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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HDAC6 Inhibitor
NR160 is a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 30 nM. This compound demonstrates low cytotoxicity in leukemia cell lines and enhances the induction of apoptosis when used in conjunction with proteasome inhibitor Bortezomib, as well as chemotherapeutic agents Epirubicin and Daunorubicin. NR160 serves as a valuable tool for researchers investigating the therapeutic potential of HDAC6 inhibition in cancer treatment. -
PHD2/HDACs Inhibitor
PHD2/HDACs-IN-1 is a dual inhibitor targeting both PHD2 and various HDACs, demonstrating potent inhibitory activity with IC50 values of 1.15 μM for PHD2, 19.75 μM for HDAC1, 26.60 μM for HDAC2, and 15.98 μM for HDAC6. This compound showcases low toxicity and exhibits renoprotective effects, making it suitable for research related to cisplatin-induced acute kidney injury (AKI). Its ability to modulate epigenetic regulation and hypoxic signaling pathways positions it as a valuable tool in exploring the underlying mechanisms of renal stress responses. -
HDAC Inhibitor
YF479 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in the modulation of gene expression. This compound impairs cell viability and suppresses both colony formation and tumor cell motility. Additionally, YF479 effectively inhibits breast tumor growth and metastasis, making it a valuable tool for research in breast cancer clinical trials. -
CYP17A1/HDAC6 Inhibitor
CYP17A1/HDAC6-IN-1 is a dual inhibitor targeting both CYP17A1 and HDAC6, exhibiting IC50 values of 0.284 μM and 0.6015 μM, respectively. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology. Its ability to simultaneously inhibit these targets suggests potential applications in therapeutic strategies against malignancies driven by steroidogenesis and histone deacetylation. -
HDAC8 Inhibitor
HDAC8-IN-2 is a potent inhibitor of histone deacetylase 8 (HDAC8) with IC50 values of 0.27 μM for Schistosoma mansoni HDAC8 and 0.32 μM for human HDAC8. This compound demonstrates significant efficacy in killing schistosome larvae and markedly reduces the egg-laying capacity of adult worm pairs. These properties make HDAC8-IN-2 a valuable tool for research focused on schistosomiasis and histone deacetylation processes. -
HDAC3 Inhibitor
HDAC3-IN-4 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 of 89 nM, demonstrating effective targeting of this enzyme. It promotes the degradation of PD-L1 through the modulation of cathepsin B (CTSB) activity in lysosomes, exhibiting a DC50 of 5.7 μM. HDAC3-IN-4 shows high selectivity for HDAC3 compared to other HDAC isoforms, including HDAC1, HDAC6, HDAC7, and HDAC8, making it a valuable tool for studying epigenetic regulation and potential immunotherapeutic approaches. -
HDAC Inhibitor
FITC-SAHA is a fluorescein-conjugated derivative of SAHA, serving as a potent inhibitor of histone deacetylases (HDACs). This compound effectively modulates histone acetylation, influencing gene expression and cellular processes. FITC-SAHA is primarily utilized in cancer research and studies related to Alzheimer's disease, facilitating the investigation of HDAC's role in these conditions. Its fluorescent labeling aids in the visualization and analysis of cellular and molecular interactions. -
PfHDAC1 Inhibitor
HDAC1-IN-4 is a potent inhibitor of Plasmodium falciparum histone deacetylase 1 (PfHDAC1), demonstrating significant antimalarial activity with an IC50 of less than 5 nM. This compound exhibits a favorable safety profile with reduced cytotoxicity. HDAC1-IN-4 serves as a valuable tool for investigating the role of histone deacetylases in malaria research and may provide insights for novel therapeutic strategies against Plasmodium falciparum infections. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), demonstrating IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, and 29 nM for PI3Kδ. It also exhibits selective inhibition with IC50 values of 1.3 nM for HDAC1, 3.4 nM for HDAC2, 972 nM for HDAC4, 17 nM for HDAC6, and 12 nM for HDAC8. Due to its significant anticancer properties, PI3K/HDAC-IN-2 is valuable for research applications in cancer biology and therapeutic development. -
HDAC
Estrogen Receptor β/HDAC Probe 1 is a near-infrared fluorescent probe designed to simultaneously target the estrogen receptor β and histone deacetylase (HDAC). This probe enables the study of dynamic interactions between these two critical proteins, facilitating the investigation of their roles in cellular signaling and gene regulation. It is particularly useful in cancer research and other studies involving estrogen signaling pathways and epigenetic modifications. -
mTOR/HDAC Inhibitor
mTOR/HDAC-IN-1 is a dual inhibitor targeting mTOR and HDAC, exhibiting IC50 values of 0.49 nM and 0.91 nM for mTOR and HDAC1, respectively. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and signaling pathways. Its selective inhibition profile offers potential for elucidating the roles of mTOR and HDAC in tumorigenesis and for developing novel cancer treatment strategies. -
HDAC3 Inhibitor
HDAC3-IN-T247 is a potent and selective inhibitor of HDAC3 (histone deacetylase 3), demonstrating an IC50 of 0.24 µM. This compound selectively enhances the acetylation of NF-κB in HCT116 cells, making it valuable for studies in cancer and viral pathogenesis. HDAC3-IN-T247 exhibits significant anticancer properties by inhibiting the proliferation of cancer cells and can also activate HIV gene expression in latently infected cells, thus serving as a useful tool for investigations in oncology and HIV research. -
HDAC2 Inhibitor
HDAC2-IN-2 is a selective inhibitor of histone deacetylase 2 (HDAC2), exhibiting a Kd value ranging from 0.1 to 1 μM. This compound is instrumental in studying the role of HDAC2 in various biological processes, including gene expression regulation and cell differentiation. Its inhibitory action makes it a valuable tool for researchers investigating epigenetic modifications and potential therapeutic targets in cancer and neurodegenerative diseases. -
LSD1/HDAC6/MAO-A Inhibitor
LSD1/HDAC6-IN-2 is a potent inhibitor targeting LSD1, HDAC6, and MAO-A, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. It demonstrates significant inhibitory effects on the growth of multiple myeloma cell lines, including MM.1S, MM.1R, and RPMI-8226. This compound is suitable for research applications focused on acute myeloid leukemia and lymphoma, providing insights into potential therapeutic mechanisms. -
HDAC3 Inhibitor
PT3 is a selective inhibitor of histone deacetylase 3 (HDAC3), demonstrating an IC50 value of 0.25 μM. This compound shows promising brain penetration capabilities and bioavailability following oral administration. PT3 is valuable for investigating the role of HDAC3 in neurodegenerative disorders, particularly in the context of Alzheimer’s disease research. -
HDAC Related
Ac-Arg-Gly-Lys(Ac)-AMC is a substrate specifically designed for the study of histone deacetylases (HDACs). It serves as a useful tool for measuring HDAC activity in various biological assays. This compound is instrumental in investigating the role of HDACs in cellular processes, as well as drug development related to cancer and other diseases where HDAC modulation may be therapeutic. -
HDAC3 Inhibitor
(E,E)-RGFP966 is a selective inhibitor of Histone Deacetylase 3 (HDAC3) that is capable of penetrating the central nervous system. This compound is particularly relevant for the investigation of neurodegenerative disorders, including Huntington's disease. Its specificity for HDAC3 makes it a valuable tool in studying the epigenetic regulation of gene expression and the accompanying mechanistic pathways involved in this condition. -
DNMT And HDAC Aual Inhibitor
DNMT/HDAC-IN-1 is a dual inhibitor targeting DNA methyltransferases (DNMT) and histone deacetylases (HDACs), demonstrating IC50 values of 56.84 nM for HDAC1 and 17.39 nM for HDAC6. This compound induces apoptosis in tumor cells and is valuable for cancer research applications, providing insights into the mechanisms of epigenetic regulation in malignancies. Its role in modulating both DNMT and HDAC activities makes it a significant tool for investigating therapeutic strategies in oncology. -
HDAC1 Inhibitor
HDAC1-IN-7 is a potent inhibitor of histone deacetylase 1 (HDAC1), exhibiting an IC50 of 0.957 mM. This compound serves as a valuable tool for investigating the role of HDAC1 in various biological processes, including gene expression regulation and cellular differentiation. Its application is relevant in studies of cancer biology and neurodegenerative disorders, where modulation of HDAC1 activity may provide insights into therapeutic strategies. -
HDAC11 Inhibitor
HDAC11-IN-2 is a selective inhibitor of Histone Deacetylase 11 (HDAC11), exhibiting an IC50 of 51.1 µM for HDAC11 and 5 µM for HDAC8. This compound effectively inhibits de novo lipogenesis and promotes fatty acid oxidation, addressing hepatic lipid accumulation and its associated pathological features in MASLD mouse models. Additionally, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172, further regulating metabolic pathways involved in lipid metabolism within the liver. -
HDAC6 Inhibitor
Bavarostat is a potent inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 17 nM, capable of crossing the blood-brain barrier. As a PET radiotracer, it can be labeled with 18F for in vivo mapping of HDAC6 distribution and assessing target occupancy in non-human primate models. Bavarostat selectively enhances tubulin acetylation without affecting histone acetylation, making it a valuable tool for research into neurodegenerative diseases, such as Alzheimer’s, as well as various cancers. -
PROTAC HDAC6 Degrader
HDAC6 Degrader-3 is a selective inhibitor that promotes the degradation of histone deacetylase 6 (HDAC6) through ternary complex formation and the ubiquitin-proteasome pathway, exhibiting a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces significant hyperacetylation of α-tubulin. This compound is valuable for research applications focused on neurodegenerative diseases and cancer, where modulation of HDAC6 activity may play a critical role. -
PROTAC HDAC Degrader
HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD). -
HDAC11 Inhibitor
TD034 is a selective, reversible, and noncovalent inhibitor of HDAC11, exhibiting an IC50 value of 5.1 nM and a Ki of 1.5 nM. This compound specifically targets HDAC11 without affecting other histone deacetylases or sirtuins, and it inhibits the defatty acylation of the substrate SHMT2. Additionally, TD034 reduces the levels of YAP1 through its action on HDAC11. This reagent is suitable for investigating the role of HDAC11 in lung cancer research. -
HDAC6/MAO-A/LSD1 Inhibitor
HDAC6-IN-3 is a potent inhibitor of histone deacetylase 6 (HDAC6), with an IC50 ranging from 0.02 to 1.54 μM for various HDAC isoforms, including HDAC1, HDAC2, HDAC3, and HDAC8. Additionally, it exhibits significant inhibitory activity against monoamine oxidase A (MAO-A) with an IC50 of 0.79 μM and lysine-specific demethylase 1 (LSD1). This compound serves as a valuable tool for research applications in cancer biology and epigenetics and is equipped with an alkyne functionality, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
HDAC6 Inhibitor
HDAC6-IN-23 is a potent inhibitor of the histone deacetylase HDAC6, exhibiting oral bioavailability. This compound demonstrates significant biological activity by modulating histone acetylation, which plays a crucial role in gene regulation and cellular processes. It is primarily utilized in research focused on neurodegenerative disorders, cancer therapy, and the study of protein homeostasis. -
HDAC Ligand
HDAC Ligand-1 is a selective histone deacetylase (HDAC) ligand that serves as a valuable building block for the synthesis of PROTAC HDAC degraders. This compound can facilitate the development of innovative therapeutic agents targeting HDAC enzymes, enhancing the understanding of their role in various biological processes. Its applications extend to cancer research and epigenetic studies, providing insights into the modulation of gene expression and cellular behavior. -
HDAC6/10 Inhibitor
HDAC-IN-4 is a selective inhibitor of HDAC6 and HDAC10, demonstrating pIC50 values of 7.2 and 6.8 in BRET assays, respectively. This compound exhibits antitumoral activity, making it a significant tool for the investigation of cancer biology and the modulation of gene expression. Its selective inhibition of these histone deacetylases positions HDAC-IN-4 as a valuable reagent for research focusing on epigenetic regulation and potential therapeutic applications in cancer treatment. -
HDAC Inhibitor
BG48 is a potent histone deacetylase (HDAC) inhibitor that selectively targets HDAC1 and HDAC2. By inhibiting the enzymatic activity of these enzymes, BG48 modulates gene expression and can influence cellular processes such as differentiation, proliferation, and apoptosis. This compound is valuable for research applications in cancer biology, neurodegenerative diseases, and epigenetic studies. -
HDAC I/IIb Inhibitor
Purinostat is a selective inhibitor of histone deacetylases (HDAC) I and IIb, exhibiting potent anti-leukemic activity. It effectively reduces the survival of Philadelphia chromosome-positive leukemic cells and CD34+ leukemic progenitors from chronic myeloid leukemia patients. By targeting HDAC I/IIb, Purinostat disrupts critical pathways for leukemic stem cell survival, influencing factors such as c-Myc, β-Catenin, E2F, Ezh2, Alox5, and mTOR. Additionally, Purinostat enhances glutamate metabolism in leukemic stem cells by upregulating GLS1. -
HDAC Inhibitor
HNHA is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 100 nM. The compound effectively induces cell cycle arrest at the G1/S phase through the upregulation of p21. HNHA has demonstrated the ability to inhibit tumor growth and neovascularization, suggesting potential applications in cancer research, particularly in the context of breast cancer therapeutics. -
PROTAC HDAC Degrader
JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models. -
HDAC Inhibitor
HDAC-IN-40 is a potent alkoxyamide-based inhibitor of histone deacetylases (HDACs), specifically targeting HDAC2 and HDAC6 with Ki values of 60 nM and 30 nM, respectively. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. HDAC-IN-40 can be utilized to explore the role of histone deacetylation in tumor development and progression, as well as to investigate potential therapeutic interventions in various cancers. -
PRMT5 Inhibitor
CMP-5 dihydrochloride is a specific and selective inhibitor of PRMT5, effectively blocking its methyltransferase activity without affecting PRMT1, PRMT4, or PRMT7. This compound inhibits the methylation of S2Me-H4R3 on histones, making it a valuable tool for studying PRMT5's role in cellular processes. Additionally, CMP-5 dihydrochloride has been shown to prevent EBV-driven transformation of B-lymphocytes while sparing normal B cells, highlighting its potential applications in cancer research and therapeutic development. -
EZH2 Inhibitor
CPI-905 is a potent and selective inhibitor of Enhancer of Zeste Homolog 2 (EZH2), a key enzyme involved in histone methylation and gene silencing. This compound effectively disrupts the methyltransferase activity of EZH2, leading to reactivation of tumor suppressor genes. CPI-905 is primarily utilized in cancer research, particularly in studies focusing on malignancies driven by EZH2 mutations or overexpression. -
EZH2 Inhibitor
GSK926 is a selective inhibitor of the histone lysine methyltransferase EZH2, exhibiting an IC50 of 0.02 μM and a Ki of 7.9 nM. This compound demonstrates SAM-competitive behavior and is active in cellular systems. GSK926 serves as a valuable tool in cancer research, particularly in studies targeting epigenetic regulation and the oncogenic functions of EZH2. -
PRMT5 Inhibitor
GSK591 hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5), exhibiting an IC50 of 4 nM. This compound is primarily utilized in research related to epigenetic regulation, particularly in the context of cancer biology. Its ability to modulate methylation processes makes it a valuable tool for studying the role of PRMT5 in various cellular functions and disease mechanisms. -
EZH2 Inhibitor
DCE_42 is a potent inhibitor of Enhancer of Zeste Homolog 2 (EZH2) with an IC50 value of 22.6 µM. This compound effectively inhibits cell proliferation, making it a valuable tool for investigating EZH2-related pathways in lymphoma research. Its specificity for EZH2 presents opportunities for studying the role of epigenetic regulation in cancer biology. -
Histone Methyltransferase
Fagaronine chloride is an alkaloid that acts as an inhibitor of histone methyltransferases. It possesses significant anti-tumor activity and has been shown to inhibit the reverse transcriptase of RSii tumor virus within a concentration range of 6-60 μg/mL. By interacting with the template primer, Fagaronine chloride disrupts DNA synthesis, making it a valuable tool for research into retroviral infections and cancer biology. -
HDAC1/2 Inhibitor
BG47 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, functioning as an optoepigenetic probe. Upon light-induced trans-to-cis isomerization, BG47 competitively inhibits the deacetylase activity of its targets, resulting in increased acetylation of Histone H3K9. This compound is relevant for research applications in neurological diseases, providing insights into epigenetic regulation and its implications in various disorders. -
PRMT1 Inhibitor
PRMT1-IN-2 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), exhibiting an IC50 of 55.4 μM. This compound induces histone hypomethylation in HepG2 cells, highlighting its potential role in epigenetic regulation. PRMT1-IN-2 is suitable for investigating the biological functions of PRMT1 and its implications in various cellular processes and diseases. -
Histone Methyltransferase
MS453 is a potent and selective inhibitor of the histone methyltransferase SETD8, exhibiting an IC50 of 804 nM. It preferentially targets a cysteine residue adjacent to the binding site, demonstrating specificity over 28 other methyltransferases. The crystal structure elucidates the binding mode of MS453 to SETD8, offering valuable insights for the design of advanced chemical probes aimed at this important target in epigenetic regulation. -
Histone Methyltransferase Inhibitor
(1-Nitroethene-1,2-diyl)dibenzene is a potent inhibitor of protein arginine methyltransferase 1 (PRMT1), exhibiting an IC50 of 11 μM in histone H4 methylation assays. This compound also effectively inhibits histone H4 methylation by PRMT8 at concentrations of 10 and 100 μM, while showing no effect on histone H3.1 methylation mediated by CARM1 or Set7/9. Its specificity and potency make it a valuable tool for studying histone methylation processes and their implications in epigenetics and gene regulation. -
SMYD3 Inhibitor
EPZ030456 is a potent and selective inhibitor of SMYD3, exhibiting an IC50 of 48 nM. This compound is primarily utilized in cancer research due to its role in targeting histone methylation processes associated with tumorigenesis. Its specificity for SMYD3 makes it a valuable tool for elucidating the mechanisms underlying cancer progression and for potential therapeutic applications. -
EZH2 Inhibitor
MC3629 is a selective inhibitor of the histone methyltransferase EZH2, demonstrating significant anti-tumor activity. It effectively inhibits the proliferation and self-renewal of SHH MB cancer cells while also inducing apoptosis. MC3629 serves as a valuable tool for investigating drug resistance mechanisms and the aggressiveness of tumors in cancer research. -
Histone Methyltransferase
4-Methoxycinnamyl alcohol targets histone methyltransferases and exhibits significant anticancer properties. It demonstrates cytotoxic activity against MCF-7, HeLa, and DU145 cancer cell lines, with IC50 values of 14.24, 7.82, and 22.10 μg/mL, respectively. Notably, 4-Methoxycinnamyl alcohol induces cell necrosis rather than apoptosis, as evidenced by a 48-hour DNA fragmentation assay. This compound is derived from Foeniculum vulgare, highlighting its potential relevance in cancer research applications. -
SMYD2 Inhibitor
(R)-BAY-598 is a potent inhibitor of the protein-lysine methyltransferase SMYD2, exhibiting an IC50 value of 1.7 μM. This compound selectively interferes with SMYD2 activity, making it a valuable tool for studying the role of lysine methylation in various biological processes. It is applicable in research focused on cancer biology and epigenetic regulation, facilitating the understanding of disease mechanisms and the development of potential therapeutic strategies. -
G9a Antagonist
GA001 is a potent G9a antagonist with an IC50 of 1.32 μM. This compound has been shown to induce autophagy and apoptosis, making it a valuable tool for research in breast cancer. Its ability to modulate epigenetic regulation offers significant potential in understanding cancer biology and developing therapeutic strategies. -
SMYD2 Inhibitor
EPZ032597 is a selective, noncompetitive inhibitor of SMYD2, exhibiting an IC50 value of 16 nM. This compound is relevant for research into pancreatic ductal adenocarcinoma, targeting the modulation of epigenetic regulation involved in cancer progression. Its specificity for SMYD2 makes it a valuable tool for investigating the enzyme's role in tumor biology and potential therapeutic strategies. -
Histone Methyltransferase
Acedapsone is a histone methyltransferase inhibitor with notable antimalarial and antimicrobial activities. Primarily utilized as a long-acting therapeutic for leprosy, Acedapsone also presents potential for research in epigenetic modulation and the treatment of other related infections. Its mechanism of action and biological profile make it a valuable reagent for studies in microbial resistance and histone modification.
