GSK3368715 hydrochloride is a reversible, orally active inhibitor targeting type I protein arginine methyltransferases (PRMTs). It demonstrates potent inhibitory activity with IC50 values of 3.1 nM for PRMT1, 48 nM for PRMT3, 5.7 nM for PRMT6, and 1.7 nM for PRMT8, while exhibiting weaker activity against PRMT4 (IC50 1148 nM). This compound effectively induces changes in arginine methylation states, modifies exon usage, and exhibits significant anticancer effects, making it valuable for research in cancer biology and epigenetic regulation.
GSK3368715 hydrochloride is a reversible, orally active inhibitor targeting type I protein arginine methyltransferases (PRMTs). It demonstrates potent inhibitory activity with IC50 values of 3.1 nM for PRMT1, 48 nM for PRMT3, 5.7 nM for PRMT6, and 1.7 nM for PRMT8, while exhibiting weaker activity against PRMT4 (IC50 1148 nM). This compound effectively induces changes in arginine methylation states, modifies exon usage, and exhibits significant anticancer effects, making it valuable for research in cancer biology and epigenetic regulation.
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