2095432-59-8
中文名稱(chēng)
MS049 (hydrochloride)
英文名稱(chēng)
MS049 (hydrochloride)
CAS
2095432-59-8
分子式
C15H25ClN2O
分子量
284.83
MOL 文件
2095432-59-8.mol
2095432-59-8 結(jié)構(gòu)式
基本信息
中文別名
化合物 MS049 DIHYDROCHLORIDE1-哌啶乙胺,N-甲基-4-(苯基甲氧基)-,鹽酸鹽(1:2)
英文別名
MS049 dihydrochlorideMS049 (hydrochloride)
物理化學(xué)性質(zhì)
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; PBS (pH 7.2): 10 mg/ml
形態(tài)A crystalline solid
常見(jiàn)問(wèn)題列表
生物活性
MS049 dihydrochloride 是一種高效、選擇性和細(xì)胞活性的 PRMT4 和 PRMT6 雙重抑制劑，IC50 分別為 34 nM 和 43 nM。MS049 dihydrochloride 降低了 HEK293 細(xì)胞的 Med12me2a 和 H3R2me2a 水平。MS049 dihydrochloride 對(duì) HEK293 細(xì)胞無(wú)毒，并且沒(méi)有影響其的生長(zhǎng)。體外研究
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. |