UNC0321

A highly potent inhibitor of G9a histone methyltransferase

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5mg

￥987.00

790.00

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10mg

￥1512.00

1210.00

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50mg

￥7012.00

5610.00

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100mg

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200mg

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Background

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 UNC0321 is a potent and selective G9a HMTase inhibitor, exhibiting a K_i value of 63 pM.⁴ UNC0321 inhibits G9a with assay-dependent IC₅₀ values of 6-9 nM and GLP, a closely-related H3K9 HMTase, with assay-dependent IC₅₀ values of 15-23 nM.⁴ It is more than 40,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and JMJD2E.⁴

1.Tachibana, 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 embryogenesisGenes Dev.16(14)1779-1791(2002) 2.Wagschal, A., Sutherland, H.G., Woodfine, K., et al.G9a histone methyltransferase contributes to imprinting in the mouse placentaMol. Cell Biol.28(3)1104-1113(2008) 3.Thomas, L.R., Miyashita, H., Cobb, R.M., et al.Functional analysis of histone methyltransferase G9a in B and T lymphocytesJ. Immunol.181(1)485-493(2008) 4.Liu, F., Chen, X., Allali-Hassani, A., et al.Protein lysine methyltransferase G9a inhibitors: Design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolinesJ. Med. Chem.53(15)5844-5857(2010)