PQA-18 

PQA-18 is a unique PAK2 inhibitor (IC₅₀: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice^[1].

PQA-18 (0.1-20 μM, 6-24 h) markedly inhibits ConA (HY-P2149)-induced production of IL2, IL4, IL6 and TNFα in human peripheral lymphocytes (IC₅₀: 450, 650, 580 and 460 nM, respectively) and IL2 production at protein (IC₅₀: 400 nM) and mRNA levels in Jurkat cells^[1].
PQA-18 (10 μM) attenuates the phosphorylation of cofilin-1 and histone H4 by inhibiting the corresponding kinases^[1].
PQA-18 (0.1 nM-1 μM) inhibits PAK2 kinase activity in a non-competitive and concentration-dependent manner by its autophosphorylation at Ser141(IC₅₀ of 10 nM, K_m of 2.1 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PQA-18 (0.5 mg/kg, i.p., three times a week) displays immunosuppressing activity in C57BL/6J mice immunized with NP-CGG, with inhibiting the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens^[1].
PQA-18 ointment (100 mg/mouse, contains 0.05%-0.1% PQA-18, three times a week, 17 weeks) improves dermatitis and IgE levels in Nc/Nga mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

409.52

C₂₅H₃₁NO₄

1604678-82-1

O=C(C1=NC2=C(OC/C=C(C)/C)C=CC=C2C(OC/C=C(C)/C)=C1)OC/C=C(C)\C

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• [1]. Ogura M, et al. Prenylated quinolinecarboxylic acid derivative suppresses immune response through inhibition of PAK2. Biochem Pharmacol. 2016 Apr 1;105:55-65.  [Content Brief]