sirt2

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

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC that acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].

SIRT2-IN-9 is a selective SRIT2 inhibitor with an IC50 value of 1.3 μM.SIRT2-IN-9 inhibits the proliferation of MCF-7 breast cancer cells.SIRT2-IN-9 can be used for cancer research.

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).

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.

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.

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

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.

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

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

Tenovin-6 is a p53 transcriptional activity agonist.

Tenovin-3 acts as a p53 activator.

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.

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

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)

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).

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

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

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

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 .

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

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).