sirt

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

SIRT5 inhibitor 1 is a potent and selective inhibitor of human Sirtuin 5 deacylase (IC50: 0.11 μM) and is associated with aging-related diseases.

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].

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].

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

SIRT6-IN-1, a novel SIRT6 inhibitor, reduces glycemia and improves oral glucose tolerance in unfed wild-type mice.

SIRT7 inhibitor 97491 is an HDAC inhibitor with high specificity for SIRT7 (IC50 = 325 nM). SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.

Nicotinamide, a vitamin B3 derivative, is an inhibitor of SIRT1 (IC50=50-180 μM) and SIRT2 (IC50=2 μM). Nicotinamide can be used as a precursor of nicotinamide adenine dinucleotide or NAD+, which can be supplemented by dietary intake and can prevent or treat melanoglossia and pellagra.

Fisetin belongs to a group of natural flavonols with a variety of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-aging and neuroprotective effects.

UBCS039 is the first synthetic Sirt6 activator(EC50 : 38 μM)

SIRT-IN-6 (Compound 14) is a pan-inhibitor of SIRT1/2/3 with an IC50 value of >50 μM. It shows potential as a research agent for studies involving metabolic disorders, inflammation, cancer, and neurodegenerative diseases.

SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. It effectively suppresses the expression of SIRT1, SIRT2, and SIRT3, leading to increased acetylation and activation of p53. Additionally, SIRT-IN-7 inhibits the proliferation of breast cancer cells and induces apoptosis and autophagy, demonstrating antitumor activity.

SIRT-IN-4 is an inhibitor specifically targeting the NAD+-dependent lysine deacetylase Sirtuin2 (Sirt2) with an IC50 of 0.35 μM. It effectively inhibits Sirt2 deacetylation, thereby reducing cell viability and impeding the migration of prostate cancer cells. SIRT-IN-4 is useful for research on Sirt2's roles in cell cycle regulation and gene expression control.

SIRT-IN-3, a potent inhibitor of SIRT1 with an IC50 value of 17 μM, exhibits approximate 4-fold and 14-fold greater selectivity for SIRT1 over SIRT2 and SIRT3, with respective IC50 values of 74 μM for SIRT2 and 235 μM for SIRT3 [1].

SIRT6-IN-5(SIRT6 inhibitor 5) is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

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.

SIRT5 inhibitor 4 (compound 11) is a dose-dependent and selective SIRT5 (Sirtuin5) inhibitor with an IC50 value of 26.4 μM for SIRT5 and no inhibitory effect on SIRT1/2/3 isoforms at 400 μM, with anticancer potential.

SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with IC50=2.3 μM that has inhibitory activity through SIRT5-dependent deacetylation and can be used to study cancer and neurodegenerative diseases.

SIRT5 inhibitor 5 is a selective and substrate-competitive SIRT5 inhibitor with an IC50 of 210 nM, which does not occupy the NAD+ binding pocket and can be used to study cancer and metabolism-related diseases.

SIRT5 inhibitor 6 is a novel and potent Sirtuin 5 inhibitor with an IC50 = 310 nM for the treatment of sepsis-associated acute kidney injury (AKI) that modulates protein succinylation and pro-inflammatory cytokine release in the kidney and attenuates renal dysfunction and pathologic injury.

SIRT5 inhibitor 7 (compound 58), a substrate-competitive and selective SIRT5 inhibitor with IC 50 = 310 nM, significantly attenuated renal dysfunction and pathological damage in lipopolysaccharide (LPS)- and cecum ligation/perforation (CLP)-induced septic AKI mice, and modulated proteinsuccinimidylation and proinflammatory cytokine release and pro-inflammatory cytokine release in the kidneys of acute kidney injury (AKI) mice.

SIRT5 inhibitor 8 (compound 10) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=5.38 μM, with potential anticancer effects.

SIRT5 inhibitor 9 (compound 14) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=4.07 μM and has potential anticancer effects.