Cas No.: | 2095432-47-4 |
Chemical Name: | N1,N2-dimethyl-N1-((3-(4-((1r,3r)-3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine dihydrochloride |
Synonyms: | EPZ020411; EPZ-020411; EPZ 020411; EPZ020411 HCl; EPZ020411 hydrochloride |
SMILES: | C(N(C)CC1=CNN=C1C1=CC=C(O[C@H]2C[C@H](OCCC3CCOCC3)C2)C=C1)CNC.[H]Cl.[H]Cl |
Formula: | C25H40Cl2N4O3 |
M.Wt: | 515.52 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7); dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression; exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies. |