Biological Activity
GPS167 is a specific small molecule splicing regulator SRSF10 inhibitor, modulates BCLAF1 splicing with IC50 of 2 uM in human colorectal HCT116 cells, directly inhibits CLK1, CLK2 and CLK4, but not SRPK1 and DYRK1A.GPS167 promotes the dephoshorylation of SRSF10 and changes its interaction with partner proteins.GPS167 treatment leads to a partial dephosphorylation of SRSF10 and increases the recovery of CLK1 and CLK4.GPS167 impairs the growth of cancer cell line, elicits p53-dependent cytotoxicity.GPS167 is cytotoxic for human colorectal cancer organoids but not normal organoids.
In Vitro
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In Vivo
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References & source
1. Muhammad Sohail, et al. NAR Cancer. 2021 May 25;3(2):zcab019.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.