DK1-04e serves as a prodrug for the potent SIRT5 inhibitor DK1-04 (IC50 = 340 nM), demonstrating significant anti-tumor activity in breast cancer models. The compound effectively suppresses mammary tumor progression in both MMTV-PyMT transgenic mice and human xenograft models, with cellular studies confirming SIRT5 inhibition disrupts cancer cell proliferation and transformation.

AGK2 is a potent and selective SIRT2 inhibitor, exhibiting an IC50 of 3.5 μM against this target. While it primarily acts on SIRT2, it also weakly inhibits SIRT1 (IC50 = 30 μM) and SIRT3 (IC50 = 91 μM), demonstrating lower potency toward these isoforms.

SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.

E1231 (E-1231) is a small molecule SIRT1 activator with EC50 of 0.83 uM, interactes with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα).

JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines.

MIND4-19 is a potent SIRT2 inhibitor with an IC50 value of 7.0 μM. MIND4-19 can be used for researching Huntington's disease.

Sirtuin modulator 2 (Compound 132) is a sirtuin modulator with an ED50 equal or less than 50 μM.

SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.

UBCS385 (Sirt4 inhibitor 60) is a potent, selective inhibitor of mitochondrial deacylase Sirtuin 4 (Sirt4) with IC50 of 0.9 uM.

UBCS373 (Sirt4 inhibitor 69) is a highly isoform selective inhibitor of mitochondrial deacylase Sirtuin 4 (Sirt4) with IC50 of 16 uM.

SirReal1.1 is a potent, selective inhibitor of Sirtuin 2 (Sirt2) with IC50 of 0.16 uM.

SCIC2.1 is a potent small molecule SIRT1 activator (175%, AC50=36.8 uM), directly binds SIRT1 and protects SIRT1 from thermal degradation.

MDL-811 (MDL811) is a potent, selective and allosteric SIRT6 activator with EC50 of 5.7 uM (activated SIRT6 deacetylation), two-fold greater activity than MDL-800 (EC50=12.3 uM, Cat# 35760).

MC3482 is a potent, specific SIRT5 inhibitor, increases the ammonia content in cells leading to autophagy and mitophagy, shows selective SIRT5 inhibition vs SIRT1-3..

MC3138 is a potent and selective small-molecule SIRT5 activator, inhibits proliferation in SIRT5-low PDAC cell lines and organoids.

MC 2494 is a nove potent, pan-Sirtuin (SirT) inhibitor, increases RIP1 acetylation in the death domain and induces bona fide tumour-restricted acetylated RIP1/caspase-8-mediated apoptosis.

FLS-359 (FLS-359) is a selective, allosteric inhibitor of sirtuin 2 (SIRT2) deacetylase activity with IC50 of 3 uM, shows no activity against SIRT1 and SIRT3, exhibits broad-spectrum antiviral activity.

40569Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.

2800Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.

SRT1720 is a selective SIRT1 activator with EC50 of 0.16 μM, but is >230-fold less potent for SIRT2 and SIRT3.

SRT1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 μM) versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5 = 37 μM；SIRT3: EC1.5 > 300 μM).

SIRT2 Inhibitor II, AK-1 inhibits SIRT2 selectively over SIRT1 and SIRT3.

OSS-128167 is a novel SIRT6 inhibitor.

AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM).

3-TYP is a selective SIRT3 inhibitor.

Salermide is an inhibitor of SIRT1 and SIRT2, causing tumor-specific apoptotic cell death. In MOLT4 leukemia cells, salermide causes 90% apoptosis within 72 hours (IC50 ~ 20 μM) by reactivating proapototic genes that are repressed by SIRT1.

Tenovin-1 is a p53 activator and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2.

Tenovin-6 is the water soluble analog of Tenovin-1 and acts as a potent SIRT1 (IC50=21 uM) and SIRT2 (IC50= 10 uM) inhibitor as well as p53 activator.

Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.