SET7/9 SAM-Screener™ Assay Kit | Cayman Chemical
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SET7/9 SAM-Screener™ Assay Kit

Item № 600490
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     384 wells $375.00 0.00
     1920 wells $1,400.00 0.00

Pricing updated 2018-11-15. Prices are subject to change without notice.

  • Homogeneous fluorescence polarization assay to screen for SAM-binding site inhibitors
  • Designed for high-throughput screening
  • Plate-based fluorescence polarization measurement (ex 575 nm, em 620 nm)
  • SET7/9 SAM-Binding Site Inhibitor Screening

Most histone lysine methyltransferases contain a conserved domain (SET) that utilizes S-adenosyl-L-methionine (SAM or AdoMet) as a co-factor to catalyze the methylation of lysine.1 SET7/9 (KMT7) is a SET domain-containing mono-methyltransferase that acts on a large number of histone and non-histone targets including histone H3, TAF10, p53, viral Tat, and estrogen receptor α.2,3 Given this broad substrate specificity, SET7/9 has important implications for a variety of human diseases, and SET7/9 has emerged as a model for studying the catalytic mechanism SET domain histone methyltransferases. This fluorescence polarization assay is based upon a proprietary small molecule fluorescent probe* that binds to the SAM binding pocket in SET7/9. Binding of the small molecule probe to SET7/9 induces an increase in fluorescence polarization. Binding of the probe can be competed with the endogenous cofactor SAM or by the inhibitor sinefungin, but is unaffected by the histone H3 peptide substrate. The SET7/9 SAM-Screener™ Assay is robust (Z’ >0.6) and exhibits a greater than 100 mP shift over a range of 0-250 nM SET7/9. The assay is suitable for high-throughput screening in the provided 384-well plate or can be scaled to higher density plate formats (e.g., 1,536-well) if desired.*United States Patent 9,120,820

Needed but not supplied: Please download the kit booklet to verify if UltraPure Water (Milli-Q or equivalent) or any other components are needed for this assay.

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Technical Information
  • SET7/9 SAM-Binding Site Inhibitor Screening

Warning - this product is not for human or veterinary use.

Shipping & Storage
Dry ice in continental US; may vary elsewhere
≥ 6 months
Downloads & Resources
Product Downloads

Download Kit Booklet

Download Safety Data Sheet (SDS)

Download free InChI Key generation software

Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

Get Batch-Specific Data and Documents by Batch Number

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data pack, and GC-MS data.

References & Product Citations
Product Description References

1. Bannister, A.J., and Kouzarides, T. Regulation of chromatin by histone modifications Cell Research 21, 381-395 (2011).

2. Couture, J.F., Collazo, E., Hauk, G., et al. Structural basis for the methylation site specificity of SET7/9 Nature Structural & Molecular Biology 13(2), 140-146 (2006).

3. Dhayalan, A., Kudithipudi, S., Rathert, P., et al. Specificity analysis-based identification of new methylation targets of the SET7/9 protein lysine methyltransferase Chemistry & Biology 18, 111-120 (2011).

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