Physicochemical Properties
Molecular Formula | C24H24N4OS |
Molecular Weight | 416.54 |
CAS # | 2997615-62-8 |
Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
Targets | IC50: 1.4 nM (CLK2), 2.1 nM (CLK1), 3.2 nM (CLK4), 21.7 nM (DYRK1A), >100 nM (CLK3) |
ln Vitro | LQ23 (10-100 nM) dose-dependently inhibits SR protein phosphorylation in chondrocytes, thereby regulating the selective cleavage of genes[1]. LQ23 (10-100 nM) dose-dependently inhibits CHIR99021-stimulated Wnt signaling in HEK-293T cells with an IC50 of 2.9 μM[1]. LQ23 (30 nM) improves osteoarthritis by promoting the differentiation of bone mesenchymal stem cells (BMSCs) into chondrocytes and inhibiting cartilage degradation[1]. |
ln Vivo | LQ23 (1.5 μg/kg, single intra-articular injection) inhibits inflammation, protects cartilage, and improves joint function in Sprague-Dawley rats with osteoarthritis induced by monosodium iodoacetate (MIA) or ACLT-pMMx [1]. |
Cell Assay |
Western Blot Analysis[1] Cell Types: Chondrocytes Tested Tested Concentrations: 10-100 nM Incubation Duration: 1 h Experimental Results: Reduced phosphorylated SRSF4, SRSF5 and SRSF6. Reduced levels of β-catenin and c myc. |
Animal Protocol |
Animal/Disease Models: MIA-/ACLT-pMMx-induced osteoarthritis in Sprague-Dawley rats model[1] Doses: 1.5 μg/ kg Route of Administration: Single IA injection Experimental Results: Ameliorated the surface of the articular cartilage and the cell arrangement, reduced the thickness of the synovium, increased the gap between the femur and the tibia. Reduced the levels of inflammatory cytokines and catabolic enzymes. |
References |
[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. |
Solubility Data
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4007 mL | 12.0036 mL | 24.0073 mL | |
5 mM | 0.4801 mL | 2.4007 mL | 4.8015 mL | |
10 mM | 0.2401 mL | 1.2004 mL | 2.4007 mL |