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 (IC
50 > 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).
