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Safety Information

EPI017

Sigma-Aldrich

SIRT6 Inhibitor Screening Kit (Fluorometric)

sufficient for 100 fluorometric tests

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About This Item

UNSPSC Code:
12352200

usage

sufficient for 100 fluorometric tests

detection method

fluorometric

storage temp.

−20°C

General description

SIRT6 or Sirtuin 6 proteins are a class of proteins that possess either histone deacetylase or mono-ribosyltransferase activity. SIRT6 is a nuclear sirtuin that has been associated with aging, cellular protection, sugar metabolism and certain types of cancer. Broad therapeutic applications are foreseen for SIRT6 inhibitors, including uses in diabetes, immune-mediated disorders, and cancer. Unlike other known protein deacetylases, which simply hydrolyze acetyl-lysine residues, the sirtuin-mediated deacetylation reaction hydrolyzes acetyl-lysine and NAD. This hydrolysis yields the deacetylated substrate, O-acetyl-ADP-ribose and nicotinamide, itself an inhibitor of sirtuin activity. Studies suggest that the human sirtuins may function as intracellular regulatory proteins with mono-ADP-ribosyltransferase activity. 

Features and Benefits

Compatible with high-throughput handling systems.

Suitability

Suitable for screening, characterizing and studying SIRT6 inhibitors

Principle

In this Sirtuin 6 inhibitor screening kit, Sirtuin 6 deacetylates the substrate, followed by cleavage of the deacetylated substrate to release the fluorescent group, which is detected fluorometrically (λex = 400 nm/λem = 505 nm).

Signal Word

Danger

Hazard Classifications

Acute Tox. 4 Dermal - Acute Tox. 4 Oral - Aquatic Chronic 3 - Eye Dam. 1 - Repr. 2 - Resp. Sens. 1 - Skin Irrit. 2 - Skin Sens. 1

Storage Class Code

10 - Combustible liquids

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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SIRT6 inhibitors with salicylate-like structure show immunosuppressive and chemosensitizing effects.
Damonte P, et al.
Bioorganic & Medicinal Chemistry, 25, 5849-5858 (2017)
Overexpression of sirtuin 6 suppresses inflammatory responses and bone destruction in mice with collagen-induced arthritis.
Lee HS, et al.
Arthritis and Rheumatism, 65, 1776-1785 (2013)
Neural sirtuin 6 (Sirt6) ablation attenuates somatic growth and causes obesity.
Schwer B, et al.
Proceedings of the National Academy of Sciences of the USA, 107, 21790-21794 (2010)
Sirtuin 6 protects cardiomyocytes from hypertrophy in vitro via inhibition of NF-?B-dependent transcriptional activity.
Yu SS, et al.
British Journal of Pharmacology, 168, 117-128 (2013)

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