pCAF Inhibitor Screening Kit (Fluorometric)

pCAF (P300/CBP-associated factor, EC 2.3.1.48) also known as K (lysine) acetyltransferase 2B (KAT2B), possesses intrinsic histone acetyltransferase (HAT) activity. pCAF contributes to transcriptional activation by acetylating chromatin and transcription factors through its HAT activity. Deregulated HAT activity plays an important role in various cancers. pCAF inhibitors have potential applications in cancer therapy. pCAF uses both histone 3 (H3) and histone 4 (H4) as substrates. BioVision’s pCAF Inhibitor Screening Kit utilizes H3 peptide and Acetyl CoA as the substrates. pCAF acetylates the peptide and generates Coenzyme A with a free thiol group. The CoA is detected using a Thiol Detecting Probe that reacts with thiol groups and gives enhanced fluorescence that can be measured at Ex/Em = 392/482 nm. In the presence of pCAF specific inhibitors, the enzymatic activity is inhibited resulting in decreased or total loss of fluorescence. This assay kit is a simple, sensitive, and rapid tool to screen potential pCAF inhibitors.

• Detection method: Fluorescence (Ex/Em = 392/482 nm) • Applications: Screening/studying/characterizing potential inhibitors of pCAF

• Simple procedure; takes ~ 45 min • Fast and convenient • Kit contains the necessary reagents for testing putative pCAF inhibitors

pCAF

P300/CBP-associated factor Inhibitor Screening Kit (Fluorometric), K (lysine) acetyltransferase 2B Inhibitor Screening Kit (Fluorometric), KAT2B Inhibitor Screening Kit (Fluorometric)

• pCAF Assay Buffer • pCAF Enzyme • Acetyl CoA (Lyophilized) • H3 Peptide (Lyophilized) • Thiol Detecting Probe • pCAF Inhibitor (Garcinol)

-20°C

gel pack

12 months

see datasheet

Screening/studying/characterizing potential inhibitors of pCAF

Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.