Bpsbioscience/SGC 0946/27649-1/10 mg
商品编号：
27649-1
品牌：
bpsbioscience
市场价：
¥3700.00
美元价：
2220.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
MW: 618.6 Da
Formula: C28H40BrN7O4
Target: DOT1L
Background:
DOT1L is a unique protein lysine methyltransferase (PKMT) catalyzing the methylation of histone H3 on Lysine 79 (H3K79). SGC 0946 is a potent and specific inhibitor of DOT1L . As a brominated analogue of EPZ004777, SGC 0946 exhibits substantially increased cellular inhibitory potency than its predecessor, where SGC 0946 reduces the methylation of H3K79 in both MCF10A (IC50: 8.8 nM) and A431 (IC50: 2.65 nM) cells compared with EPZ004777 (IC50: 84 nM and 264 nM respectively). This greatly increased cellular inhibitory potency of SGC 0946 can be attributed to lower off-rate and to improved cell permeability.
Description:
SGC 0946 is a potent small-molecule inhibitor specific for protein methyltransferase DOT1L
Synonym(s):
1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5--bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydro-xytetrahydrofuran-2-yl]methyl](isopropyl)amino]pro-pyl]-3-[4-(2,2-dimethylethyl)phenyl]urea
Biological Activity:
SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM. SGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs, including a panel of 12 PMTs and DNMT1. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation.
Solubility:
Soluble in DMSO 100 mg/ml or ethanol 100 mg/ml.
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):
Yu W, et al. Nat Commun. 2012;3:1288.
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。
