MS049 (hydrochloride)
| 中文名称 | MS049 (hydrochloride) |
|---|---|
| 中文同义词 | 化合物 MS049 DIHYDROCHLORIDE;1-哌啶乙胺,N-甲基-4-(苯基甲氧基)-,盐酸盐(1:2) |
| 英文名称 | MS049 (hydrochloride) |
| 英文同义词 | MS049 (hydrochloride);MS049 dihydrochloride |
| CAS号 | 2095432-59-8 |
| 分子式 | C15H25ClN2O |
| 分子量 | 284.83 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2095432-59-8.mol |
| 结构式 |  |
MS049 (hydrochloride) 性质
| 溶解度 | DMF：30mg/mL； DMSO：30mg/mL；乙醇：30mg/mL； PBS（pH 7.2）：10 mg/mL |
|---|---|
| 形态 | 结晶固体 |
MS049 dihydrochloride 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 dihydrochloride 降低了 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。MS049 dihydrochloride 对 HEK293 细胞无毒，并且没有影响其的生长。
MS049 dihydrochloride (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 dihydrochloride (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 dihydrochloride 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. |