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/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 1,900
Sinefugin 5,000
BIX01294 >500,000
Chaetocin 280

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, PA, USA

Further Information

More information can be found on our website Methyltransferase Assays.

Reference compound IC50 for MLL3

Reference compound IC50 for MLL3

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