PRMT1-IN-3 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), demonstrating an IC50 of 4.11 μM. In addition to its primary activity against PRMT1, it also inhibits PRMT6 and PRMT8 with IC50 values of 23.3 and 30.1 μM, respectively. PRMT1-IN-3 effectively reduces asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells, leading to cell cycle arrest, apoptosis, and decreased migration and colony formation in MDA-MB-231 cells. This compound serves as a potential chemotherapeutic sensitizer for Paclitaxel and is valuable for research concerning TNBC.
PRMT1-IN-3 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), demonstrating an IC50 of 4.11 μM. In addition to its primary activity against PRMT1, it also inhibits PRMT6 and PRMT8 with IC50 values of 23.3 and 30.1 μM, respectively. PRMT1-IN-3 effectively reduces asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells, leading to cell cycle arrest, apoptosis, and decreased migration and colony formation in MDA-MB-231 cells. This compound serves as a potential chemotherapeutic sensitizer for Paclitaxel and is valuable for research concerning TNBC.
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