CLK2 inhibitor LQ23 is a potent, selective cdc2-like kinase 2 (CLK2) inhibitor with IC50 of 1.4 nM, >70-fold selecitve over CLK3.
LQ23 also display high potency against CLK1, CLK4 with IC50 of 2.1 nM and 3.4 nM.
LQ23 dose-dependently inhibit SR protein phosphorylation (pSRSF4, pSRSF5, and pSRSF6) in chondrocytes.
LQ23 treatment dose-dependently inhibits CHIR99021 (GSK3β inhibitor)-stimulated Wnt signaling in HEK-293T cells with EC50 of 2.9 uM.
LQ23 (30 nM) promotes the differentiation of BMSCs into chondrocytes in vitro, protectes chondrocytes and BMSCs from catabolic breakdown.
LQ23 (30 nM) inhibits inflammatory response in chondrocytes, effectively inhibits the expression of TNF-α, IL-6, and IL-β in TNF-α and Oncostatin M-stimulated chondrocytes.
LQ23 (1.5 ug/kg, IA injection) inhibits inflammation, protected cartilage, and improved function in the monosodium iodoacetate (MIA)-induced rat knee OA model.