product name GSK-J4 HCl
Description: GSK J4 HCl is a novel, cell permeable, and potent prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF).
References: Nature. 2012 Aug 16;488(7411):404-8.
453.96
Formula
C24H27N5O2.HCl
CAS No.
1373423-53-0(free base)
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 90 mg/mL (198.2 mM)
Water: <1 mg/mL
Ethanol:
Solubility (In vivo)
2% DMSO+dd H2O: 10 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19428168
| In Vitro |
In vitro activity: GSK J4 HCl is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μM in vitro. GSK J4 HCl is used to probe the consequences of demethylation of H3K27me3. In human primary macrophages, GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). In addition, GSK-J4 prevents the lipopolysaccharide-induced loss of H3K27me3 associated with the TNF transcription start sites and blocked the recruitment of RNA polymerase II. Kinase Assay: Cell Assay: GSK J4 inhibited TNF-α protein production in a dose-dependent manner, with an IC50 value of 9 μM. Cells used: Human primary macrophages |
|---|---|
| In Vivo | GSK J4 showed significant growth-inhibitory activity against SF8628 subcutaneous tumors. |
| Animal model | Mice harboring subcutaneous SF8628 K27M xenografts |
| Formulation & Dosage | 100 mg/kg/day; i.p.; for 10 days |
| References | Nature. 2012 Aug 16;488(7411):404-8; Nat Med. 2014 Dec;20(12):1394-6. |
