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CLK2 inhibitor LQ23

Chemical Structure : CLK2 inhibitor LQ23

CAS No.: 2997615-62-8

CLK2 inhibitor LQ23 (LQ23)

Catalog No.: PC-22056Not For Human Use, Lab Use Only.

CLK2 inhibitor LQ23 is a potent, selective cdc2-like kinase 2 (CLK2) inhibitor with IC50 of 1.4 nM, >70-fold selecitve over CLK3.

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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 416.54
    Formula C24H24N4OS
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-4-Methyl-1-((5-(3-(thiophen-3-ylethynyl)-1H-indazol-5-yl)pyridin-3-yl)oxy)pentan-2-amine

    References

    1. Yongqiang Sun, et al. J Med Chem. 2024 Mar 18.

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