EPZ020411 hydrochloride |
| رقم الكتالوجGC36000 |
هيدروكلوريد EPZ020411 هو مثبط انتقائي لـ PRMT6 مع IC50 من 10 نانومتر ، ولديه> 10 أضعاف انتقائية لـ PRMT6 على PRMT1 و PRMT8يمكن استخدام هيدروكلوريد EPZ020411 في أبحاث السرطان
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070015-25-5
Sample solution is provided at 25 µL, 10mM.
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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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