CAS NO: | 1797983-32-4 |
规格: | 98% |
分子量: | 454 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Background:
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer. GSK-J4 is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 , an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base. However, the free base is a weak inhibitor of JMJD3 (IC50 >100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.