85-2073-52　Histone Lysine Demethylase Inhibitor VIII, GSK-J4 10mg　CAS No:1373423-53-0　217431

特徴

• A cell-permeable GSK-J1 prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50uM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-alpha production in primary human macrophage cultures (IC50 = 9uM by ELISA). GSK-J4 has been used to study the effect of KDM2B (Jumonji (JmjC) domain histone 3 lysine 36 (H3K36) di-demethylase) inhibition on the survival and DNA repair potential of glioblastoma cells. It has also been used in sulforhodamine B (SRB) cell growth assay and cell viability assay.
• Synonyms:GSK-J1 Pro-Drug, JHDM Inhibitor II Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate
• Molecular Formula:C₂₄H₂₇N₅O₂
• Molecular Weight:417.5
• Appearance:Tan semi-solid
• Purity:≥98% (HPLC)
• Primary Target:H3K27me3 demethylases JMJD3 & UTX
• Solubility:DMSO
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.