Epigenetics
Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.
- DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
- HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
- Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
- RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
- Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.
Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.
3 key components involved in the regulation of epigenetic modifications
Epigenetics Writer
Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).
Epigenetics Reader
Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.
Epigenetics Eraser
Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.
Catalog No.
Product Name
Application
Product Information
Citations
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Sirtuin Modulator
Sirtuin modulator 6 is a selective modulator of sirtuin proteins, known for its role in enhancing cellular longevity. This compound exhibits potential therapeutic effects in the context of metabolic disorders such as diabetes and obesity, as well as neurodegenerative and cardiovascular diseases. Its mechanism of action supports research into the modulation of sirtuin pathways, providing insights into various age-related health conditions. -
Sirtuin Modulator
Sirtuin modulator 8 is an effective activator of sirtuin proteins, demonstrating the capacity to enhance sirtuin activity. This compound significantly reduces the expression of monocyte chemoattractant protein-1 (MCP-1) while increasing fibroblast growth factor 21 (FGF21) levels. By regulating genes associated with inflammation and metabolism, Sirtuin modulator 8 is a valuable tool for researching metabolic disorders such as diabetes and obesity, as well as inflammatory diseases. -
Sirt2 inhibitor
SirReal-1 is a selective inhibitor of SIRT2, with an IC50 of 3.7 μM. This compound is utilized in research to investigate the biological role of SIRT2 in various cellular processes and its potential implications in cancer and neurodegenerative diseases. SirReal-1 serves as a valuable tool for elucidating the mechanisms of SIRT2-related signaling pathways. -
Sirtuin Inhibitor
Sirtuin-1 Inhibitor 1 is a selective inhibitor of Sirtuin-1, a key regulator in metabolic processes and cellular aging. This compound demonstrates potential in the study of obesity-related diabetes and age-associated diseases by modulating the activity of Sirtuin-1. Its application in research can enhance understanding of metabolic disorders and the molecular underpinnings of aging. -
SIRT1 Activator
YK-3-237 is a selective activator of SIRT1, targeting mutant p53 proteins. This compound has demonstrated the ability to inhibit the proliferation of triple-negative breast cancer cells, making it a valuable tool for research into cancer biology and potential therapeutic strategies. It may provide insights into the role of SIRT1 in tumor progression and cellular metabolism. -
SirT1 Enhancer
DDL-218 is a potent enhancer of the SirT1 protein, specifically targeting its activity. It has demonstrated efficacy in augmenting SirT1 function in ApoE4-expressing neurons and in murine models of Alzheimer's disease. DDL-218 serves as a valuable tool for investigating SirT1-related pathways and their implications in neurodegenerative disorders, particularly Alzheimer's disease. -
SIRT2 Inhibitor
SIRT2-IN-11 is a selective inhibitor of the SIRT2 enzyme, exhibiting an IC50 value of 18.5 μM. This compound induces apoptosis in a p53-dependent manner, leading to the upregulation of CDKN1A, PUMA, and NOXA, along with increased p53 acetylation. SIRT2-IN-11 is a valuable tool for investigating p53-related cancer mechanisms and therapeutic strategies. -
SIRT2 Inhibitor
AC-93253 is a potent and selective inhibitor of SIRT2, achieving an IC50 value of 6 μM. This compound is instrumental in investigating the role of SIRT2 in tumor biology and may aid in the development of therapeutic strategies targeting SIRT2-related pathways in cancer research. Its specificity enhances the potential for targeted studies in cellular and molecular biology. -
SIRT2 Inhibitor
MIND4-19 is a selective inhibitor of SIRT2, demonstrating an IC50 value of 7.0 μM. This compound is primarily utilized in research related to Huntington's disease, offering insights into the therapeutic potential of SIRT2 modulation in neurodegenerative disorders. Its potency and target specificity make MIND4-19 a valuable tool for studying the role of SIRT2 in disease mechanisms and potential treatments. -
SIRT1 Activator
SIRT1 Activator 2 is a potent SIRT1 activator with an ED50 of less than 5 μM. This compound enhances the activity of SIRT1, a key regulator of cellular lifespan and metabolism. It is utilized in research applications focused on aging, metabolic disorders, and the modulation of cellular stress responses. -
Sirtuin Activator
SIRT1 Activator 3 is a potent activator of Sirtuin 1 (SIRT1), which plays a critical role in cellular metabolism and aging. This compound demonstrates the ability to suppress tumor necrosis factor-alpha (TNF-α) in a dose-dependent manner, highlighting its potential in inflammation modulation. SIRT1 Activator 3 is applicable in research focused on anti-obesity and anti-diabetic therapies, offering insights into metabolic regulation and therapeutic interventions for related disorders. -
SIRT6 Fluorogenic Substrate
CrBKA is a fluorogenic small-molecule substrate specifically designed for SIRT6, a member of the sirtuin family of NAD+-dependent deacetylases. This compound exhibits weak activity, making it suitable for probing SIRT6 enzymatic function in various biological contexts. Its application in research includes the study of cellular metabolism, aging, and the modulation of gene expression through deacetylation processes. -
SIRT1/3 Activator
Nicotinamide riboside is an orally active NAD+ precursor that functions as an activator of SIRT1 and SIRT3. This compound elevates NAD+ levels, enhances oxidative metabolism, and provides protective effects against metabolic abnormalities induced by high-fat diets. Additionally, nicotinamide riboside has been shown to mitigate cognitive decline in transgenic mouse models of Alzheimer’s disease, making it a valuable reagent for research in metabolism and neurodegenerative disorders. -
SIRT1 Modulator
Cannabisin F is a modulator of SIRT1, derived from hempseed lignanamide. It exhibits significant anti-inflammatory and antioxidant properties, making it a valuable candidate for research focused on neurodegenerative diseases. Cannabisin F may influence critical pathways involving SIRT1, NF-κB, and Nrf2, contributing to its potential therapeutic applications. -
Sirtuin Inhibitor
Z26395438 is a potent inhibitor of Sirtuin-1, exhibiting an IC50 value of 1.6 μM. This compound is instrumental in research involving metabolic regulation, aging, and cellular stress responses. Its ability to modulate Sirtuin activity highlights its potential applications in studying various physiological and pathological processes. -
Sirtuin Modulator
Sirtuin modulator 3 is a N-phenyl benzamide derivative that functions as a sirtuin modulator. This compound has been shown to influence sirtuin activity, which is implicated in various biological processes, including aging and cellular regulation. Its biological activity makes it a valuable tool for research in the fields of metabolism, epigenetics, and age-related diseases. -
Sirtuin ligand
WAY-354574 is a potent ligand for sirtuin deacetylases, primarily utilized in research related to Huntington's disease (HD). This compound modulates sirtuin activity, impacting cellular processes associated with neurodegeneration. Researchers can apply WAY-354574 to investigate the therapeutic potential and molecular mechanisms underlying HD and related disorders. -
SIRT1 Inhibitor
CHIC35 is a selective inhibitor of SIRT1, exhibiting an IC50 of 0.124 μM. It demonstrates preferential inhibition of SIRT1 over SIRT2 (IC50=2.8 μM) and SIRT3 (IC50>100 μM). This compound is recognized for its anti-inflammatory properties and is applicable in research related to CHARGE syndrome. -
SIRT6 Activator
CL5D is a selective activator of the protein deacetylase SIRT6, enhancing its deacetylation activity and catalytic efficiency. By promoting conformational changes, specifically involving the Arg-65 residue, CL5D serves as a valuable tool for investigating the regulatory mechanisms of SIRT6. This compound is applicable in research areas related to metabolism, DNA repair, and aging, facilitating a deeper understanding of SIRT6’s biological functions. -
SIRT1 Activator
F0911-7667 is a potent activator of SIRT1, promoting autophagic cell death in U87MG and T98G glioblastoma cells through the activation of the AMPK-mTOR-ULK complex. Additionally, this compound has demonstrated its ability to reduce p53 acetylation in IMR32 neuroblastoma cells, providing protective effects against cell death induced by amyloid-beta (Aβ) fragments. Its unique mechanism and biological activities make it valuable for research in cancer and neurodegenerative disease models. -
SIRT Inhibitor
SIRT1/2/3-IN-2 is a potent inhibitor of SIRT1, SIRT2, and SIRT3, exhibiting inhibition rates of 27%, 72%, and 71% respectively at a concentration of 200 μM. This compound is instrumental in studying the roles of sirtuins in various biological processes, particularly their involvement in cancer biology. SIRT3, known as a potential tumor suppressor or promoter, has been linked to lymph node-positive breast cancer and oral squamous cell carcinoma, making SIRT1/2/3-IN-2 valuable for cancer research applications. -
SIRT2 Inhibtor
Sirt2-IN-5 is a selective inhibitor of SIRT2, a member of the sirtuin family involved in various cellular processes, including metabolism and stress response. This compound effectively reduces SIRT2 activity, thus influencing downstream signaling pathways associated with neuroprotection and cancer biology. It is useful in research applications focusing on the roles of SIRT2 in disease models and exploring therapeutic strategies targeting sirtuins. -
SIRT2 Inhibitor
SIRT2-IN-10 is a selective inhibitor of SIRT2, exhibiting an inhibitory concentration (IC50) of 1.3 μM. This compound is instrumental in studying its role in cancer pathology and neurodegenerative disorders, enabling research into potential therapeutic applications. Its ability to modulate SIRT2 activity makes it a valuable tool for investigating cellular mechanisms and disease progression. -
SIRT7 Inhibitor
Epigenetic factor-IN-1 is a selective SIRT7 inhibitor that plays a crucial role in modulating epigenetic regulation. It demonstrates a strong binding affinity for the SIRT7 protein, making it an important tool for exploring the mechanisms of epigenetic modifications. This compound is particularly relevant for liver cancer research, providing insights into the role of SIRT7 in cancer biology and therapeutic development. -
sirtuin SirT2 Inhibitor
Tenovin-D3 hydrochloride is a selective inhibitor of the sirtuin SirT2, which plays a crucial role in cellular regulation. This compound has been shown to enhance the expression of p21 (CDKN1A) independently of the p53 pathway. It is suitable for research applications focused on aging, cancer biology, and the modulation of cellular stress responses to explore the therapeutic potential of sirtuin inhibition. -
SIRT2 Inhibitor
Sirt2-IN-6 is a potent and selective inhibitor of SIRT2, exhibiting an IC50 of 0.815 μM. It demonstrates significant biological activity in modulating SIRT2-related pathways and is valuable for cancer research applications. This compound facilitates the exploration of SIRT2's role in oncogenesis and therapeutic development. -
SIRT1/2 Inhibitor
hsa62 is a dual inhibitor targeting SIRT1 and SIRT2, demonstrating IC50 values of 1.3 μM and 5.5 μM, respectively. This compound effectively modulates the activity of sirtuins, enzymes involved in various cellular processes, including metabolism and aging. hsa62 is suitable for research investigating the role of sirtuins in cellular regulation, disease models, and therapeutic applications. -
SIRT1 Activator
DCHC is a specific activator of SIRT1, enhancing its enzymatic activity without increasing SIRT1 expression levels. This compound is particularly useful in studies investigating mitochondrial damage and dysfunction, offering insights into metabolic regulation and cellular stress responses. DCHC's ability to activate SIRT1 makes it a valuable tool for exploring the roles of sirtuins in cellular health and disease. -
SIRT5 Inhibitor
SIRT5 Inhibitor 6 is a selective and potent inhibitor of SIRT5 that functions through a substrate-competitive mechanism, demonstrating an IC50 value of 3.0 μM. This compound shows promise in therapeutic applications for septic acute kidney injury (AKI) in vivo, making it a valuable tool for research in kidney health and related pathologies. -
SIRT1/SIRT2 Inhibitor
Guttiferone G is a selective inhibitor of the human SIRT1 and SIRT2 deacetylases, exhibiting IC50 values of 9 μM and 22 μM, respectively. This compound demonstrates weak cytotoxicity in the A2780 human ovarian cancer cell line, with an IC50 of 8.0 μg/mL. Guttiferone G is derived from Garcinia macrophylla and may serve as a valuable tool in research studies exploring SIRT1 and SIRT2 modulation in cellular processes. -
SIRT5 Inhibitor
SIRT5 inhibitor 5 is a potent inhibitor of the SIRT5 enzyme, exhibiting an IC50 value of 0.21 µM. This compound functions as a substrate-competitive inhibitor, specifically not occupying the NAD+-binding pocket, thereby modulating SIRT5 activity. SIRT5 inhibitor 5 is valuable in research focused on elucidating the role of SIRT5 in metabolic pathways and providing insights into its potential implications in various diseases. -
SIRT5 Inhibitor
SIRT5 Inhibitor 4 is a selective inhibitor of the SIRT5 enzyme, demonstrating an IC50 value of 26.4 μM. This compound exhibits minimal activity against other SIRT subtypes, with an IC50 greater than 400 μM, underscoring its specificity. It serves as a valuable tool for investigating the biological roles of SIRT5 in metabolic regulation and related pathways. Research applications include studying SIRT5's involvement in cellular processes and potential therapeutic targets in metabolic disorders. -
SIRT6 Activator
SIRT6 activator 2 is a specific activator of sirtuin 6, known for its anti-lipid accumulation properties. This compound effectively downregulates key transcription factors LXR and SREBP-1c, along with their downstream target genes involved in lipogenesis. SIRT6 activator 2 is valuable for research focused on lipid metabolism and associated diseases, enabling the exploration of therapeutic strategies targeting metabolic disorders. -
SIRT2 Inhibitor
AGK7 is a selective inhibitor of sirtuin 2 (SIRT2), demonstrating significant neuroprotective effects in the context of Parkinson's disease. This compound has been shown to alleviate alpha-synuclein toxicity and improve inclusion morphology in cellular models. In addition, AGK7 effectively protects against dopaminergic cell death in both in vitro studies and Drosophila models, making it a valuable tool for researching neurodegenerative disorders. -
SIRT3 Inhibitor
SIRT-IN-5 is a selective inhibitor of SIRT3, demonstrating an IC50 value of 2.88 μM. This compound has been shown to promote the differentiation of multiple myeloma cells, facilitating increased expression of differentiation antigens such as CD49e, as well as enhancement of human immunoglobulin light chains λ and κ. SIRT-IN-5 is a valuable tool in research focused on the modulation of cellular differentiation processes in hematological malignancies. -
SIRT1/2 Inhibitor
Sirtuin-IN-1 is a selective inhibitor of SIRT1 and SIRT2, with IC50 values of 6.2 μM and 4.2 μM, respectively. This compound has been shown to induce G1 phase cell cycle arrest, demonstrating its potential as an anti-cancer agent. Sirtuin-IN-1 is particularly effective against glioma, making it a valuable tool for research into cancer therapeutics and the exploration of sirtuin-related biological pathways. -
SIRT1 Inhibitor
Sirtuin Modulator 4 is a selective SIRT1 inhibitor, demonstrating an EC50 value of 51-100 μM. This compound plays a critical role in modulating cellular pathways associated with lifespan extension and offers potential in researching a variety of conditions, including diabetes, obesity, neurodegenerative diseases, cardiovascular disorders, inflammation, and cancer. Its ability to inhibit SIRT1 makes it a valuable tool for studying the therapeutic implications of sirtuin regulation in metabolic and age-related diseases. -
SIRT1 Modulator
SIRT1-IN-5 is a selective modulator of the NAD-dependent protein deacetylase SIRT1. It demonstrates significant activity in regulating deacetylation processes, contributing to cellular metabolism and stress response. This compound can be utilized in research focused on aging, metabolic diseases, and neurodegenerative disorders, making it a valuable tool for exploring the therapeutic potential of SIRT1 modulation. -
SIRT2 Inhibitor
SIRT2-IN-14 is a selective inhibitor of SIRT2, demonstrating an IC50 value of 0.196 μM. This compound effectively modulates SIRT2 activity, making it a valuable tool for studying the role of SIRT2 in various biological pathways. Research applications may include investigations into neurodegenerative diseases, cancer biology, and cellular metabolism, providing insights into the therapeutic potential of targeting SIRT2. -
SIRT5 Inhibitor
SIRT5 inhibitor 2 is a selective inhibitor of the SIRT5 enzyme, exhibiting an IC50 value of 2.3 μM. It effectively inhibits SIRT5-dependent desuccinylation processes, making it a valuable tool for investigating the roles of SIRT5 in various biological contexts. This compound is suitable for research applications focusing on cancer biology and neurodegenerative diseases, aiding in the exploration of therapeutic strategies targeting SIRT5 activity. -
Sirtuin Modulator
Sirtuin Modulator 5 is a potent activator of SIRT1, demonstrating a DC50 value of less than 50 μM. This compound enhances cellular lifespan and facilitates research into various age-related and stress-related diseases, including diabetes, obesity, neurodegenerative disorders, cardiovascular diseases, blood clotting disorders, inflammation, and cancer. Additionally, Sirtuin Modulator 5 may promote increased mitochondrial activity, making it a valuable tool in the study of metabolic and age-related diseases. -
SIRT1 Inhibitor
ZINC08792355 is a selective SIRT1 inhibitor that plays a crucial role in the regulation of cellular processes associated with aging, metabolic disorders, and oncogenesis. This compound facilitates the exploration of SIRT1-related pathways in research on age-related diseases, diabetes, and cancer, making it a valuable tool for investigators studying these important biological phenomena. -
SIRT1 Activator
SRT3657 is a selective activator of SIRT1, exhibiting properties that enhance neuronal resilience. Its brain-permeable nature allows for effective modulation of SIRT1 activity, contributing to neuroprotection. This compound is valuable for research applications aimed at understanding neurodegenerative diseases and exploring potential therapeutic strategies. -
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.
