The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.1,2,3 UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of <15 nM in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.4
1Tachibana, M., Sugimoto, K., Nozaki, M., et al. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis. Genes Dev161779-1791(2002).
2Wagschal, A., Sutherland, H.G., Woodfine, K., et al. G9a histone methyltransferase contributes to imprinting in the mouse placenta. Mol Cell Biol28(3)1104-1113(2008).
3Thomas, L.R., Miyashita, H., Cobb, R.M., et al. Functional analysis of histone methyltransferase G9a in B and T lymphocytes. J Immunol181485-493(2008).
4unlisted. G9a/GLP selective methyltransferase chemical probe, UNC0638. (2010).
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Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.
Manufacturer, supplier, and vendor of biochemical reagents, assay kits, forensic chemistry standards, antibodies, and proteins for scientific research
Analytical testing services and custom synthesis also available