产品
编 号:F286834
分子式:C19H19ClN4O5
分子量:418.83
产品类型
结构图
CAS No: 2366149-83-7
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产品详情
生物活性:
PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
体外研究:
PRMT5 IN-1 (0-500 nM) inhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×105 M-1 min-1] very rapidly with a Kinact of 0.068 min-1 and a good binding affinity (KI=55 nM).PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) inhibits the expression of cellular sDMA with an IC50 value of 0.012 μM.PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) inhibits cell proliferation in a dose-dependent manner with an IC50 value of 0.06 μM.