sirt1

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.

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.

SRT 1720 dihydrochloride is a selective activator of SIRT1 (EC1.5: 0.16 μM) and shows less potent activities on SIRT2 (EC1.5: 37 μM) and SIRT3 (EC1.5: 300 μM).

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.

JGB1741 (ILS-JGB-1741) is a potent and selective inhibitor of SIRT1 with an IC50 of 15 μM. It modulates the Bax/Bcl2 ratio, cytochrome c release, and PARP cleavage, and increases acetylated p53 levels, leading to p53-mediated apoptosis. JGB1741 can be used in breast cancer studies.

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

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

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.

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.

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

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

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).

SRT1720 hydrochloride (SRT1720 HCl) is a selective activator of SIRT1 (EC1.5: 0.16 μM) and shows less potent activities on SIRT2/SIRT3 (EC1.5s: 37 μM/300 μM).

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.

Oxypaeoniflorin a monoterpene glycoside compound isolated from Paeoniae, is an antioxidant, is neuroprotective and anti-inflammatory.

Liriopesides B (Nolinospiroside F) exhibited potential anticancer activity against human ovarian cancer A2780 cells.

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.

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK/p38 MAPK pathways.

Sirtinol is a selective SIRT1/2 inhibitor (IC50: 131/38 μM).

BML-278 is a SIRT1 activator with an EC150 of 1 μM. It increases H3K9 methylation and inhibits H3K9 acetylation in parental and maternal prokaryotes, improving early embryonic development. BML-278 induces cell cycle arrest at the G1 S phase in primary human mesenchymal stromal cells, delaying senescence. It also reduces microtubule protein acetylation in U937 cells and increases mitochondrial density in mouse C2C12 myoblasts.

E1231 is an activator of SIRT1 . E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression.