| 产品名称 | GSK J4 HCl - Inhibitors / Activators - Demethylase(s) |
| 产品货号 | 27627-2 |
| 产品价格 | 现货询价，电话：010-67529703 |
| 产品规格 | 50 mg |
| 产品品牌 | bpsbioscience |
| 产品概述 | |
| 产品详情 |
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.
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