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

PubChem ID

167551

Name

Anacardic Acid

Measurement

910nM - IC50

PubChem ID

969516

Name

Curcumin

Measurement

87000nM - IC50

PubChem ID

3037648

Name

MB 3

Measurement

25000nM - IC50

PubChem ID

5490884

Name

Garcinol

Measurement

4900nM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault