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Synthesis and Activity of N-oxalylglycine and Its Derivatives as Jumonji C-domain-containing Histone Lysine Demethylase Inhibitors

Shohei Hamada, Tae-Dong Kim, Takayoshi Suzuki, Yukihiro Itoh, Hiroki Tsumoto, Hidehiko Nakagawa, Ralf Janknecht, Naoki Miyata

Bioorg Med Chem Lett. 2009 May 15;19(10):2852-5.

PMID: 19359167

Abstract:

N-Oxalylglycine (NOG) derivatives were synthesized, and their inhibitory effect on histone lysine demethylase activity was evaluated. NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme assays, and their dimethyl ester prodrugs DMOG and 21 exerted histone lysine methylating activity in cellular assays.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR4244394 N-Oxalylglycine N-Oxalylglycine Price
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