GSK J4 hydrochloride is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.
|Source||Mol Cells (2018). Figure 4. GSK J4|
|Cell Lines||THP-1 cells|
|Incubation Time||48 h|
|Results||To further determine the mechanisms underlying transcriptional regulation of p21 via KDM6B, we conducted luciferase reporter assay using p21-luciferase reporter system in HEK 293T cells. Ectopic expression of KDM6B accelerated p21 transcription (Fig. 4B), whereas KDM6B inhibition by GSK-J4 showed reduction of p21 expression|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
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