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SIRT2 Inhibitor
SR94 is a selective SIRT2 inhibitor that features a unique six-membered ring structure with variable R2 substituents. This compound demonstrates potential in the investigation of cancer, ischemia-reperfusion injury, and neurodegenerative diseases. Its targeted inhibition of SIRT2 makes it a valuable tool for understanding the role of this enzyme in various biological processes and disease states. -
SIRT6 Modulator
IMU-856 is a small molecule modulator of SIRT6, exhibiting oral bioavailability and systemic action. It selectively inhibits the deacetylase activity of SIRT6 while simultaneously increasing its protein levels. This compound has demonstrated the ability to restore intestinal barrier function, making it a valuable tool for research on celiac disease and related gastrointestinal disorders. -
SIRT1 Activator
SRTCX1002 is a selective activator of the SIRT1 enzyme, functioning primarily through the promotion of p65 deacetylation, which subsequently inhibits NF-κB activity. This compound effectively suppresses inflammatory responses, demonstrated by its ability to inhibit stimuli-induced NF-κB transcriptional activation and reduce LPS-induced TNFα secretion, with IC50 values of 0.71 µM and 7.58 µM, respectively. SRTCX1002 serves as a valuable reagent for research focused on inflammation and related signaling pathways. -
SIRT5 Inhibitor
SIRT5 Inhibitor 7 is a selective substrate-competitive inhibitor targeting SIRT5, known for its anti-inflammatory properties. This compound effectively regulates protein succinylation and reduces the release of pro-inflammatory cytokines, offering potential renal protective effects. SIRT5 Inhibitor 7 demonstrates notable in vivo efficacy in mouse models of acute kidney injury induced by lipopolysaccharide (LPS) and cecal ligation/perforation (CLP), making it a valuable tool for researching sepsis-related kidney damage. -
Sirtuin Modulator
FLS-359 is an orally active allosteric modulator of sirtuin 2, demonstrating an IC50 of 3 μM. This compound exhibits significant antiviral activity, effectively inhibiting both RNA and DNA viral replication. FLS-359 is valuable for research applications focused on viral pathogenesis and therapeutic strategies targeting sirtuin signaling pathways. -
SIRT1 Activator
SRTCX1003 is an orally active SIRT1 activator that enhances SIRT1 activity, leading to the modulation of various biological processes. This compound has been shown to suppress inflammatory responses, making it a valuable tool for research related to inflammation and metabolic disorders. Its application in studies focused on SIRT1-mediated pathways provides insights into potential therapeutic approaches for a range of diseases. -
Sirtuin Modulator
Sirtuin Modulator 2 (Compound 132) is a selective modulator of sirtuin enzymes, exhibiting an effective dose (ED50) of 50 μM or lower. This compound plays a critical role in the regulation of cellular processes such as aging, metabolism, and stress response. Its ability to influence sirtuin activity makes it valuable for research in fields like cancer biology, neurodegenerative diseases, and metabolic disorders. -
Sirtuin Substrate
Ac-QPKK(Ac)-AMC is a fluorogenic substrate specifically designed for sirtuin enzymes, facilitating the study of sirtuin-mediated deacetylation processes. This reagent enables the quantitative analysis of sirtuin activity, making it a valuable tool for investigating the role of sirtuins in various biological processes and disease states, including aging and metabolic disorders. Researchers can leverage Ac-QPKK(Ac)-AMC to explore sirtuin function in high-throughput screening assays and in-depth mechanistic studies. -
SIRT1 Inhibitor
ZINC08792229 is a potent inhibitor of SIRT1, a nicotinamide adenine dinucleotide (NAD+)-dependent deacetylase playing a crucial role in cellular regulation. This compound exhibits significant biological activity that may contribute to research on SIRT1-related diseases, including aging, diabetes, and cancer. It serves as a valuable tool for exploring the therapeutic potential of targeting SIRT1 in various pathological conditions. -
SIRT1/SIRT2 Inhibitor
Aristoforin, a hypericin derivative, selectively inhibits SIRT1 and SIRT2, resulting in G1 phase cell cycle arrest. This compound also scavenges hydroxyl free radicals and demonstrates protective effects against Fe2+-induced DNA breakage. Aristoforin is valuable for research in the context of breast cancer and colon adenocarcinoma studies. -
SIRT6 Modulator
SIRT6 modulator-1 is a selective modulator of SIRT6, a key enzyme involved in regulating metabolic processes and DNA repair. This compound influences SIRT6 activity, enhancing its role in chromatin dynamics and cellular stress responses. SIRT6 modulator-1 has potential applications in research focused on aging, metabolic disorders, and cancer by elucidating the pathways regulated by SIRT6. -
SIRT3 Inhibitor
SIRT3-IN-2 is a selective inhibitor of the SIRT3 enzyme, demonstrating a reduction of SIRT3 activity by 39% at a concentration of 200 µM. This compound is valuable for investigations into metabolic homeostasis and its implications in tumor suppression. SIRT3-IN-2 can be utilized in research aimed at understanding the regulatory roles of sirtuins in cellular metabolism and cancer biology. -
SIRT2 Inhibitor
SIRT2-IN-15 is a selective inhibitor of the SIRT2 deacetylase and deamyloacylase enzymes, demonstrating IC50 values of 7 μM and 37 μM, respectively. This compound modulates cellular acetylation states, making it a valuable tool for investigating the roles of SIRT2 in various biological processes, including neurodegenerative diseases, cancer metabolism, and aging. SIRT2-IN-15 can be utilized in research applications focusing on the molecular mechanisms of SIRT2-related pathways and potential therapeutic targets. -
SIRT1 Activator
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol is a potent SIRT1 activator that enhances SIRT1 activity significantly. This compound has demonstrated anti-tumor activity, making it a valuable tool for research in cancer biology and therapeutic interventions targeting SIRT1 modulation. Its role in promoting cellular metabolism and longevity pathways further supports its use in studies related to aging and metabolic disorders. -
SIRT2 Inhibitor
A2B57 is a selective inhibitor of SIRT2, exhibiting an IC50 value of 6.3 µM. This compound effectively modulates the activity of SIRT2, making it a valuable tool for exploring the role of this enzyme in various biological processes. Its application extends to studies in neurodegeneration, metabolism, and cellular stress responses, providing insights into SIRT2-related pathways. -
SIRT1/2/3 Inhibitor
SIRT-IN-6 is a pan-inhibitor targeting SIRT1, SIRT2, and SIRT3, with IC50 values exceeding 50 μM. This compound is valuable for studying its effects in metabolic, inflammatory, oncologic, and neurodegenerative disorders. Its broad inhibition profile makes it a suitable tool for elucidating the roles of sirtuins in various biological processes and disease states. -
SIRT2 Inhibitor
A1B11 is a selective inhibitor of Sirtuin 2 (SIRT2) with an IC50 value of 5.3 μM. This compound is primarily utilized in research focused on neurodegenerative diseases, where SIRT2 modulation plays a critical role in the underlying mechanisms of pathology. A1B11 provides a valuable tool for investigating the therapeutic potential of SIRT2 inhibition in various neurodegenerative conditions. -
SIRT1/3 Activator
Nicotinamide riboside (triflate) is a potent activator of the SIRT1 and SIRT3 pathways, functioning as an orally active precursor to NAD+. This compound significantly elevates NAD+ levels, thereby enhancing oxidative metabolism and providing protective effects against metabolic disturbances triggered by high-fat diets. Additionally, it has demonstrated neuroprotective properties, as evidenced by its ability to mitigate cognitive decline in transgenic mouse models of Alzheimer’s disease, making it valuable for research in metabolic health and neurodegenerative disorders. -
Endogenous Ceramide
Ceramides Mixture consists of endogenous ceramides, including hydroxy and non-hydroxy fatty acid-containing variants. It plays a crucial role in maintaining the permeability barrier of the epidermis. This mixture is involved in key biological activities such as growth inhibition, cell cycle arrest, and modulation of telomerase activity, making it valuable for research applications focused on skin physiology, aging, and cellular signaling pathways. -
Telomerase Inhibitor
MST-312 is a telomerase inhibitor developed as a chemically modified derivative of epigallocatechin gallate (EGCG) found in green tea. It demonstrates significant biological activity by selectively inhibiting telomerase, an enzyme commonly associated with cancer cell immortality. MST-312 is primarily utilized in cancer research, particularly in the study of multiple myeloma and other malignancies, offering insights into potential therapeutic strategies targeting telomerase activity. -
Telomerase Inhibitor
Telomerase-IN-3 is a potent telomerase inhibitor that directly targets the activity of the hTERT promoter. By inhibiting hTERT, this compound plays a critical role in reducing telomerase activity, thereby impacting cellular lifespan and growth. Telomerase-IN-3 is useful for research applications focused on cancer biology, cellular aging, and the development of therapies aimed at telomerase-related diseases. -
TRF2 Inhibitor
FKB04 is a potent inhibitor of telomeric repeat binding factor 2 (TRF2), impairing telomere maintenance mechanisms in liver cancer cells. This activity results in T-loop defects, telomere shortening, and subsequent cellular senescence. FKB04 has demonstrated efficacy in inhibiting tumor growth in human liver cancer xenograft models, notably in BALB/c mice implanted with Huh-7 cells. Its application is primarily in liver cancer research, making it a valuable tool for exploring therapeutic strategies targeting telomere dynamics. -
Telomerase Inhibitor
Telomerase-IN-1 is a potent telomerase inhibitor, exhibiting an IC50 of 0.19 µM. This compound effectively targets telomerase activity, making it a valuable tool for investigating telomerase-related mechanisms in cellular biology. Its application is particularly relevant in cancer research, where telomerase activity is often upregulated, contributing to unlimited cellular proliferation. -
Telomerase Inhibitor
Telomerase-IN-2 is a telomerase inhibitor that functions by reducing the expression of dyskerin, effectively decreasing telomerase activity with an IC50 of 0.89 µM. This compound has demonstrated promising anti-cancer activity, making it a valuable tool for research into telomerase-related cancer therapeutics and cellular aging studies. Its ability to target telomerase presents potential applications in cancer biology and therapies aimed at inhibiting tumor proliferation. -
Prokaryotic Telomerase
TelN Protelomerase is a prokaryotic telomerase derived from bacteriophage N15 that exhibits cleaving-joining activity essential for the synthesis of linear prophage DNA with terminally closed ends in lysogenic bacteria. This enzyme functions by cleaving both strands of DNA and subsequently joining the ends to produce covalently closed hairpin structures. TelN Protelomerase is valuable for research applications involving bacteriophage biology, telomere dynamics, and the study of lysogenic conversion mechanisms. -
Telomerase Inhibitor
Telomerase-IN-8 is an orally active inhibitor of telomerase, exhibiting an IC50 of 0.98 μM. This compound demonstrates significant antiproliferative activity against various tumor cell lines, including PC3, Bcap-37, MGC-803, and HepG2. Additionally, Telomerase-IN-8 displays substantial antitumor efficacy in S180 sarcoma and HepG2 hepatoma xenograft models. It serves as a valuable tool for investigating telomerase-targeted approaches in cancer research. -
Telomerase Inhibitor
Telomerase-IN-7 is a potent telomerase inhibitor with an IC50 of 0.03 μM. By selectively targeting the telomerase enzyme, it effectively impedes cellular proliferation associated with various cancers. This compound is applicable in cancer research, particularly in studies focusing on telomere biology and cellular aging mechanisms. -
Telomerase Inhibitor
7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP) is a nucleotide analogue that serves as an effective telomerase inhibitor, with an IC50 of 11 μM. This compound is utilized in various research applications to study telomere biology and elucidate the mechanisms of telomerase activity. Its unique structure allows for the exploration of telomerase's role in cellular aging and cancer development. -
Telomerase Inhibitor
FJ-5002 is a potent telomerase inhibitor with an IC50 of 2 μM. It effectively induces telomere shortening and leads to increased chromosomal abnormalities, as well as senescence-like features in the human leukemia cell line U937. This compound exhibits significant antitumor activity, making it an important tool in cancer research and the study of telomerase-related mechanisms in tumorigenesis. -
PROTAC Target Protein Ligand
TERT ligand-1 is a PROTAC target protein ligand that facilitates the synthesis of the PROTAC NU-PRO-1. This compound has shown efficacy in inducing degradation of telomerase reverse transcriptase (TERT) in cancer cells. TERT ligand-1 is instrumental in research applications focused on targeted protein degradation and cancer therapeutics development. -
Telomerase Inhibitor
3′-Azido-2′,3′-dideoxy-GTP (AZddGTP) is a selective inhibitor of telomerase, exhibiting a Ki value of 1.5 μM. This compound can be incorporated into the 3′-terminus of DNA by telomerase, leading to the inhibition of telomerase activity. Research applications include studying telomerase function and its role in cellular aging and cancer biology, particularly in HeLa cells in vitro. -
TERT Activator
TERT Activator-2 is a selective activator of telomerase reverse transcriptase (TERT), known to enhance the expression of TERT in cellular models. This compound is instrumental in studies focused on telomere maintenance and cellular lifespan, facilitating research into aging and age-related diseases. Its ability to modulate telomerase activity positions TERT Activator-2 as a valuable tool in the exploration of cellular senescence and regenerative medicine. -
Telomerase Inhibitor
Macrocalin B is a diterpenoid that acts as a potent telomerase inhibitor. This compound effectively inhibits the proliferation of various cancer cell lines, including K562, HL-60, A549, MKN, CA, and HCT, with IC50 values ranging from 2.81 to 171 μM. Notably, Macrocalin B demonstrates nanomolar level inhibition of telomerase in K562 cells. This makes it a valuable tool for research into cancer biology and potential therapeutic applications targeting telomerase activity. -
L2H2-6OTD Intermediate
L2H2-6OTD intermediate-2 is an intermediate in the synthesis of telomerase inhibitors, specifically designed for applications in antibody-drug conjugate (ADC) development. This compound plays a crucial role in enhancing the efficacy of targeted cancer therapies by inhibiting telomerase activity, thereby contributing to the selective cytotoxicity against tumor cells. Researchers can leverage this intermediate for further investigation into novel therapeutic strategies in cancer treatment. -
PBK Inhibitor
PBK-IN-9 is a potent inhibitor of PDZ binding kinase (PBK), a key regulator involved in various cellular processes. This compound demonstrates significant biological activity by inhibiting PBK's kinase activity, making it an essential tool for studying cellular signaling pathways and cancer biology. PBK-IN-9 is widely used in research applications focused on understanding the role of PBK in tumor progression and therapeutic resistance. -
TopI Inhibitor
(1R,9R)-Exatecan mesylate is a potent inhibitor of topoisomerase I, with an IC50 of 0.975 μg/mL in mice and 0.82 μg/mL in humans. This non-prodrug camptothecin derivative stabilizes the enzyme-DNA cleavable complex, effectively blocking topoisomerase I activity and inducing apoptosis. (1R,9R)-Exatecan mesylate demonstrates significant anti-proliferative effects on a variety of malignant tumor cells and addresses P-glycoprotein-mediated multidrug resistance. It is utilized in preclinical research across multiple cancer types, including pancreatic, lung, breast cancers, and leukemia. -
Top I Inhibitor
(1S,9R)-Exatecan mesylate is a potent topoisomerase I inhibitor that acts by stabilizing the enzyme-DNA cleavable complex, thereby blocking enzyme activity and inducing apoptosis. With an IC50 value of 0.975 μg/mL in mice and 0.82 μg/mL in humans, this non-prodrug camptothecin derivative effectively inhibits the proliferation of various malignant tumor cells and tumor growth while overcoming P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is utilized in preclinical studies on multiple cancers, including pancreatic, lung, breast cancers, and leukemia. -
Topoisomerase II Inhibitor
Merbarone is an orally active inhibitor of topoisomerase II, functioning primarily by obstructing the enzyme's capacity to mediate DNA cleavage without stabilizing the covalent complexes formed between topoisomerase II and DNA. As an anticancer agent, Merbarone demonstrates effective cytotoxicity in various cancer cell lines, making it a valuable tool for cancer research and therapeutic studies focused on topoisomerase-targeted therapies. -
TOP2A Transcriptional Inhibitor
PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). This compound effectively eliminates undifferentiated human pluripotent stem cells (hPSCs), making it a valuable tool for stem cell research and differentiation studies. Its ability to precisely target TOP2A provides researchers with a means to manipulate pluripotency and investigate cellular differentiation processes. -
Topoisomerase Inhibitor
Ellipticine hydrochloride is a potent topoisomerase II inhibitor, functioning as an effective antineoplastic agent. It disrupts DNA replication and transcription processes, leading to cytotoxic effects in rapidly dividing cells. This compound is utilized in cancer research to investigate mechanisms of tumorigenesis and therapeutic response. -
Anti-Cancer Agent
Coralyne chloride is a protoberberine alkaloid that functions as a potent anti-cancer agent by inhibiting topoisomerase I. It acts as a topoisomerase I poison, inducing DNA cleavage mediated by this enzyme. Coralyne chloride is also utilized in the preparation of coralyne derivatives, which serve as DNA-binding fluorescent probes, making it valuable for various research applications in cancer biology and molecular imaging. -
TOP2B Inhibitor
Topobexin is a selective inhibitor of Topoisomerase II beta (TOP2B), demonstrating an IC50 value of 0.19 μM for TOP2B and 4.8 μM for TOP2A in DNA decatenation assays. By binding to non-homologous residues within the obex pocket, Topobexin effectively targets the ATPase domain of TOP2B. This compound mitigates anthracycline-induced DNA double-strand breaks and associated apoptotic signaling without impairing the anticancer effects of anthracyclines in cancer cells. It serves as a valuable tool for research into anthracycline-induced cardiotoxicity, revealing insights into cellular stress responses and cardiac function. -
Camptothecin Derivative
7-Ethylcamptothecin is a derivative of Camptothecin and functions primarily as a DNA topoisomerase I inhibitor. This compound demonstrates considerable antitumor activity against various tumor cell lines, making it an important tool in cancer research. Additionally, 7-Ethylcamptothecin serves as a crucial precursor for the synthesis of 20 (S)-O-substituted benzoyl-7-ethylcamptothecin compounds, facilitating further exploration of potential therapeutic agents in oncology. -
Topoisomerase I/II Inhibitor
DACA is a potent inhibitor of topoisomerase I and II, capable of penetrating the blood-brain barrier. It demonstrates significant activity against various cancer types, including colorectal cancer, leukemia, and lung cancer. This compound serves as a valuable tool for investigating the mechanisms of these diseases and developing targeted therapies. -
Topoisomerase Inhibitor
LMP744 is a potent Topoisomerase I (Top1) inhibitor that functions as a DNA intercalator, disrupting the DNA replication process. This compound demonstrates significant antitumor activity, making it a valuable tool in cancer research. LMP744 can be utilized to study the mechanisms of Top1 inhibition and its effects on cell proliferation and apoptosis in various cancer models. -
TOP2 Inhibitor
T638 is a potent inhibitor of topoisomerase II (TOP2), demonstrating an IC50 of 0.7 µM against TOP2A activity. This compound exhibits significant anti-proliferative effects on cancer cells, making it a valuable tool for cancer research. Its ability to selectively disrupt topoisomerase activity positions T638 as an important reagent for investigating mechanisms of tumor growth and exploring potential therapeutic strategies. -
Topoisomerase IIα Inhibitor
ARN-21934 is a selective inhibitor of human topoisomerase IIα, effectively crossing the blood-brain barrier. It demonstrates potent inhibition of DNA relaxation, with an IC50 value of 2 μM, significantly outperforming Etoposide (IC50 = 120 μM). Due to its favorable in vivo pharmacokinetic properties, ARN-21934 is a promising candidate for further anticancer research and therapeutic development. -
Topoisomerase I Inhibitor
LMP744 hydrochloride is a potent Topoisomerase I inhibitor that functions as a DNA intercalator, disrupting the normal processes of DNA replication and transcription. This compound exhibits significant antitumor activity, making it a valuable tool in cancer research. Its ability to inhibit Topoisomerase I highlights its potential applications in studies targeting DNA damage response and therapeutic resistance in various malignancies. -
Antidiabetic/Antioxidant/Anitcancer Agent
Quercetin-3'-O-glucoside is a flavonoid glycoside that exhibits antidiabetic, antioxidant, and anticancer activities. It reduces liver glucose-6-phosphatase activity, modulates insulin and glucose levels, and enhances antioxidant enzyme functions in liver and kidney tissues. In cancer research, Quercetin-3'-O-glucoside inhibits DNA topoisomerase II, induces S-phase cell cycle arrest, and promotes caspase-3-mediated apoptosis in hepatocellular carcinoma cells. Additionally, it selectively disrupts EGFR-mediated signaling pathways and inhibits the migration and invasion of pancreatic cancer cells. This compound is valuable for studies focused on pancreatic cancer, diabetes, hepatocellular carcinoma, and other malignancies. -
Antitumor Agent
Bisantrene dihydrochloride is an effective antitumor agent that acts primarily through DNA intercalation. It specifically targets eukaryotic type II topoisomerases, disrupting DNA replication and transcription. Furthermore, Bisantrene dihydrochloride is a substrate of the multidrug resistance protein, MDR1, making it a relevant compound for studies on drug resistance mechanisms in cancer research.

