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GSK-J4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK-J4图片
CAS NO:1373423-53-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)417.5
FormulaC24H27N5O2
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: ≥ 36 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES O=C(OCC)CCNC1=NC(C2=NC=CC=C2)=NC(N3CCC4=CC=CC=C4CC3)=C1
Synonyms GSK-J-4; GSK-J 4; GSK-J4
实验参考方法
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: Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK J4 is an inhibitor of JMJD3 and UTX.


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 VivoGSK J4 showed significant growth-inhibitory activity against SF8628 subcutaneous tumors.
Animal modelMice harboring subcutaneous SF8628 K27M xenografts
Formulation & Dosage100 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.