GSK-J5 Hydrochloride is a selective jumonji H3K27 demethylase inhibitor that modulates the proinflammatory macrophage response. The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.1,2 GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), 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.3 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.3 Storage and Stability: For long term storage, we suggest that GSK-J5 (hydrochloride) be stored as supplied at -20C. It should be stable for at least two years. GSK-J5 (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the GSK-J5 (hydrochloride) in the solvent of choice. GSK-J5 (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of GSK-J5 (hydrochloride) in ethanol is approximately 20 mg/ml and approximately 30 mg/ml in DMSO and DMF. GSK-J5 (hydrochloride) is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, GSK- J5 (hydrochloride) should first be dissolved in DMF and then diluted with the aqueous buffer of choice. GSK-J5 (hydrochloride) has a solubility of approximately 0.1 mg/ml in a 1:7 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.
Molecular Weight:
453.96
CAS Number:
[1394854-51-3]
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