CAS NO: | 2095432-59-8 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 321.29 |
---|---|
Formula | C15H26Cl2N2O |
CAS No. | 1502816-23-0(free base) |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 56 mg/mL (174.3 mM) |
Water: 56 mg/mL (174.3 mM) | |
Ethanol: 50 mg/mL (155.6 mM) | |
Other info | Chemical Name: [2-(4-Benzyloxy-piperidin-1-yl)-ethyl]-methyl-amine InChi Key: HBOJWAYLSJLULG-UHFFFAOYSA-N InChi Code: InChI=1S/C15H24N2O/c1-16-9-12-17-10-7-15(8-11-17)18-13-14-5-3-2-4-6-14/h2-6,15-16H,7-13H2,1H3 SMILES Code: CNCCN1CCC(OCC2=CC=CC=C2)CC1 |
Synonyms | MS049 diHCl; MS-049; MS 049. |
In Vitro | In vitro activity: MS049 does not inhibit any of the methyltransferases at 50 μM or demethylases at 10 μM and does not display appreciable binding to any of the methyllysine/methylarginine reader proteins using the DSF assay at 200 μM. MS049 demonstrated excellent selectivity over a broad range of epigenetic and nonepigenetic targets. In cellular assays, MS049 potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells. Cell Assay: MS 049 reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner. MS 049 treatment (72 h exposure) 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 (n = 3)) in HEK293 cells. |
---|---|
In Vivo | |
Animal model | |
Formulation & Dosage | |
References | J Med Chem. 2016 Oct 13;59(19):9124-9139. |