantation modelTranspl. Immunol.57101246(2019).