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Cat. Number
065878998820396
Chemical Name
SET8 Methyltransferase Inhibitor Screening Assay Kit
References
Synonyms
  • SET domain-containing (lysine methyltransferase) 8
  • PR-Set7
  • SETD8
Stability 6 months
Storage -80°C
Shipping Dry ice in continental US; may vary elsewhere

Background Reading

Couture, J., Collazo, E., Brunzelle, J.S., et al. Structural and functional analysis of SET8, a histone H4 Lys-20 methyltransferase. Genes Dev 19 1455-1465 (2005).

Shi, X., Kachirskaia, I., Yamaguchi, H., et al. Modulation of p53 function by SET8-mediated methylation at lysine 382. Mol Cell 27(4) 636-646 (2007).

Song, M., and Ghosh, A. FGF2-induced chromatin remodeling regulates CNTF-mediated gene expression and astrocyte differentiation. Nat Neurosci 7(3) 229-235 (2004).

Chiang, P.K., Gordon, R.K., Tal, J., et al. S-adenosylmethionine and methylation. FASEB J 10 471-480 (1996).

Loenen, W.A.M. S-Adenosylmethionine: Jack of all trades and master of everything? Biochem Soc Trans 34(2) 330-333 (2006).

Yin, Y., Liu, C., Tsai, S.N., et al. SET8 recognizes the sequence RHRK20VLRDN within the N terminus of histone H4 and mono-methylates lysine 20. J Biol Chem 280(34) 30025-30031 (2005).

Dorgan, K.M., Wooderchak, W.L., Wynn, D.P., et al. An enzyme-coupled continuous spectrophotometric assay for S-adenosylmethionine-dependent methyltransferases. Anal Biochem 350 249-255 (2006).

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700350-96well
96-Well Cover Sheet
Half Volume 96-Well Solid Plate (black)
Methyltransferase Assay Buffer 1 ea
Methyltransferase Assay Buffer Additive 1 ea
Methyltransferase Enzyme Mixture 3 × 1 ea
Methyltransferase Assay AdoHcy Positive Control 1 ea
Methyltransferase Assay S-Adenosylmethionine 3 × 1 ea
Methyltransferase Fluorometric Mixture 3 × 1 ea
Methyltransferase DMSO 1 ea
SET8 (human recombinant) MT Assay Reagent 2 × 1 ea
SET8 Assay Acceptor Peptide 2 × 1 ea
Size Global Purchasing
96 wells  

Description

SET Domain-containing Protein 8 (SET8) is a methyltransferase that selectively mono-methylates histone H4 at lysine residue 20 (H4K20), an event proven to have an important role in chromatin structure and transcriptional activation. Cayman’s SET8 Methyltransferase Inhibitor Screening Assay provides a convenient method for screening human SET8 inhibitors. The transfer of the methyl group from SAM by SET8 (provided in the kit) to the acceptor peptide (H4K20) generates S-adenosylhomocysteine, which is rapidly converted to urate and hydrogen peroxide (H2O2) using an enzyme mixture provided in the kit. The H2O2 formed is quantified using 10-acetyl-3,7-dihydroxyphenoxazine (ADHP) to produce the highly fluorescent compound resorufin (excitation 530-540 nm; emission 585-595 nm).
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