Biological Information

Background Information:

The acetylation state of histones is dependent on the activity of two proteins, histone acetyltransferase and histone deacetylase (HDAC), which acetylate and deacetylate histones, respectively. The human HDAC proteins are organized into classes based on their similarity to yeast HDAC proteins. Class I HDACs include HDAC1, HDAC2, HDAC3, and HDAC8, which are homologous to the yeast Rpd3 protein. Class II HDACs are similar to yeast HDA1 and include HDAC4, HDAC5, HDAC6, HDAC7, and HDAC9. Histone deacetylase inhibitors may induce apoptosis and find use as treatment for hematological malignancies.

Family:

Epigenetic

Sub Family:

Histone Deacetylase (HDAC)

Class:

Eraser

Protein Name:

HDAC8

Uniprot Number:

Q9BY41

Gene Name:

HDAC8

Gene ID:

55869

Gene Aliases:

RPD3

Accession Number:

NM_018486

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Substrate:

fluorogenic HDAC substrate (400 µM)

Incubation:

60 min at RT

Control Inhibitor:

Trichostatin A

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

10

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5186

Name

scriptaid

Measurement

750nM - IC50

PubChem ID

444732

Name

Trichostatin A

Measurement

710nM - IC50

PubChem ID

5222465

Name

Sodium butanoate

Measurement

50000nM - IC50

PubChem ID

Name

alpha -compound 8

Measurement

1400nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault