ART NR.: Cay700350-96 (96 wells)
Anwendungen: SET8 inhibitor screening
UniProt ID: Q9NQR1
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Schlagworte: KMT5A, SETD8, PR-Set7, PR/SET07, EC=2.1.1.-, EC=220.127.116.11, H4-K20-HMTase SETD8, Lysine N-methyltransferase 5A, SET domain-containing protein 8, N-lysine methyltransferase SETD8, PR/SET domain-containing protein 07
Caymans SET8 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET8 inhibitors. The transfer of the methyl group from SAM by SET8 to the acceptor peptide (H4K20) generates S-adenosylhomocysteine, which is rapidly converted to S-ribosylhomocysteine and adenine by adenosylhomocysteine nucleosidase. This rapid conversion prevents the buildup of adenosylhomocysteine and its feedback inhibition on the methylation reaction. Finally, the adenine is converted to hypoxanthine by adenine deaminase, which in turn is converted to urate and hydrogen peroxide (H2O2). The reaction between H2O2 and 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) produces the highly fluorescent compound resorufin. Resorufin fluorescence is analyzed using an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.