Sirtuin Inhibitor

SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC₅₀s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells.

Nocardamine (Desferrioxamine E; Nocardamin) is a cyclic trihydroxamate siderophore with iron ion chelation, antioxidant, antibacterial and other activities. Nocardamine is synthesized by Pseudomonas stutzeri under iron-deficient conditions, and excessive iron ions significantly inhibit its biosynthesis process. Nocardamine increases the level of phosphorylated ERK protein, promotes nuclear translocation of β-catenin, and restores the downregulated expression of SIRT1 protein. Nocardamine alleviates cellular oxidative stress, reduces ROS content, and simultaneously repairs the ability to form mineralized nodules and the expression of osteogenic markers. Nocardamine induces FoxA gene transcription and protein expression to assist Pseudomonas aeruginosa in iron ion uptake; it also selectively inhibits the proliferation of mycobacteria. Nocardamine induces spindle-shaped morphological changes in BM-N4 insect cells, and sufficient iron ions inhibit this cellular morphological change. Nocardamine is suitable for research related to bacterial infections.

SIRT1-IN-4 (Compound 8c) is a SIRT1 inhibitor, with an IC₅₀ of 10.04 μM. SIRT1-IN-4 can be used for the research of cancer.

AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC₅₀ of 12.5 μM.

(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC₅₀ of 98 nM.

4'-Bromo-resveratrol (4′‐BR) is a dual SIRT1/SIRT3 inhibitor with an IC₅₀ of 0.2 mM for both targets. 4'-Bromo-resveratrol induces caspase-dependent apoptosis, induces G0/G1 cell cycle arrest, and inhiibits proliferation. 4'-Bromo-resveratrol reduces lactate production, glucose uptake, and NAD⁺/NADH ratio, and downregulates lactate dehydrogenase A and glucose transporter 1 (GLUT1). 4'-Bromo-resveratrol can be used for the research of melanoma.

SIRT3-IN-1 (compound 17f) is a SIRT3 inhibitor, with IC₅₀ of 0.043 μM. SIRT3-IN-1 can be used in the research of acute leukemia (AML).

SIRT6 Human Pre-designed siRNA Set A contains three designed siRNAs for SIRT6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Sirt2-IN-2 (Compound 10) is a selective Sirt2 inhibitor with an IC₅₀ of 0.118 μM.

Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat.

Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC₅₀ of 163 nM.

SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC₅₀s of 15, 10, 33 nM, respectively.

SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC₅₀=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.

Nicotinamide-¹³C₆ is the ¹³C-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.

SIRT3 Human Pre-designed siRNA Set A contains three designed siRNAs for SIRT3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

SIRT2-IN-8 is a potent SIRT2 inhibitor. SIRT2-IN-8 can be used for Huntington’s and Parkinson’s diseases research.

RK-9123016 is a potent inhibitor of SIRT2. RK-9123016 inhibits the enzymatic activity of SIRT2 with an IC₅₀ value of 0.18 µM but not other human sirtuin members including SIRT1 and SIRT3 at 100 µM. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression.

SIRT5 Human Pre-designed siRNA Set A contains three designed siRNAs for SIRT5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

SirReal-1 is a potent and selective Sirt2 inhibitor (IC50 = 3.7 μM).

Neutrophil elastase inhibitor 5 is an inhibitor of human neutrophil elastase (HNE), proteinase 3 (PR3) and sirt2, with IC₅₀ values of 4.91, 20.69 and 2.42 μM, respectively. Neutrophil elastase inhibitor 5 inhibits superoxide anion production and elastase release in human neutrophils. Neutrophil elastase inhibitor 5 can be used for the research of neutrophil inflammatory diseases.