GSK591

GSK591 (also known as GSK3203591) is a potent and highly selective small-molecule inhibitor of Protein Arginine Methyltransferase 5 (PRMT5). Developed by GSK in collaboration with the Structural Genomics Consortium (SGC), it serves as a chemical probe to study the role of symmetric dimethylation of arginine (SDMA) in various biological processes. PRMT5 is an epigenetic enzyme that methylates histone and non-histone proteins, including RNA-binding proteins involved in splicing. GSK591 has demonstrated significant efficacy in preferentially killing spliceosomal-mutant leukemia cells, such as those with mutations in SRSF2, SF3B1, or U2AF1, by inducing splicing defects and subsequent cell-cycle arrest or apoptosis. It is often used in preclinical research to explore synergistic combinations with type I PRMT inhibitors or spliceosome modulators. GSK591 is closely related to the clinical candidate GSK3326595.

Other names

GSK3203591GSK-3203591GSK 3203591