sirt in 1

SIRT-IN-1 is a potent inhibitor of SIRT1, SIRT2, and SIRT3, with IC50 values of 15, 10, and 33 μM, respectively

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

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.

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

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 Activator 1 (Compound 5v) is a selective activator of SIRT3. It enhances the expression of SIRT3, leading to upregulation of SOD2 and OPA1. This activity effectively mitigates mitochondrial dysfunction, alleviates oxidative stress, and maintains the vitality of cardiac myocytes. SIRT3 Activator 1 is useful in the study of cardiovascular diseases.

SIRT1-IN-5 (215) is a modulator of the NAD-dependent deacetylase SIRT1 with potential application in cancer research.

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

SIRT4-IN-1 (compound 69) is a selective inhibitor of Sirtuin 4 (Sirt4) with an IC50 value of 16 μM. It does not exhibit significant effects on other sirtuin isoforms.

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

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-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.

SIRT1/2/3-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].

Sirt1/2-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].

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].

HSP70/SIRT2-IN-1 (Compound 2a) serves as a dual inhibitor targeting both SIRT2 and HSP70, exhibiting an IC50 of 17.3±2.0 μM against SIRT2. This compound possesses antitumor activity [1].

SIRT3-IN-1 (compound 17f) is an inhibitor of SIRT3, exhibiting an IC50 value of 0.043 μM. It is utilized in research related to acute myeloid leukemia (AML).

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

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].