2227587-26-8

GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM. GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.[1] GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.[1]

[1] Andrew Fedoriw, et al. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.