|S1541||Selisistat (EX 527)||<1 mg/mL||49 mg/mL||18 mg/mL|
|S2804||Sirtinol||<1 mg/mL||23 mg/mL||<1 mg/mL|
|S1899||Nicotinamide (Vitamin B3)||24 mg/mL||24 mg/mL||24 mg/mL|
|S7845||SirReal2||<1 mg/mL||84 mg/mL||<1 mg/mL|
|S5914||AK 7||<1 mg/mL||87 mg/mL||3 mg/mL|
|S8627||OSS_128167||<1 mg/mL||73 mg/mL||<1 mg/mL|
|S4900||Tenovin-6||98 mg/mL||98 mg/mL||<1 mg/mL|
|S8245||Thiomyristoyl||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8460||Salermide||<1 mg/mL||78 mg/mL||7 mg/mL|
|S8628||3-TYP||5 mg/mL||29 mg/mL||29 mg/mL|
|S1129||SRT1720 HCl||<1 mg/mL||38 mg/mL||<1 mg/mL|
|S5918||CAY10602||<1 mg/mL||56 mg/mL||<1 mg/mL|
|S4735||Salvianolic acid B||100 mg/mL||100 mg/mL||100 mg/mL|
|S8270||SRT2183||<1 mg/mL||93 mg/mL||3 mg/mL|
|S7792||SRT2104 (GSK2245840)||<1 mg/mL||16 mg/mL||<1 mg/mL|
|S2391||Quercetin||<1 mg/mL||61 mg/mL||10 mg/mL|
|S2298||Fisetin||<1 mg/mL||57 mg/mL||3 mg/mL|
|S8481||SRT3025||<1 mg/mL||100 mg/mL||5 mg/mL|
Selisistat (EX 527) is a potent and selective SIRT1 inhibitor with IC50 of 38 nM in a cell-free assay, exhibits >200-fold selectivity against SIRT2 and SIRT3. Phase 2.
The eect of Melatonin, luzindole, and EX527 treatment on apoptotic index, infarct size, lactate dehydrogenase (LDH) release, and CK release in IR-injured hearts. Representative photomicrographs of in situ detection of apoptotic myocytes by TUNEL staining. Green ﬂuorescence shows TUNEL-positive nuclei; blue ﬂuorescence shows nuclei of total cardiomyocytes; original magniﬁcation 9x400. Sacle bar: 100 um.
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
SIRT1 inhibitor exacerbates TBI-induced mitochondrial damage, promotes neuronal apoptosis and activates p38 MAPK signaling. Rats were injected intraperitoneally with the SIRT1 inhibitor sirtinol (10 mg/kg) 30 min before LFP-induced TBI. After 12 h, rats were sacrificed. (A) The expression of SIRT1 and β-actin were detected by Western blot. β-Actin was used as loading control. (B) Quantification of Western blots for SIRT1. (C) The expression of SIRT1 was analyzed by immunohistochemical staining post-TBI.
Nicotinamide (Vitamin B3), a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Immunoprecipitation-western blot for analyzing acetylated Snail in Snail-transfected 293T cells (upper) and FaDu-Snail cells (lower) treated with a vehicle control (Ctrl), a HDAC inhibitor TSA 5 nM for 8 hr, a SIRT1 inhibitor NAM(Nicotinamide) 10 mM for 8 hr, or in combination.
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM.
OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
Tenovin-6 is a small molecule activator of p53 transcriptional activity.
Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.
Salermide is a reverse amide with a strong in vitro inhibitory effect on Sirt1 and Sirt2. Compared with Sirt1, Salermide is even more efficient at inhibiting Sirt2.
3-TYP is a selective SIRT3 inhibitor which is selective for Sirt3 over Sirt1 and Sirt2. The IC50 values for SITR1, SIRT2, SIRT3 are 88 nM, 92 nM, 16 nM respectively.
SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3.
CAY10602 is a potent SIRT1 activator.
Salvianolic acid B (Sal B), an antioxidant and free radical scavenging compound, is the most abundant bioactive compound extracted from the root of Salvia miltiorrhiza Bunge.
SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.
SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.
Liver pathology and serum markers of liver injury in mice fed control (Ctrl), or ethanol (EtOH), or ethanol combined with fisetin (E/Fisetin) diet for 4 weeks. (A) Light microscopy with hematoxylin and eosin staining shows lipid accumulation (arrows) in the liver of mice after alcohol exposure, which was alleviated by fisetin administration. (B) Plasma alanine aminotransferase (ALT) and (C) aspartate aminotransferase (AST) activities. Infinity ALT and AST reagents were used formeasuring ALT and AST activities. Scale bar: 50 lm. Results are mean±SD (n = 3 to 6). Results for bars that do not share a letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.