SGC707 (1687736-54-4) is a potent (IC50?= 31 nM) and selective allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).1? Selective against 31 other methyltransferases. An extremely useful probe for investigating the role of PRMT3 in normal and pathophysiology. Cell permeable and active in vivo.
SGC 707 is a potent, selective and cell-active allosteric inhibitor of PRMT3.
the ic50 and kd value of sgc707 against prmt3was 31 ± 2 nm and 53 ± 2 nm respectively. sgc707 showed an outstanding selectivity for prmt3 against 31 other methyltransferases and a broad range of 250 non-epigenetic targets, g protein-coupled receptors (gpcrs), ion channels, and transporters. the residence time of sgc707 was 9.7 min. in both hek293 and a549 cells, sgc707 stabilized prmt3 with ec50 values of 1.3 μm and 1.6 μm, respectively. sgc707 treatment at high concentrations 50 and 100 mm for 72 h lead to some toxicity [1].
in cd-1 male mice, intraperitoneal injection of sgc707 at 30 mg/kg for over 6 h showed good plasma exposure with the peak plasma level of 38 μm. after injection 6 h, the plasma level of sgc707 decreased to 208 nm. the half-life of sgc707 was about 1 h. the 30 mg/kg dose was well tolerated in the tested mouse model [1].
1) Kaniskan?et al. (2015), A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3); Angew. Chem. Int. Ed. Engl., 54?5166
