
Bpsbioscience/EPZ005687/27624-1/5 mg
商品编号:
27624-1
品牌:
bpsbioscience
市场价:
¥3200.00
美元价:
1920.00
联系Q Q:
3392242852
电话号码:
4000-520-616
电子邮箱:
info@ebiomall.com
商品介绍
MW: 539.7 Da
CAS Registry #: 1396772-26-1
Formula: C32H37N5O3
Target: EZH2
Background:
EPZ005687 is a potent inhibitor of EZH2, an enzymatic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of histone H3 lysine 27 (H3K27), that inhibits EZH2 with Ki of 24 nM, which is 500-fold and 50-fold greater in selectivity than 15 other protein methyltransferases and closely related EZH1 respectively. EPZ005687 concentration-dependently inhibits the enzymatic activity of PRC2 with IC50 of 54 nM through binding to the S-adenosylmethionine (SAM) pocket of the EZH2 SET domain. Study results have shown that EPZ005687 reduces H3K27 methylation in a variety of lymphoma cells and induces apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells.
Description:
EPZ-005687 is a potent and selective inhibitor of EZH2.
Synonym(s):
EPZ 005687; EPZ-005687; 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide
Purity:
≥98% by HPLC
Biological Activity:
Potent and selective EZH2 inhibitor with Ki of 24 nM. It exhibits 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
Solubility:
Soluble in DMSO
Storage / Stability:
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Reference(s):
Knutson SK, et al. Nat Chem Biol. 2012 Nov;8(11):890-6.
Scientific Category:
Methyltransferase inhibitor
Product Type:
Inhibitor
Data shown is lot-specific. Contact us for specific information on other lots.
品牌介绍
bpsbioscience简介:为生命科学研究提供ELISA试剂盒(仅供科研)、抗体和抗原(仅供科研)、流式抗体,使您的检测结果更稳定可靠,用心服务科研。我公司国内总代理,华东地区代理bpsbioscience 专业经营进口胎牛血清、细胞因子、ELISA试剂盒、细胞、抗体、生物试剂、耗材、培养基、一抗、二抗、其产品吸附均匀,吸附性好,空白值低,孔底透明度高,代做ELISA实验等。