Cas No.: | 2095432-59-8 |
Chemical Name: | N-methyl-4-(phenylmethoxy)-1-piperidineethanamine,dihydrochloride |
Synonyms: | MS049 (hydrochloride);MS049 dihydrochloride |
SMILES: | C1C=C(COC2CCN(CCNC)CC2)C=CC=1.Cl.Cl |
Formula: | C15H26Cl2N2O |
M.Wt: | 321.285742282867 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM respectively. |
Target: | target: PRMT4, PRMT6; IC 50: 34 nM (PRMT4 ), 43 nM (PRMT6 ) |
In Vitro: | 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. |
References: | c[1]. Shen Y 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 Sep 15. |