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。
| 生物活性 | MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor ofPRMT4andPRMT6withIC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells[1]. |
体外研究
(In Vitro) | MS049 dihydrochloride (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM)[1].
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, IC50=1.4±0.1 μM) in HEK293 cells[1].
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[1].
Western Blot Analysis[1] | 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 (IC50=0.97±0.05 μM). |
Western Blot Analysis[1] | 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, IC50=1.4±0.1 μM) in HEK293 cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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