GPS167 is a CLK kinase inhibitor that potently and selectively inhibits recombinant human CLK1 , CLK2 and CLK4 . By inhibiting CLK-mediated phosphorylation of SRSF10 , GPS167 upregulates the protein-binding ability of CLK1 and CLK4 with SRSF10, downregulates oncogenic BCLAF1-L and upregulates tumor-suppressive BCLAF1-S , regulates alternative splicing of genes such as MDM2 and MDM4 , stabilizes p53 protein and induces DNA damage, ultimately triggering tumor cell apoptosis . GPS167 can block the epithelial-mesenchymal transition process of tumors, activate intracellular double-stranded RNA-mediated antiviral immune responses, and produce synergistic cytotoxicity when combined with microtubule-targeting drugs. GPS167 can be used in research related to various cancers including colorectal cancer .
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