1502816-23-0

生物活性靶点体外研究 1502816-23-0 试剂级价格

1502816-23-0

CAS号:1502816-23-0
英文名:MS049
中文名:1502816-23-0
CBNumber:CB43128918
分子式:C15H24N2O
分子量:248.36
MOL File:1502816-23-0.mol

1502816-23-0化学性质

沸点 :352.6±37.0 °C(Predicted)
密度 :1.03±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: ≥ 31 mg/mL (124.82 mM)
形态 :Solid
酸度系数(pKa) :10.48±0.10(Predicted)
颜色 :Light yellow to yellow
水溶解性 :H2O: 20mg/mL, clear

1502816-23-0性质、用途与生产工艺

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.