EPZ020411 dihydrochloride ( EPZ 020411 )

Catalog No. M13294 CAS No. 2095432-47-4

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Product Name

EPZ020411 dihydrochloride
Note

Research use only, not for human use.
Brief Description

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8.
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.
Synonyms

EPZ 020411
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Other Indications
Indication

——

CAS Number

2095432-47-4
Formula Weight

515.52
Molecular Formula

C25H40Cl2N4O3
Purity

>98% (HPLC)
Solubility

——
SMILES

CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4.Cl.Cl
Chemical Name

1,2-Ethanediamine, N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-,dihydrochloride

1. Mitchell LH, et al. ACS Med Chem Lett. 2015 Apr 6;6(6):655-9.

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