Sirtuin Inhibitor

Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC₅₀ of 123 nM for SirT1. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease.

MC3482 is a specific sirtuin5 (SIRT5) inhibitor.

Croconic acid disodium (Nacr) is a lysine crotonylation (Kcr) activator and electroactive material. Croconic acid disodium reduces the expression of HDAC2, HDAC3, SIRT1, and SIRT3, and increases the expression of EP300, CITED1, ACSS2, DPF2, CDYL, MLLT3, and YEATS2. Croconic acid disodium elevates intracellular crotonyl-CoA content and global histone lysine crotonylation levels. Croconic acid disodium promotes the growth of bovine fibroblasts, regulates cell cycle progression, and inhibits bovine fibroblast apoptosis (apoptosis). Croconic acid disodium improves the blastocyst development efficiency of bovine somatic cell nuclear transfer embryos. Croconic acid disodium undergoes reversible lithium intercalation/deintercalation reactions via sodium-lithium ion exchange. Croconic acid disodium is applicable to research related to cell growth promotion.

Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.

Nicotinamide-¹³C,¹⁵N (Niacinamide-¹³C,¹⁵N) is the ¹³C- and ¹⁵N-labeled Nicotinamide (HY-B0150). Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC₅₀: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD₊, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity.

Nicotinamide-d₄ is the deuterium 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.

SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC₅₀ of 0.11 μM.

PDRN (Polydeoxyribonucleotide) is a deoxynucleotide polymer mainly derived from the sperm of rainbow trout or salmon. PDRN inhibits pro-inflammatory factors and promotes VEGF expression via the cAMP-PKA pathway by activating the adenosine A_2A receptor (A_2AR), thereby driving angiogenesis and collagen deposition in fibroblasts. Degradation products of PDRN provide DNA raw materials for proliferating cells through the salvage synthesis pathway, accelerating re-epithelialization. PDRN reduces melanin synthesis and cell apoptosis by upregulating ERK/AKT phosphorylation and inhibiting the activities of MITF and tyrosinase, and resists skin aging by attenuating nuclear autophagy and blocking the interaction between LC3-SIRT1. PDRN is mainly used for wound repair, post-aesthetic surgery recovery and anti-aging research.

SIRT1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIRT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

SIRT-IN-3 is a potent SIRT inhibitor, with an IC₅₀ of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC₅₀ of 74 μM and 235 μM for SIRT2 and SIRT3, respectively).

JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2.

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.

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.

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.

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.

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.

SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury.