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.

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].

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.

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).

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

MDL-811, an allosteric activator of SIRT6, markedly enhances the deacetylation of histone H3 at lysine residues 9, 18, and 56 (H3K9Ac, H3K18Ac, and H3K56Ac), presenting potential utility in colorectal cancer research [1].

CrBKA is a fluorogenic small-molecule substrate of SIRT6 with weak activity [1] .

MDL-801 is an activator of SIRT6 deacetylation.

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