SIRT1 Inhibitor/Activator Screening Kit (Fluorometric)

Description

SIRT1 or Sirtuin 1 is a member of the Silent Information Manager 2 family. SIRT1 is an NAD-dependent histone deacetylase that can deacetylate histones and many non-histone substrates (including p53). It is mainly located in the nucleus of normal cells. However, in cancer cells, it is mainly located in the cytoplasm. SIRT1 has been shown to regulate various cellular functions that affect metabolic homeostasis and aging. SIRT1 exerts anti-apoptotic, anti-oxidant and anti-inflammatory effects on cell damage, and protects cells by regulating mitochondrial biogenesis, autophagy and metabolism by responding to cell energy and redox state. SIRT1 also promotes vasodilation and protects vascular tissue. The activation and inhibition of SIRT1 is directed against various diseases. Unlike other known protein deacetylases that simply hydrolyze acetyllysine residues, sirtuin-mediated deacetylation reaction hydrolyzes acetyllysine and NAD. This hydrolysis produces deacetylated substrates, O-acetyl-ADP-ribose and nicotinamide, which themselves are inhibitors of sirtuin activity. In our SIRT1 inhibitor/activator screening kit, Sirtuin 1 deacetylates the substrate, and then cleaves the deacetylated substrate to release a fluorophore, which is at Ex / Em = 400/505 nm Fluorescence detection was carried out. In the presence of SIRT1 inhibitors, deacetylation is prevented, thereby preventing the cleavage of the substrate and the release of the fluorescent group. Compared with the control, the SIRT1 activator can enhance the activity of SIRT1, thereby generating a higher fluorescence signal. The kit provides a fast, simple, sensitive and reliable test, suitable for high-throughput screening of SIRT1 inhibitors/activators. Include an inhibitor control (Nicotinamide) to compare the efficacy of the tested inhibitor.
Screening/characterizing/studying SIRT1 inhibitors/activators

Relevant Diseases

Neurological Disorders

Detection Method

Fluorescence (Ex/Em = 400/505 nm)

Components

• SIRT1 Assay Buffer
• 1 M DTT
• Substrate (in DMSO)
• NAD
• SIRT1 Enzyme
• Inhibitor (Nicotinamide, 4 mM)
• Developer

Shipping

Dry Ice

Storage

-80°C

Research Use Only

For research use only

Target

SIRT1

Official Name

SIRT1

Full Name

Sirtuin 1

Alternative Names

Sirtuin 1; Regulatory Protein SIR2 Homolog 1; SIR2-Like Protein 1; SIR2L1; Sirtuin (Silent Mating Type Information Regulation 2, S. Cerevisiae, Homolog) 1; Sirtuin (Silent Mating Type Information Regulation 2 Homolog) 1 (S. Cerevisiae); NAD-Dependent Protein Deacetylase Sirtuin-1

Gene ID

23411(Human); 93759(Mouse); 309757(Rat)

Uniprot ID

Q96EB6(Human); Q923E4(Mouse)