Activity-based NSD1 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
NSD1
Enzyme
Human NSD1
Synonym
Probable histone-lysine N-methyltransferase H3 lysine-36 and H4 lysine-20 specific, Androgen receptor coactivator 267 kDa protein, Androgen receptor-associated protein of 267 kDa, H3-K36-HMTase, H4-K20-HMTase, Lysine N-methyltransferase 3B, Nuclear receptor-binding SET domain-containing protein 1, ARA267, KMT3B
Substrates
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 [methyl-³H]-L- lysine
Readout
Enzymatic activity
Reference Compound IC50s
| Compounds | IC50 (nM) |
|---|---|
| SAH | 45,000 |
| Sinefugin | 110,000 |
| BIX01294 | >200,000 |
| Chaetocin | 2,300 |
Scientific Information
Q96L73 (http://www.uniprot.org/uniprot/O96L73)
Screening Location
Malvern, USA
Reference compound IC50 for NSD1
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