Sirtuin Inhibitor

Sirt5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sirt5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

SirReal2 (Standard) is the analytical standard of SirReal2 (HY-100591). This product is intended for research and analytical applications. SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration.

Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC₅₀=297 nM), SirT2 (IC₅₀=1.15 μM), and SirT5 (IC₅₀=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC₅₀=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.

CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC₅₀=0.124 μM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC₅₀=2.8 μM) or SIRT3 (IC₅₀>100 μM). CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research.

Sirt1/2-IN-3 (compound PS9) is a dual inhibitor of SIRT1/2 with IC₅₀s of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respsectivley. Sirt1/2-IN-3 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-3 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines.

SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. SIRT-IN-7 can inhibit the expression of SIRT1, SIRT2, and SIRT3, and increase the acetylation and activation of p53. SIRT-IN-7 can inhibit the proliferation, and induce apoptosis and autophagy of breast cancer cells. SIRT-IN-7 has anti-tumor activity.

SIRT1/2/3-IN-2 (compound 9) is a potent SIRT inhibitor, with inhibition rates of 27%, 72%, and 71% targeting SIRT1, SIRT2, and SIRT3, respectively, at 200 μM. SIRT3 is a potential tumor suppressor or promoter, and its increased transcription may be associated with lymph node-positive breast cancer and oral squamous cell carcinoma.

Antiproliferative agent-17 is an antiproliferative agent. Antiproliferative agent-17 inhibits Gram-positive bacteria and has anticancer activity.

Sirt2-IN-5 is a potent SIRT2 inhibtor.

SPC-180002 is a SIRT1/3 dual inhibitor, with IC₅₀ values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.

NH4-6 is a SIRT2 inhibitor with an IC₅₀ of 0.032 μM against SIRT2 and an IC₅₀ of 3 μM against SIRT1. NH4-6 inhibits the deacetylase activity of SIRT1. As a cytotoxic agent, NH4-6 reduces cancer cell viability, suppresses anchorage-independent growth of cancer cells, induces acetylation of α-tubulin, and promotes acetylation of p53. NH4-6 can be used in the research of breast cancer.

SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor with an IC₅₀ of 1.3 μM. SIRT2-IN-10 can be used for the research of cancer and neurodegenerative disease.

SIRT2-IN-17 (compound Z18) is a potent SIRT2 inhibitor. SIRT2-IN-17 reduces the expression of α-SMA and p-Smad2/3.

OXPHOS-IN-3 is a mitochondria-targeted dual OXPHOS/glycolysis inhibitor. OXPHOS-IN-3 exhibits potent antiproliferative activity against pancreatic cancer cells. OXPHOS-IN-3 induces mitochondrial dysfunction, ferroptosis, and immunogenic cell death (ICD). OXPHOS-IN-3 shows potent antitumor activity in pancreatic ductal adenocarcinoma (PDAC) models.

SIRT1 activator 1(compound 3) is a derivative of marine compound xyloallenoide A isolated from the mangrove fungus Xylaria sp.SIRT1 activator 1 shows angiogenic activities in zebrafish. SIRT1 activator 1 protects hEPC against AngII-induced senescence by increasing SIRT1 expression levels and balancing the AMPK/Akt signaling pathway.

Sirt1/2-IN-5 is a SIRT1/SIRT2 inhibitor with human SIRT1 IC₅₀ 0.3 μM and human SIRT2 IC₅₀ values 1.2 μM and pIC₅₀ 5.82. Sirt1/2-IN-5 inhibits NAD⁺-dependent deacetylase activity of SIRT1 and SIRT2. Sirt1/2-IN-5 can be used for the research of cancer, neurodegenerative disease.

Epigenetic factor-IN-1 (40569Z) is a epigenetic factor inhibitor. Epigenetic factor-IN-1 has strong binding effect on SIRT7. Epigenetic factor-IN-1 can be used for liver cancer research.

SIRT6-IN-5 (Compound 25) is a selective and safe SIRT6 inhibitor (IC₅₀ = 18.91 µM). SIRT6-IN-5 can enhance the anti proliferative effect of chemotherapy agents. SIRT6-IN-5 can be used in the research of cancer, such as breast cancer.

SJ-106C is a SIRT inhibitor, with IC₅₀ values of 0.59, 0.12, and 0.49 μM for SIRT1/2/3 respectively. SJ-106C can target mitochondria and inhibit the growth of DLBCL tumors.

SIRT2-IN-16 (compund 17) is a prostate-specific membrane antigen (PSMA)-targeted SIRT2 inhibitor.