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EPZ020411 HCl

Names

[ CAS No. ]:
1700663-41-7

[ Name ]:
EPZ020411 HCl

[Synonym ]:
N,N'-Dimethyl-N-({3-[4-({trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl}oxy)phenyl]-1H-pyrazol-4-yl}methyl)-1,2-ethanediamine
1,2-Ethanediamine, N,N-dimethyl-N-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-
EPZ020411 HCl
EPZ020411

Biological Activity

[Description]:

EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.IC50 value: 10 nMTarget: PRMT6in vitro: EPZ020411 inhibits methylation of PRMT6 substrates in cells. EPZ020411 does-dependently inhibits H3R2 methylation in PRMT6-overexpressing cells.in vivo: EPZ020411 shows good bioavailability following subcutaneous (SC) dosing in rats making it a suitable tool for in vivo studies.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Research Areas >> Cancer

[References]

[1]. Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659.


[Related Small Molecules]

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
619.2±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H38N4O3

[ Molecular Weight ]:
442.594

[ Flash Point ]:
328.3±31.5 °C

[ Exact Mass ]:
442.294403

[ LogP ]:
1.92

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.579

[ Storage condition ]:
-20℃

Related Compounds