Bioactivity | LQ23 is a selective inhibitor for CDC2-like kinase 2 (CLK2) with an IC50 of 1.4 nM. LQ23 exhibits anti-inflammatory activity[1]. |
Target | IC50: 1.4 nM (CLK2), 2.1 nM (CLK1), 3.2 nM (CLK4), 21.7 nM (DYRK1A), >100 nM (CLK3) |
Invitro | LQ23 (10-100 nM) 剂量依赖性地抑制软骨细胞中 SR 蛋白磷酸化,从而调节基因的选择性切割[1]。LQ23 (10-100 nM) 剂量依赖性地抑制 HEK-293T 细胞中 CHIR99021 刺激的 Wnt 信号传导,IC50 为 2.9 μM[1]。LQ23 (30 nM) 通过促进骨间充质干细胞 (BMSC) 分化为软骨细胞并抑制软骨退化来改善骨关节炎[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> LQ23 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | LQ23 (1.5 μg/ kg,单次关节内注射) 在 Sprague-Dawley 大鼠 monosodium iodoacetate (MIA) 或 ACLT-pMMx 诱导的骨关节炎中表现出抑制炎症,保护软骨并改善关节功能的作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 2997615-62-8 |
Formula | C24H24N4OS |
Molar Mass | 416.54 |
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]. Sun Y, Hu T, Zhang M, Song J, Qin Z, Liu M, Ji J, Li Z, Qiu Z, Bian J. Structure-Guided Discovery of Potent and Selective CLK2 Inhibitors for the Treatment of Knee Osteoarthritis. J Med Chem. 2024 Mar 28;67(6):4603-4623. |