JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines.
DK1-04e serves as a prodrug for the potent SIRT5 inhibitor DK1-04 (IC50 = 340 nM), demonstrating significant anti-tumor activity in breast cancer models. The compound effectively suppresses mammary tumor progression in both MMTV-PyMT transgenic mice and human xenograft models, with cellular studies confirming SIRT5 inhibition disrupts cancer cell proliferation and transformation.
SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
E1231 (E-1231) is a small molecule SIRT1 activator with EC50 of 0.83 uM, interactes with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα).
2-APQC is a potent activator of SIRT3 with a Kd value of 2.756 μM. It alleviates myocardial hypertrophy and fibrosis by regulating mitochondrial homeostasis, exhibiting promising cardioprotective potential in vitro and in vivo. It may serve as a potential candidate for future heart failure (HF) therapeutics.
DDL-218 is an orally active and potent SirT1 inhibitor. DDL-218 enhances SirT1 in ApoE4-expressing neurons and a murine AD model. DDL-218 can be used in the study of Alzheimer's disease.