GSK3368715 3HCl

GSK3368715 3HCl (CAS No.: 2227587-26-8) is a rationally designed synthetic small-molecule trihydrochloride, classified as an epigenetic enzyme inhibitor, used to dissect arginine methylation regulatory networks in biomedical research and early-stage drug discovery; its mechanism of action is reversible, S-adenosylmethionine (SAM)-noncompetitive inhibition of type I protein arginine methyltransferases (PRMTs), targeting PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and it can modulate asymmetric dimethylation on histone and non-histone substrates, thereby affecting RNA processing events such as exon usage and remodeling PRMT-dependent transcriptional programs. In in vitro biochemical evaluations, this compound exhibits high potency, with reported Kiapp values of approximately 1.5–81 nM; enzymatic inhibition is generally in the low-nanomolar range for PRMT1, PRMT6, and PRMT8, in the tens-of-nanomolar range for PRMT3, and relatively weaker for PRMT4, approaching the micromolar range; overall in vitro activity can be summarized as spanning the nanomolar to micromolar range, depending on the subtype and experimental conditions. In cellular systems, it is used as a tool compound to assess pathway occupancy and methylation-state biomarkers, epitranscriptomic and alternative splicing effects, and downstream gene expression, and is commonly applied in biochemical profiling, target validation, mechanism-of-action studies, and phenotypic experiments in PRMT-related cellular models such as those derived from tumors; it may also be combined with exploratory animal models to elucidate PRMT biology and pathway dependency. The concentrations or doses used in experiments typically depend on the specific experimental design and research objectives. This product is for laboratory research use only, suitable for biochemical, cellular, and animal model studies, and is not intended for any human or veterinary use.