Activity-based MLL2 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
MLL2
Enzyme
Human MLL2; 5 component complex
Synonym
Complex of MLL2: Histone-lysine N-methyltransferase MLL2, ALL1-related protein, ALR, KMT2B, WDR5: WD repeat-containing protein 5, BMP2-induced 3-kb gene protein, RBBP5: Retinoblastoma-binding protein 5, Retinoblastoma-binding protein RBQ-3, ASH2L: Set1/Ash2 histone methyltransferase complex subunit ASH2, ASH2-like protein, DPY30: Protein dpy-30 homolog, Dpy-30-like protein
Substrates
Core Histone, 0.05 mg/mlSAM, 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 | 22,500 |
Sinefugin | 38,000 |
BIX01294 | >500,000 |
Chaetocin | 400 |
Scientific Information
Screening Location
Malvern, USA
Reference compound IC50 for MLL2