Activity-based PRMT1 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
PRMT1
Enzyme
Human PRMT1
Synonym
Protein arginine N-methyltransferase 1, Interferon receptor 1-bound protein 4, HMT2, HRMT1L2, IR1B4, ANM1
Substrates HotSpot assay:
Histone H4, 5 µM; SAM, 1 µM
Substrates FlashPlate assay:
H4 (1-15)-Biotin, 40 nM; SAM, 1 µM
Assay Properties
Reaction
S-adenosyl-L-[methyl-³H]methionine + histone L-arginine = S-adenosyl-L-homocysteine + histone [methyl-³H]-L- arginine
Readout
Enzymatic activity
Reference Compound IC50s HotSpotTM assay
| Compounds | IC50 (nM) |
|---|---|
| SAH | 97 |
| Sinefugin | 110 |
| GSK 3368715 | 65 |
Reference Compound IC50s FlashPlate Assay
| Compounds | IC50 (nM) |
|---|---|
| SAH | 5,500 |
| Sinefugin | 720 |
| GSK 3368715 | 2.3 |
Scientific Information
Q99873 (http://www.uniprot.org/uniprot/Q99873)
Screening Location
Malvern, USA
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