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EPZ020411 hydrochloride

Chemical Structure : EPZ020411 hydrochloride

CAS No.: 2070015-25-5

EPZ020411 hydrochloride (EPZ-020411 hydrochloride;EPZ 020411 hydrochloride)

Catalog No.: PC-43301Not For Human Use, Lab Use Only.

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).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EPZ020411 hydrochloride 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).
EPZ020411 dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression.
EPZ020411 exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

Physicochemical Properties

M.Wt 479.0551
Formula C25H39ClN4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

H2O: ≥ 41 mg/mL

Chemical Name/SMILES

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]-,hydrochloride

References

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

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