Biological Information
Background Information:
Histone acetyltransferases (HAT) are enzymes that covalently modify the N-terminal lysine of all four core histones in nucleosomes by the addition of acetyl groups from acetyl-CoA. HAT enzymes regulate transcription via chromatin remodeling; HAT’s are recruited on to the chromatin template and transcription is enhanced by acetylation of promoter proximal nucleosomal histones. Upon acetylation the histone complex relaxes facilitating other proteins to act on the DNA. P300 acetylase activity is not limited to histones since it can also acetylate non histone targets like p53 and ERa. P300 directly interacts with transcription factors and acts as a global transcriptional coactivator; it plays a critical role in a variety of cellular process including cell cycle control, differentiation, and apoptosis. P300 deregulation is believed to play an important role in Cancer.
Family:
Epigenetic
Sub Family:
Histone Acetyltransferase (HAT)
Class:
Writer
Protein Name:
P300
Uniprot Number:
Q09472
Protein Aliases:
histone acetyltransferase p300
Gene Name:
EP300
Gene ID:
2033
Gene Aliases:
p300|KAT3B
Accession Number:
NM_001429
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Substrate:
Histone H3 full length (10 nM)
Tracer:
[3H] Acetyl-coenzyme A (25 nM)
Incubation:
10 min at RT
Control Inhibitor:
Garcinol
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
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault