中文同义词:
PRMT4和PRMT6双重抑制剂(MS049);化合物MS049
英文同义词:
MS049;MS049 2HCl;2-[4-(benzyloxy)piperidin-1-yl]ethyl}(methyl)amine;MS049;MS-049;MS 049;1-Piperidineethanamine, N-methyl-4-(phenylmethoxy)-
沸点
352.6±37.0 °C(Predicted)
密度
1.03±0.1 g/cm3(Predicted)
酸度系数(pKa)
10.48±0.10(Predicted)
生物活性
MS049 是一种高效、选择性和细胞活性的 PRMT4 和 PRMT6 双重抑制剂，IC50 分别为 34 nM 和 43 nM。MS049 降低了 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。MS049 对 HEK293 细胞无毒，并且没有影响其的生长。
靶点
IC50: 34 nM (PRMT4), 43 nM (PRMT6)
体外研究
MS049 (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC 50 =0.97±0.05 μM).
MS049 (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC 50 =1.4±0.1 μM) in HEK293 cells.
MS049 is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets.
Western Blot Analysis
Cell Line: HEK293 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 20 hours
Result: Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC 50 =0.97±0.05 μM).
Western Blot Analysis
Cell Line: HEK293 cells
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC 50 =1.4±0.1 μM) in HEK293 cells.
Concentration:
0.1, 1, 10 μM
Result:
Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC 50 =0.97±0.05 μM).
Concentration:
0.1, 1, 10, 100 μM
Result:
Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC 50 =1.4±0.1 μM) in HEK293 cells.
