SGC2085

SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins[1].

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

PRMT6:5.2 μM (IC50)

SGC2085 hydrochloride (1 μM, 10 μM, 50 μM；48 h) 对 21 种人类蛋白质甲基转移酶的具有完全选择性[1]。 SGC2085 hydrochloride (10 μM；48 h) 表现出低细胞渗透性，在 HEK293 细胞中无细胞活性[1]。

SGC2085 is dissolved in DMSO and diluted with appropriate medium before use. HEK293 cells are grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL). Thirty percent confluent cells are treated with inhibitors or DMSO. After 48 h, media are removed and cells are lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8.0, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% Triton X-100, 12.5 U/mL benzonase), complete EDTA-free protease inhibitor cocktail. After 3 min incubation at room temperature, SDS is added to 1% final concentration. Lysates are run on SDS-PAGE, and immunoblotting is done as outlined below to determine the levels of unmethylated and methylated BAF155[1].