| Bioactivity | 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]. |
| Invitro | PQA-18 (0.1-20 μM, 6-24 h) 抑制 ConA (HY-P2149) 诱导的人外周淋巴细胞中 IL2、IL4、IL6、TNFα 的产生 (IC50 分别为 450、650、580 和 460 nM) 和 Jurkat 细胞中 IL2 蛋白和 mRNA 产生 (IC50: 400 nM)[1]。PQA-18 (10 μM) 通过抑制相应的激酶来减弱 cofilin-1 和 histone H4 的磷酸化[1]。PQA-18 通过在 Ser141 处的自磷酸化抑制 PAK2 的活性[1]。PQA-18 (0.1 nM-1 μM) 通过在 Ser141 处自磷酸化以非竞争性和浓度依赖性方式抑制 PAK2 激酶活性 (IC50 为 10 nM，Km 为 2.1 μM)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PQA-18 相关抗体: Real Time qPCR[1] Cell Line: |
| In Vivo | PQA-18 (0.5 mg/kg，腹腔注射，每周三次) 在 NP-CGG 免疫的 C57BL/6J 小鼠中显示出免疫抑制活性，可抑制调节性 T 细胞亚群的数量和针对 T 细胞依赖性抗原的免疫球蛋白 (Ig) 的产生[1]。PQA-18 软膏 (100 mg/小鼠，含 0.05%-0.1% PQA-18，每周三次，17 周) 可改善 Nc/Nga 小鼠的皮炎和 IgE 水平[1]。QA-18 (1 mg/kg，6周) 对小鼠肝脏和肾脏无明显影响[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 1604678-82-1 |
| Formula | C25H31NO4 |
| Molar Mass | 409.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ogura M, et al. Prenylated quinolinecarboxylic acid derivative suppresses immune response through inhibition of PAK2. Biochem Pharmacol. 2016 Apr 1;105:55-65. |