Bpsbioscience/EPZ5676/27625-1/10 mg
商品编号：
27625-1
品牌：
bpsbioscience
市场价：
¥4700.00
美元价：
2820.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
MW: 562.7 Da
CAS Registry #: 1380288-87-8
Formula: C30H42N8O3
Target: Dot1L
Background:
EPZ5676 is a potent inhibitor of DOT1L histone methyltransferase that, according to X-ray crystallographic analysis, occupies the S-adenosyl methionine (SAM) binding pocket of DOT1L and induces conformational changes in DOT1L resulting in the opening of a hydrophobic pocket beyond the amino acid portion of SAM. EPZ5676 has been investigated for the treatment of MLL-rearranged leukemia in multiple studies where results have shown that EPZ5676 inhibits H3K79 methylation and the expression of MLL-fusion target gene and potently kills acute leukemia cell lines bearing MLL translocation.
Description:
EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM.
Synonym(s):
(2R,3S,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol
Purity:
≥98% by HPLC
Biological Activity:
EPZ5676 selectively inhibits DOTIL with an IC50 of 0.8 nM, which is 37000-fold greater in selectivity vs. other methyltransferases, including CARM1, EHMT1/2, EZH1/2, PRMT1/2/5/6/8, SETD7, SMYD2/3, and WHSC1/1L1. Inhibits H3K79 methylation in tumors.
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):
Daigle SR, et al. Blood. 2013 Aug 8;122(6):1017-1025.
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。
