Sirtuin

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.

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).

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.

MDL-800 is a SIRT6 modulator with antitumor activity for the study of hepatocellular carcinoma and non-small cell lung cancer.

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

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

SRT 1720 is a selective activator of human SIRT1 (EC1.5: 0.16 μM) and exhibits more than 230-fold lower potency for SIRT2 and SIRT3.

MC3482 is a specific inhibitor of sirtuin5 (SIRT5).

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

SIRT7 inhibitor 97491 is an HDAC inhibitor with high specificity for SIRT7 (IC50 = 325 nM). SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.

AGK2（IC50=3.5 μM） is an effective, and specific SIRT2 inhibitor.

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

Niacinamide is an important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and or cure of blacktongue and PELLAGRA. Most animals cannot manufacture this compound in amounts sufficient to prevent nutr

N-Caffeoyltryptophan (trans-Caffeoyl-L-tryptophan), a potential Sirt inhibitor, is screened using coffee extract. N-Caffeoyltryptophan inhibited Sirt2 (IC50; 8.7 μM) better than Sirt1(IC50; 34μM).

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

Ophiopogonin D' can activate SIRT1 in a dose-dependent manner. Ophiopogonin D' also noncompetitively inhibits UGT1A6 and UGT1A10.

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.

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

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.

Tenovin-6 is a p53 transcriptional activity agonist.

Inauhzin (INZ)(INZ) is a novel small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human Y cells without causing apparently genotoxic stress(IC50=3 uM, in A549 cell).

Tenovin-3 acts as a p53 activator.

SRT 2183 is a selective activator of Sirtuin-1 (SIRT1, EC1.5 : 0.36 μM).

UBCS039 is the first synthetic Sirt6 activator(EC50 : 38 μM)

Scopolin (Scopoloside) formation is increased by the enhanced activity of PAL. Scopolin can reduce the clinical symptoms of rat AIA by inhibiting inflammation and angiogenesis, and this compound may be a potent agent for angiogenesis related diseases and can serve as a structural base for screening more potent synthetic analogs.

SIRT-IN-2 is a potent SIRT1 2 3 inhibitor [IC50s of 4, 1, and 7 μM, respectively].

Cambinol (SIRT1/2 Inhibitor IV) is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1/2 (IC50: 56/59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Cambinol inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 μM) and no inhibitory for the class I and II HDACs. In BCL6-expressing Burkitt lymphoma cell lines, Cambinol-induced apoptosis has been attributed to the hyperacetylation of p53 and BCL6.Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Sirt2-IN-1 is an inhibitor of sirtuin 2 (IC50 = 163 nM).

SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.

1. Ganoderic acid D is one of the major components in Ganoderma triterpenes. 2. Ganoderic acid D treatment for 48h inhibits the proliferation of HeLa human cervical carcinoma cells with an IC(5) value of 17.3 + - .3 microM.

Tenovin-6 Hydrochloride is an SIRT1, SIRT2 and HDAC8 inhibitor(IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively), and is also a potent p53 activator .

ADTL-SA1215 is a selective SIRT3 activator with SIRT3 deacetylase activity that inhibits the proliferation and migration of human breast cancer MDA-MB-231 cells through the SIRT3-driven autophagy mitochondrial autophagy signaling pathway, and can be used in the study of triple negative breast cancer.

SRT 1720 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).

Ginkgolide C (BN-52022), a natural product, can enhance the cardiac function of rats in the body.

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.

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

SRT 1460 is a 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.

RK-9123016 is a SIRT2 inhibitor. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression.

SIRT6-IN-5（SIRT6 inhibitor 5） is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

Salermide, an inhibitor of Sirt1 and Sirt2, induces cancer-specific apoptotic cell death.

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

Et-29 is a selective inhibitor of SIRT5 inhibitor with a Ki of 40 nM.

Splitomicin (1-Naphthalenepropanoic Acid) (IC50 of 60 μM), a specific inhibitor of NAD(+)-dependent histone deacetylase Sir2p, displays a high activity in a cell-based assay.

Z26395438 is an inhibitor of Sirtuin-1 with IC50 of 1.6 μM.

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.