sirt6

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.

MDL-800 is a SIRT6 modulator with antitumor activity for the study of hepatocellular carcinoma and non-small cell lung cancer.

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.

SIRT6-IN-4 (Compound 10d) is a selective inhibitor of SIRT6 with an IC50 of 5.68 μM. It inhibits the proliferation of MCF-7 cells, with an IC50 of 8.30 μM, and causes cell cycle arrest at the G2 M phase. Additionally, SIRT6-IN-4 impedes cell migration and invasion of MCF-7 and induces apoptosis. In mouse models, this compound exhibits antitumor activity.

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

SIRT6 activator 12q is a potent, selective, and orally active compound that activates SIRT6. It demonstrates IC50 values of 171.20 μM for SIRT1, >200 μM for SIRT2, SIRT3, and SIRT5, and 0.58 μM for SIRT6, indicating its high specificity towards SIRT6. This compound effectively inhibits cell growth and migration, induces apoptosis, and causes cell cycle arrest at the G2 phase, showcasing its anticancer activity.

SIRT6-IN-3 (compound 8a), a selective SIRT6 inhibitor (IC50 = 7.49 μM), impedes the proliferation of pancreatic ductal adenocarcinoma (PDAC) cells and prompts apoptosis. It enhances the responsiveness of cancer cells to gemcitabine by obstructing the DNA damage repair pathway, thus serving as a valuable tool in pancreatic cancer research [1].

SZU-B6, a PROTAC degrader, targets and degrades SIRT6 with DC50 values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells. It inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cell lines. Additionally, SZU-B6 induces apoptosis in SK-HEP-1 cells and causes cell cycle arrest at the G2 M phase. It demonstrates anti-tumor activity in murine models.

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

MDL-801 is an activator of SIRT6 deacetylation.

CrBKA, a fluorogenic small-molecule substrate of SIRT6, exhibits weak activity [1].

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