EPZ020411 hydrochloride |
Katalog-Nr.GC36000 |
EPZ020411 Hydrochlorid ist ein selektiver Inhibitor von PRMT6 mit einem IC50 von 10 nM, es hat eine >10-fache SelektivitÄt fÜr PRMT6 gegenÜber PRMT1 und PRMT8. EPZ020411 Hydrochlorid kann fÜr die Krebsforschung verwendet werden.
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Cas No.: 2070015-25-5
Sample solution is provided at 25 µL, 10mM.
EPZ020411 hydrochloride 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.
[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.
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