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GSK-J2
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-J2图片
CAS NO:1394854-52-4
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)389.45
FormulaC22H23N5O2
CAS No.1394854-52-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>40 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILESO=C(O)CCNC1=NC(C2=CC=CN=C2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1
SynonymsGSKJ2; GSKJ 2; GSKJ-2
实验参考方法
In Vitro

In vitro activity: In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3.


Kinase Assay: purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·H2O, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.


Cell Assay: Interestingly, the relative selectivity of JIB-04 toward KDM5B over KDM5C in vitro translates to a ~10-50-fold greater growth-inhibitory activity against breast cancer cell lines.

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
ReferencesNature. 2012 Aug 16;488(7411):404-8; J Cell Biochem. 2015 Nov;116(11):2628-36