Activity-based SETDB1 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
SETDB1
Enzyme
Human SETDB1
Synonym
Histone-lysine N-methyltransferase SETDB1, ERG-associated protein with SET domain,
Histone H3-K9 methyltransferase 4, SET domain bifurcated 1, KG1T, KIAA0067, ESET, KMT1E, TDRD21
Substrates
Histone H3, 5 μM
SAM, 1 μM
Assay Properties
Reaction
S-adenosyl-L-[methyl-³H]methionine + histone L- lysine = S-adenosyl-L-homocysteine + histone [methyl-³H]-L- lysine
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| SAH | 3,400 |
| Chaetocin | 9,700 |
| Sinefungin | 120,000 |
Scientific Information
Q15047 (http://www.uniprot.org/uniprot/Q15047)
Screening Location
Malvern, USA
Further information
More information can be found on our website Methyltransferase Assay Services.
Reference compound IC50 for SETDB1
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