Protein arginine methyltransferase 1 (PRMT1) is a major type 1 arginine methyltransferase associated with the activation of estrogen and androgen receptors; therefore, may represent a therapeutic target for hormone-dependent cancers. TC-E 5003 is an inhibitor of PRMT1 with an IC50 value of 1.5±0.2µM. The GI50 value of TC-E 5003 for the growth of MCF7a and LNCaP cell lines are 1.97 ± 0.14 and 4.49 ± 0.14µM, respectively.[1] TC-E 5003 at concentrations of 0.125 – 1µM dose-dependently suppressed lipopolysaccharide-induced nitric oxide (NO) production in RAW264.7 cells. Treatment with TC-E 5003 also markedly reduced the expressions of inducible NO synthase, cyclooxygenase-2, tumor necrosis factor-α, interleukin (IL)-1β, and IL-6, and downregulated the nuclear translocation of nuclear factor kappa B subunits.[2] TC-E-5003 at a dose of 0.5mg exerted an anti-tumor effect (31.76%) in A549 tumor-bearing mice.[3]
搜索
