MS049 (hydrochloride) |
| カタログ番号GC14240 |
MS049 (塩酸塩) は、それぞれ 34 nM および 43 nM の IC50 を持つ PRMT4 および PRMT6 の強力で選択的な細胞活性二重阻害剤です。 MS049 (塩酸塩) は、HEK293 細胞の Med12me2a および H3R2me2a のレベルを低下させます。 MS049 (塩酸塩) は毒性がなく、HEK293 細胞の増殖には影響しません。
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Cas No.: 2095432-59-8
Sample solution is provided at 25 µL, 10mM.
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IC50: 34 nM for PRMT4; 43 nM for PRMT6
MS049 is a dual PRMT4 and PRMT6 inhibitor.
PRMTs have been reported to have a key role in the regulation of the arginine methylation pattern and level of a plethora of different substrates, including both histones and non-histone proteins. Therefore, the dysregulation of PRMTs has been linked to various human diseases.
In vitro: Previous study evaluated selectivity of MS049 and its two close analogs against other PRMTs. It was found that none of these compounds showed inhibition against PRMT5 and PRMT7. In addition, all three compounds were more potent against PRMT4 and PRMT6 than other type I PRMTs. MS049 showed good selectivity over PRMT8 (>30-fold) and excellent selectivity over PRMT1 and PRMT3 (>300-fold). Moreover, MS049 could reduce the H3R2me2a mark in HEK293 cells in a concentration dependent manner. The effect of the 8 μM MS049 treatment matched with that of the catalytically inactive mutant. In addition, MS049 treatment was able to inhibit endogenous PRMT4 methyltransferase activity in a concentration dependent manner leading to reduced levels of cellular asymmetric arginine dimethylation of Med12 in HEK293 cells [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Shen Y1 et al. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Oct 13;59(19):9124-9139.
| Cas No. | 2095432-59-8 | SDF | |
| Chemical Name | N-methyl-4-(phenylmethoxy)-1-piperidineethanamine, dihydrochloride | ||
| Canonical SMILES | CNCCN(CC1)CCC1OCC2=CC=CC=C2.Cl.Cl | ||
| Formula | C15H24N2O • 2HCl | M.Wt | 321.3 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1124 mL | 15.5618 mL | 31.1236 mL |
| 5 mM | 0.6225 mL | 3.1124 mL | 6.2247 mL |
| 10 mM | 0.3112 mL | 1.5562 mL | 3.1124 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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