Sirtuin

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

Sirtuin Modulator 5, a sirtuin modulating agent, activates SIRT1 with an efficacy marked by a DC50 value of less than 50 μM. It is applicable in enhancing cell longevity and is researched for its therapeutic potential in a wide range of diseases such as those associated with aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular diseases, blood clotting disorders, inflammation, cancer, and flushing. Furthermore, it holds promise for conditions that could benefit from boosted mitochondrial activity [1].

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 4, a sirtuin modulator, exhibits an inhibitory effect on SIRT1, presenting an EC 50 value ranging from 51-100 μM. It is potentially useful in research aimed at prolonging cell lifespan and preventing a broad spectrum of diseases and disorders such as diabetes, obesity, neurodegenerative, cardiovascular diseases, inflammation, and cancer.

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

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

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

WAY-270360 (N-[4-(1H-benzimidazol-2-yl)phenyl]-2,4-dimethoxybenzamide) is a sirtuin modulator and an epidermal growth factor receptor (EGFR) inhibitor.

Benzamide, 3-methoxy-N-(3-thiazolo[5,4-b]pyridin-2-ylphenyl) (3-methoxy-N-(3-(thiazolo[5,4-b]pyridin-2-yl)phenyl)benzamide) is a sirtuin modulator and useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including diabetes, cardiovascular disease, bloo

SIRT5 inhibitor 1 is a potent and selective inhibitor of human Sirtuin 5 deacylase (IC50: 0.11 μM). sIRT5 inhibitor 1 is associated with ageing-related diseases.

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

JFD00244 is an inhibitor of sirtuin 2 (SIRT2). It has an anti-tumor effect.

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

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

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.

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).

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.

SRT 1720 is a selective activator of human SIRT1 (EC1.5: 0.16 μM) and is >230-fold less potent for SIRT2 and SIRT3.

Fisetin is a natural flavonol extracted from Rhus succedanea L that is structurally and functionally related to kaempferol, can modulate sirtuins,with antioxidant, anticancer, neuroprotection effects.

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

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

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

YK-3-237 (B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid) reduces acetylation of mtp53 and exhibits anti-proliferative effects toward triple-negative breast cancer (TNBC) cells carrying mtp53.

MIND4-19 is an inhibitor of SIRT2 with antitumor activity.

SirReal1-O-propargyl, a moiety based on SirReal1, is a selective and highly potent inhibitor of Sirtuin 2 (Sirt2), demonstrating an IC50 of 2.4 μM. It operates by binding to the cereblon ligand through a linker, facilitating the formation of PROTAC for the degradation of Sirt2[1].

WAY-354574 is an active compound that targets the deacetylase Sirtuin, utilized in research focused on Huntington's disease (HD) [1].

B2 (Linazolamide intermediate B impurity 2) promotes inclusion formation in cellular models of Huntington's disease and Parkinson's disease

AK-1 is a sirtuin 2 (SIRT2) inhibitor (IC50:12.5 µM).that prevents hippocampal neurodegeneration in Alzheimer's disease models and induces cell cycle arrest in colon carcinoma cells.

Selisistat S-enantiomer (EX-527 S-enantiomer) is an effective and specific SIRT1 inhibitor (IC50 = 98 nM) and shows >200-fold selectivity against SIRT2 3.

SIRT5 inhibitor 8 (compound 10) serves as a competitive inhibitor of sirtuin SIRT5, exhibiting an IC50 of 5.38 μM, and possesses anticancer potential [1].

SIRT5 inhibitor 9 (compound 14), with an IC50 of 4.07 μM, is a competitive inhibitor of the sirtuin SIRT5, exhibiting potential anticancer properties [1].

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

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 .

CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patient-derived breast cancer cells is correlated with shorter survival.

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)

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

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

CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM). Upregulation of SIRT3 transcription is associated with oral squamous cell carcinoma (OSCC) and breast cancer with lymph node involvement, while SIRT3 down-regulation inhibits the growth of OSCC cells and sensitizes them to radiation and chemotherapy.

Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosylceramide, sphingomyelin, free fatty acids, and cholesterol in primary human keratinocytes. Nicotinamide (40 µM) induces apoptosis in SNU-398, SNU-739, and HepG2 hepatocellular carcinoma (HCC) cells, and it prevents the formation of neoplastic lesions in a diethylnitrosamine-induced mouse model of HCC. Unlike niacin, nicotinamide does not reduce plasma lipid levels or induce flushing.

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+.

7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. It exhibited either alone or as hybrid with other active pharmacophores diverse pharmacological profiles. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake ( IC 50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC 50 s of 1.18 μM and 0.97 μM, respectively [1].

Tenovin-D3 is a sirtuin SirT2 inhibitor. It acts by increasing p21 (CDKN1A) expression in a p53-independent manner.

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

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

Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo.Demethyleneberberine suppresses CYP2E1, hypoxia inducible factor α, and inducible nitric oxide synthase, which contributes to oxidative stress and restored sirtuin 1/AMP-activated protein kinase/peroxisome proliferator-activated receptor-γ coactivator-1α pathway-associated fatty acid oxidation in chronic ethanol-fed mice.

Tenovin-6 is a p53 transcriptional activity agonist.

Nicotinamide Hydrochloride is a form of vitamin B3 or niacin that inhibits sirtuin 2 ( SIRT2 ) activity in vitro , with an EC 50 of 2 μM. Nicotinamide Hydrochloride inhibits up to 90% melanoma cell number and increases cellular NAD + , ATP, ROS levels. Nicotinamide Hydrochloride inhibts tumor growth in vivo and improves survival of melanoma-bearing mice, which can be used for the research of skin cancers such as melanoma .

Nicotinamide ascorbate is a bioactive chemical.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.