Biological Information
Background Information:
Histone methyl transferases catalyze the transfer of methyl groups to arginine and lysine groups of histones. There are two major histone methyl transferases: Lysine and arginine specific, both need S-Adenosyl methionine as a cofactor (methyl group donor). Histone methy transferases regulate gene expression by modulation of DNA packaging into chromatin; post-translational modifications of histones via methylation control chromatin structure, DNA accessibility, and recruitment of regulatory factors during transcription. Histone methylation plays an important epigenetic role by propagating chromatin states and gene expression patterns from mother to daughter cells.
Family:
Epigenetic
Sub Family:
Histone Methyltransferase (HMT)
Class:
Writer
Protein Name:
SUV39H1
Uniprot Number:
O43463
Gene Name:
SUV39H1
Gene ID:
6839
Gene Aliases:
KMT1A
Accession Number:
NM_003173
Organism:
Human
Construct Details:
Fragment (2-end), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant histone methyltransferase SUV39H1 expressed in a baculovirus infected Sf9 cells is used. Test compound and/or vehicle is preincubated with 0.5 μg/ml enzyme‡ in modified Tris-HCl buffer pH 8.5 for 120 minutes at 37°C. The reaction is initiated by adding 0.072 μM Histone H3 and 1.22 μCi [3H]AdoMet. An aliquot is removed and counted to determine the amount of [3H]CH3 peptide formed. Compounds are screened at 10 μM.
Substrate:
0.072 µM Histone H3
Incubation:
120 min at 37°C
Control Inhibitor:
Chaetocin
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
10
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei