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

PubChem ID

65482

Name

Sinefungin

Measurement

42μM - IC50

PubChem ID

11657687

Name

Chaetocin

Measurement

0.17μM - IC50

PubChem ID

73357457

Name

935693-62-2

Measurement

91μM - IC50

PubChem ID

Name

AdoHCys

Measurement

110μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei