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/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 1,700
Sinefugin 4,500
BIX01294 >200,000
Chaetocin 340

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, PA, USA

Further Information

More information can be found on our website Methyltransferase Assays.

Reference compound IC50 for MLL1

Reference compound IC50 for MLL1

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