PeptideDB

LQ23 2997615-62-8

LQ23 2997615-62-8

CAS No.: 2997615-62-8

LQ23 is a selective inhibitor of CDC2-like kinase 2 (CLK2) with IC50 of 1.4 nM. LQ23 exhibits anti-inflammatory activity
Sales Email:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

LQ23 is a selective inhibitor of CDC2-like kinase 2 (CLK2) with IC50 of 1.4 nM. LQ23 exhibits anti-inflammatory activity.

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
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.