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.

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.

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.

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.

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

Sirt1 2-IN-4 (compound PS3) is a potent triple inhibitor of SIRT1, SIRT2, and SIRT3, exhibiting IC50 values of 1.2 μM (SIRT1), 1.9 μM (SIRT2), and 18.6 μM (SIRT3), respectively. It effectively inhibits p53 deacetylation, indicating potential anticancer properties [1].

SIRT1 2 3-IN-1 (compound 10) is a potent, selective, and cell-permeable inhibitor targeting SIRT1, SIRT2, and SIRT3, with inhibitory concentrations (IC50s) of 0.54 μM, 0.253 μM, and 0.72 μM, respectively. It is utilized in cancer research [1].

Sirt1 2-IN-2 (compound hsa55) is a dual inhibitor, targeting SIRT1 with an IC50 of 1.8 μM and SIRT2 with an IC50 of 2.4 μM. It effectively inhibits p53 deacetylation while enhancing the acetylation of p53 and α-tubulin, promoting apoptosis and exhibiting anti-proliferative effects on human leukemia cell lines [1].

SIRT1-IN-5 (215) is a modulator of the NAD-dependent protein deacetylase SIRT1.

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

SIRT1-IN-3 (compound 3j) is a potent and selective inhibitor of silent information regulator 1 (SIRT1) with an IC50 of 4.2 μM [1].

Sirt1 2-IN-1 (Compound 7) is an inhibitor of SIRT1 and SIRT2, with IC50 values of 1.81 μg mL for SIRT1, 2.10 μg mL for SIRT2, and 20.5 μg mL for SIRT3, and exhibits α-microtubulin hyperacetylation activity, demonstrating significant anticancer effects.

SIRT1-IN-2 (compound 3h) is a potent and selective inhibitor of SIRT1 (silent information regulator 1) with an IC50 of 1.6 μM [1].

Sirt1 2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1 2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively. This compound effectively inhibits p53 deacetylation while simultaneously elevating p53 and α-tubulin acetylation levels. Additionally, Sirt1 2-IN-3 promotes apoptosis and exhibits antiproliferative effects on human leukemia cell lines [1].

SIRT1-IN-4 (Compound 8c) is an inhibitor of SIRT1, with an IC50 value of 10.04 μM. It is applicable for cancer research.

SIRT1-A2 is a SIRT1 activator.

SIRT1 Activator 1 (Compound 3), a marine-derived xyloallenoide A derivative from the Xylaria sp. mangrove fungus, exhibits angiogenic effects in zebrafish and protects human endothelial progenitor cells (hEPCs) from AngII-induced senescence. It achieves this by elevating SIRT1 expression and modulating the AMPK Akt signaling pathway [1].

SIRT1/2 Inhibitor IV (cannabinol) is a small-molecule inhibitor of SIRT1 and SIRT2 with IC50 values of 56 μM and 59 μM, respectively.

SIRT1-I5 is a SIRT1 inhibitor. It shows a potent effect on the prostate cancer cell line.