MLL3 Methyltransferase Assay Service

Activity-based MLL3 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
MLL3
Enzyme
Human MLL3; 5 component complex
Synonym
Complex of MLL3: Histone-lysine N-methyltransferase MLL3, Homologous to ALR protein, HALR, KIAA1506, KMT2C, 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
CompoundsIC50 (nM)
SAH1,900
Sinefugin5,000
BIX01294>500,000
Chaetocin280
Scientific Information
MLL3 Q8NEZ4 (http://www.uniprot.org/uniprot/Q8NEZ4)WDR5 P61964 (http://www.uniprot.org/uniprot/P61964)RBBP5 Q15291 (http://www.uniprot.org/uniprot/Q15291)ASH2L Q9UBL3 (http://www.uniprot.org/uniprot/Q9UBL3)DPY30 Q9C005 (http://www.uniprot.org/uniprot/Q9C005)
Screening Location
Malvern, USA
Reference compound IC50 for MLL3
Reference compound IC50 for MLL3