Bpsbioscience/GSK J4 HCl/27627-2/50 mg
商品编号：
27627-2
品牌：
bpsbioscience
市场价：
¥8900.00
美元价：
5340.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
MW: 454 Da
CAS Registry #: 1373423-53-0
Formula: C24H27N5O2 • HCl
Target: JMJD3, UTX
Background:
GSK J4 is a potent cell-permeable inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3. GSK J4 is an ethyl ester derivative of GSK J1, a JMJD3 inhibitor (IC50= 60 nM) with restricted cellular permeability due to the highly polar carboxylate group, and rapidly hydrolyzed by macrophage esterase upon administration leading to the generation of pharmacologically relevant intracellular concentration of GSK-J1 . GSK J4 has been found to dose-dependently inhibit the production of tumor-necrosis factor-α (TNF-α), a LPS-driven cytokine involved in various fnflammatory disorders (IC50 = 9 µM).
Description:
GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.
Synonym(s):
ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
Purity:
≥98% by HPLC
Biological Activity:
Inhibits JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family (IC50 value > 50 µM).
Solubility:
Soluble in DMSO 84 mg/ml, water 84 mg/ml, ethanol 84 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):
Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8.
Scientific Category:
Demethylase 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。
