| Hazard Information | Back Directory | [Description]
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-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.3 For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 and GSK-J5 , respectively. See the Structural Genomics Consortium (SGC) website for more information. | [Uses]
GSK-J2 sodium is the sodium form of GSK-J2 (HY-15648A). GSK-J2 is an isomer of GSK-J1, and does not have any specific activity. GSK-J1 (HY-15648) is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A[1]. | [References]
1. Agger, K., Cloos, P.A.C., Christensen, J., et al. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development Nature 449(7163),731-734(2011).
2. Hübner, M.R., and Spector, D.L. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation Cold Spring Harb. Symp. Quant. Biol. 75,43-49(2010).
3. Kruidenier, L., Chung, C.W., Cheng, Z., et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response Nature 488,404-408(2012). |
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