MLL1 Methyltransferase Assay Service

Activity-based MLL1 Methyltransferase Assay for compound screening and profiling via radiometric HotSpotTM methyltranferase assay.
Target Overview
CAT#
MLL1
Enzyme
Human MLL1; 5 component complex
Synonym
Complex of MLL1: Histone-lysine N-methyltransferase MLL, CXXC-type zinc finger protein 7, ALL1, HTRX, KMT2A, TRX1, 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
Nucleosomes, 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)
SAH1,700
Sinefugin4,500
BIX01294>200,000
Chaetocin340
Scientific Information
MLL1 Q03164 (http://www.uniprot.org/uniprot/Q03164)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 MLL1
Reference compound IC50 for MLL1