sirt in 2

SIRT-IN-2 is a potent SIRT1/2/3 inhibitor [IC50s of 4, 1, and 7 μM, respectively].

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

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.

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].

SIRT3 activator2 (compound 2a) acts as an activator of SIRT3. It is presumed to bind directly with SIRT3 in SH-SY5Y cells, as inferred through thermal stability, facilitating the SIRT3-dependent clearance of α-Syn. Furthermore, SIRT3 activator2 enhances motor functions in Parkinsonian mice and dose-dependently prevents the loss of dopaminergic (DA) neurons in the substantia nigra.

SIRT6 activator2 (compound 31) is a sirtuin6 activator known for its anti-lipid accumulation properties. It significantly downregulates LXR, SREBP-1c, and their target genes, making it valuable for research into lipid metabolism-related diseases.

SIRT2-IN-16 (compound 17) is a SIRT2 inhibitor targeted at prostate-specific membrane antigen (PSMA).

SIRT2-IN-17 (compound Z18) is a potent inhibitor of SIRT2, effectively reducing the expression of α-SMA and p-Smad2/3.

SIRT2-IN-12 (Compound 3) is a SIRT2 inhibitor with an IC50 value of 50 μM.

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-A2 is a SIRT1 activator.

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-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.

SIRT2-IN-9 is a selective SRIT2 inhibitor with an IC50 value of 1.3 μM.SIRT2-IN-9 inhibits the proliferation of MCF-7 breast cancer cells.SIRT2-IN-9 can be used for cancer research.

SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor (IC50: 1.3 μM) useful for cancer and neurodegenerative disease research.

Sirt2-IN-6 is a potent and selective inhibitor of SIRT2 (IC50: 0.815 μM) and can be used to study cancer.

Sirt2-IN-5, a potent inhibitor of SIRT2, is specifically (2S)-2-[(Z)-4-(3-chlorophenyl)-3-methylbutanoylamino]-5-methylhexanoic acid [exact (1:1) of (2S,4R)-4-[(Z)-4-(3-chlorophenyl)-3-methylbutanoylamino]-5-methylhexanoic acid].

SIRT2-IN-11 (AEM1) is a selective inhibitor of SIRT2 with an inhibitory concentration (IC50) of 18.5 μM. It induces apoptosis in a p53-dependent manner, activates the expression of CDKN1A, PUMA, and NOXA, and enhances the acetylation of p53. This compound is utilized in the study of p53-associated cancers.

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].

Sirt2-IN-7 (compound 22), a selective SIRT2 inhibitor with an IC50 of 178.2 nM and a Ki of 154.3 nM, is employed 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].

Sirt1/2-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].

Sirt1/2-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].

HSP70/SIRT2-IN-2 (Compounds 1a), a dual inhibitor of SIRT2 and HSP70, exhibits an IC50 of 45.1±5.0 μM against SIRT2 and demonstrates antitumor activity [1].