3-TYP is a selective SIRT3 inhibitor.

A novel potent, selective Sirt2 inhibitor with IC50 of 0.118 uM.

A novel potent, selective Sirt2 inhibitor with IC50 of 3.745 uM.

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.

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

Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 and 59 μM, respectively.

CAY10602 is a SIRT1 activator.

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).

OSS-128167 is a novel SIRT6 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.

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

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

SIRT5 inhibitor is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.

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).

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

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

SRTCX1002 (SRTCX-1002) is a small molecule activator of SIRT1 (STAC) with EC1.5 of 0.4 uM, enhances deacetylation of cellular p65 protein with IC50 of 0.84 uM in cellular p65 acetylation assay.

SRTCX1003 (SRTCX-1003) is a small molecule activator of SIRT1 (STAC) with EC1.5 of 0.61 uM, enhances deacetylation of cellular p65 protein with IC50 of 1.42 uM in cellular p65 acetylation assay.

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.

EX 527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits >200-fold selectivity against SIRT2 and SIRT3.

Inauhzin(INZ) is a novel small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress(IC50=3 uM, in A549 cell).

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.

Nicotinamide riboside tartrate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.

Nicotinamide riboside malate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.

SIRT-IN-3 is a potent SIRT inhibitor, with an IC50 of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC50 of 74 μM and 235 μM for SIRT2 and SIRT3, respectively).

SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..

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.

CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 µM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC50=2.8 µM) or SIRT3 (IC50>100 µM). CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research.

SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect.

7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake (IC50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC50s of 1.18 μM and 0.97 μM, respectively.

3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity.

NRD167 is a potent and selective SIRT5 inhibitor.

Ainsliadimer C, a potential activator of SIRT1, ameliorates inflammatory responses in adipose tissue.

ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.

SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches.

AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease.

Sirt2-IN-5 is a potent SIRT2 inhibtor.

DK1-04 is a potent, selective, cell-permeable small-molecule SIRT5 inhibitor with IC50 of 0.34 uM, shows no inhibition on SIRT1-3/6 at 83 uM.

DK1-04e (DK1-04 prodrug) is the prodrug of DK1-04, a potent, selective, and cell-permeable small-molecule SIRT5 inhibitor with IC50 of 0.34 uM; DK1-04e inhibits the cellular growth of breast cancer cells by targeting SIRT5. DK1-04e impairs mammary tumor growth in MMTV-PyMT transgenic mice and human breast cancer mouse model. SIRT5 inhibition suppressed the transformed properties of cultured breast cancer cells and significantly reduced mammary tumor growth in vivo, in both genetically engineered and xenotransplant mouse models.

NH4-13 is a potent, SIRT2-selective inhibitor with IC50 of 87 nM, no inhibition against SIRT1/3/5/6 (CI50>50 uM).NH4-13 (30 mg/kg) significantly impaired tumor growth in HCT-116 tumor xenograft.

NH4-6 is a potent, selective pan SIRT1-3 inhibitor with IC50 of 3.0/0.032/2.3 uM for SIRT1/2/3, respectively.NH4-6 does not inhibits SIRT5 and SIRT6.NH4-6 (30 mg/kg) significantly impaired tumor growth in HCT-116 tumor xenograft.

SIRT2 inhibitor 55 is a potent and selective SIRT2 inhibitor with IC50 of 250 nM.SIRT2 inhibitor 55 displays >300 to >800-fold selectivity over SIRT1 and 3, respectively.SIRT2 inhibitor 55 dose-dependently increases tubulin acetylation in treated non-small cell lung cancer cell line NCI-H460.SIRT2 inhibitor 55 shows cytotoxicity in in B-cell lymphoma and other cancer cell lines (Raji cell IC50=11.9 uM).

SIRT2 inhibitor 56 is a potent selective SIRT2 inhibitor with IC50 of 780 nM.SIRT2 inhibitor 56 displays >300 to >800-fold selectivity over SIRT1 and 3, respectively.SIRT2 inhibitor 56 dose-dependently increases tubulin acetylation in treated non-small cell lung cancer cell line NCI-H460.SIRT2 inhibitor 56 shows cytotoxicity in in B-cell lymphoma and other cancer cell lines (Raji cell IC50=9.1 uM).SIRT2 inhibitor 56 induces apoptosis and shows anti-proliferation effect in OCI-Ly8-LAM53 (OCI) cells.

SIRT3 inhibitor 8 is a SIRT3 selective inhibitor with IC50 of 6 uM, 6.8- and 5.3-fold selectivity for SIRT3 versus SIRT1 and SIRT2.SIRT3 inhibitor 8 reduced DLBCL cell viability and triggered activation of autophagy.

SIRT5 inhibitor 32 is an efficient, cellularly active small molecule that targets SIRT5.SIRT5 inhibitor 32 inhibits cell growth of SIRT5-dependent AML cell lines SKM-1, OCIAML2 and MOLM-13 with IC50 of 9, 20, and 24 uM, respectively.SIRT5 inhibitor 32 is also shown to inhibit SIRT5 in HeLa cells by using an assay that produce in-cell fluoresence in response to SIRT5 activity in the mitochondria.SIRT5 inhibitor 32 displays cytoselective toxicity towards SIRT5-dependent AML cells (SKM-1) over HEK293T cells in culture.

SIRT6 activator CL5D is a novel small-molecule activator of SIRT6 deacetylation, stimulates 4-fold activation of SIRT6 (1 uM) against H3K9ac (20 uM) at 3 uM.CL5D demonstrate competitive inhibition with Ki of 13.4 uM.CL5D exhibited time-dependent deacetylation at H3K9 by SIRT6 in HEK293T cells.

YC8-02 is a small molecule mitochondrial-targeting SIRT3 inhibitor with IC50 of 0.53 uM.YC8-02 inhibits SIRT1 and SIRT2 with IC50 of 2.8 and 0.062 uM in in vitro biochemical assays.YC8-02 manifested increased ratio of mitochondria to total cell concentration, as measured by mass spectrometry in purified mitochondria extracts and total cell lysates.YC8-02 increased mitochondrial protein acetylation, inhibited GDH activity and induced autophagy in DLBCL cells.YC8-02 could phenocopy the effects of SIRT3 depletion.YC8-02 (30 mg/kg) caused regression of the tumors in DLBCL xenografts, with no evidence of discomfort or weight loss.

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.

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.

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.

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.

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.

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.

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

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..

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).

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

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

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

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

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.