Activity-based DOT1L Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
DOT1L
Enzyme
Human DOT1L
Synonym
Histone-lysine N-methyltransferase, H3 lysine-79 specific, Histone H3-K79 methyltransferase, H3-K79-HMTase, DOT1-like protein, Lysine N-methyltransferase 4, KIAA1814, KMT4
Substrates
Oligo Nucleosomes, 0.05 mg/ml
SAM, 1 µM
Assay Properties
Reaction
S-adenosyl-L-[methyl-³H]methionine + histone L-lysine = S-adenosyl-L-homocysteine + histone N⁶-[methyl-³H]-L-lysine
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| SAH | 450 |
| Sinefungin | 20,000 |
Scientific Information
Q8TEK3 (http://www.uniprot.org/uniprot/Q8TEK3)
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Methyltransferase Assays.
Reference compound IC50 for DOT1
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