sirtuin

Sirtuin modulator 1 (SRT3025 Hydrochloride) is a modulator of SIRT1 with EC1.5 of < 1 μM.

Sirtuin-1 inhibitor 1 is an inhibitor against deacetylase-1 (Sirtuin-1) and can be used to study senescence and cell death in the organism.

Sirtuin modulator 2 (N-(3-(imidazo[2,1-b]thiazol-6-yl)phenyl)-2-methoxybenzamide) exhibits antidiabetic, anti-inflammatory and antitumor activities.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator.

SIRT5 inhibitor 1 is a potent and selective inhibitor of human Sirtuin 5 deacylase (IC50: 0.11 μM) and is associated with aging-related diseases.

SIRT1-IN-1 is a selective inhibitor of SIRT1 with an IC50 of 205 nM. SIRT1-IN-1 is an inhibitor of cytomegalovirus (CMV) with antiviral activity.

Nicotinamide, a vitamin B3 derivative, is an inhibitor of SIRT1 (IC50=50-180 μM) and SIRT2 (IC50=2 μM). Nicotinamide can be used as a precursor of nicotinamide adenine dinucleotide or NAD+, which can be supplemented by dietary intake and can prevent or treat melanoglossia and pellagra.

Nicotinamide riboside increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic abnormalities.

Fisetin belongs to a group of natural flavonols with a variety of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-aging and neuroprotective effects.

Dihydrocoumarin (melilotin) is a compound found in Melilotus officinalis. Dihydrocoumarin is a yeast Sir2p inhibitor. Dihydrocoumarin also inhibits human SIRT1 and SIRT2 with IC50s of 208 μM and 295 μM, respectively.

AK-7 is a brain-permeable SIRT2 inhibitor and to characterize its cholesterol-reducing properties in neuronal models with an IC50 of 15.5 μM.

Nicotinamide riboside chloride, also known as NR and SRT647, is a pyridine-nucleoside form of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide or NAD+.

3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) is a selective SIRT3 inhibitor.

Resveratrol analog 1, an analog of Resveratrol, is a natural polyphenolic phytoalexin with antioxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.

SIRT-IN-1 is a potent inhibitor of SIRT1, SIRT2, and SIRT3, with IC50 values of 15, 10, and 33 μM, respectively

Selisistat R-enantiomer (EX-527 (R-enantiomer)) is a R-enantiomer of Selisistat (T6111) with much less activity than Selisistat (IC50 of SIRT1 > 100 μM).

Sirtuinmodulator 8 is a modulator of silent information regulator proteins (sirtuins) that activates their activity. It significantly reduces the expression of monocyte chemoattractant protein-1 (MCP-1) while enhancing the expression of fibroblast growth factor 21 (FGF21). Sirtuinmodulator 8 regulates the expression of genes related to inflammation and metabolism, showing potential for research into metabolic diseases [such as diabetes and obesity] and inflammatory diseases.

Thiomyristoyl is an effective and selective SIRT2 inhibitor (IC50: 28 nM). It inhibits SIRT1 (IC50: 98 μM) but no effect on SIRT3 even at 200 μM.

Gardenia yellow (Crocin I) has anti atherosclerosis and hypolipidemic effects.

CAY10602 is a SIRT1 activator derived from high throughput screening for compounds that enhance SIRT1-mediated deacetylation of a SIRT1-specific substrate. Functional assays indicate that CAY10602 dose-dependently suppresses NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, achieving approximately 75% inhibition at 60 μM without cytotoxicity.

1. Agrimol B is a main active ingredient isolated from Agrimonia pilosa Ledeb.