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.
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Catalog No.
Product Name
Application
Product Information
Citations
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HCV/HDAC6 Inhibitor
Nicoxamat, also known as N-Hydroxynicotinamide, functions as an inhibitor of hepatitis C virus (HCV) and selectively targets HDAC6. This compound exhibits antiviral activity against HCV, making it a useful tool in research on hepatitis C infection. Its role as an HDAC6 inhibitor further supports investigations into epigenetic regulation and potential therapeutic strategies. -
Naa50 Inhibitor
Naa50-IN-1 is a potent inhibitor of N-alpha-acetyltransferase 50 (Naa50), exhibiting an IC50 of 7 nM against the human enzyme. This compound shows selectivity for related acetyltransferases, Naa10 and Naa60. Naa50-IN-1 interacts with the substrate-binding pocket of Naa50, with its binding affinity augmented by the presence of AcCoA, making it a valuable tool for investigating the biological roles of protein acetylation. Research applications include studies on gene regulation and enzyme activity related to Naa50 and its substrates. -
EZH2 Inhibitor
TDI-6118 is a potent inhibitor of the histone methyltransferase EZH2, known for its ability to penetrate the blood-brain barrier. This compound exhibits significant biological activity in targeting EZH2, making it a valuable tool for investigating central nervous system malignancies. Its application in research may contribute to a better understanding of the molecular mechanisms underlying various brain cancers. -
CARM1/HDAC2 inhibitor
CARM1/HDAC2-IN-1 is a dual inhibitor targeting both CARM1 and HDAC2, exhibiting IC50 values of 3.71 nM and 4.07 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. CARM1/HDAC2-IN-1 is suitable for studies investigating the role of these epigenetic regulators in tumor biology and therapeutic strategies. -
DOT1L Inhibitor，PROTAC
DOT1L705 is a PROTAC degrader that selectively targets DOT1L, facilitating the recruitment of the VHL E3 ubiquitin ligase for proteasomal degradation of the protein. This leads to a significant reduction in H3K79 methylation levels, ultimately decreasing the viability of leukemia cells. DOT1L705 is particularly relevant for research focused on MLL-rearranged leukemia, making it a valuable tool for investigating the underlying mechanisms of disease progression. -
HuR Inhibitor
SRI-43265 is a selective inhibitor of human antigen R (HuR) dimerization, a crucial process impacting HuR's role in post-transcriptional regulation of target mRNAs. By disrupting HuR multimers, SRI-43265 demonstrates potential in studying cancer and inflammatory processes, where HuR's activity contributes to pathogenesis. This reagent is valuable for investigating the molecular mechanisms underlying these diseases and for exploring therapeutic strategies targeting HuR functions. -
HuR Inhibitor
ZM-32 is a potent inhibitor of human antigen R (HuR), a critical regulator of mRNA stability. By downregulating the expression of vascular endothelial growth factor A (VEGF-A) and matrix metalloproteinase 9 (MMP9), ZM-32 effectively inhibits angiogenesis in breast cancer. Demonstrating broad-spectrum anti-proliferative effects across various cancer cell lines, ZM-32 also shows significant antitumor efficacy in mouse models of the MDA-MB-231 breast cancer cell line. -
HuR-ARE Inhibitor
Azaphilone-9 (AZA-9) is a potent inhibitor of the HuR-ARE RNA interaction, demonstrating an IC50 value of 1.2 μM. By binding to the RNA-binding protein Hu antigen R (HuR), Azaphilone-9 disrupts the stabilization of various oncogenic mRNAs in tumor cells. This mechanism suggests that Azaphilone-9 may serve as a valuable tool for investigating cancer cell growth and progression in research applications targeting RNA-protein interactions. -
HuR Inhibitor
Okicenone is an inhibitor of Hu protein R (HuR), a key regulator of messenger RNA stability and translation. By disrupting HuR oligomerization and its RNA binding capabilities, Okicenone modulates HuR trafficking, influencing cytokine expression and T-cell activation. This compound is valuable in research focused on immune response modulation and the role of mRNA-binding proteins in cellular processes. -
METTL3 Inhibitor
METTL3-IN-1 is a potent METTL3 inhibitor designed to selectively inhibit the activity of the METTL3 methyltransferase. This compound demonstrates significant biological activity in modulating RNA methylation, making it a valuable tool for studying the role of METTL3 in various cellular processes. It is applicable in research areas such as epitranscriptomics and cancer biology, where understanding RNA modifications is crucial. -
METTL3 Inhibitor
METTL3-IN-2 is a selective inhibitor of the methyltransferase METTL3, exhibiting an IC50 value of 6.1 nM. This compound effectively inhibits cell proliferation in Caov3 ovarian cancer cells, providing a valuable tool for research into the regulation of RNA methylation and its implications in cancer biology. METTL3-IN-2 can be utilized in studies focused on understanding METTL3's role in tumor growth and the development of targeted cancer therapies. -
METTL3 Inhibitor
METTL3-IN-3 is a selective inhibitor of the methyltransferase METTL3, which plays a critical role in RNA m6A methylation. This compound demonstrates significant inhibition of METTL3 activity, thereby impacting the regulation of gene expression and RNA metabolism. METTL3-IN-3 is valuable for research applications focusing on epitranscriptomics, RNA modifications, and their implications in various biological processes and diseases. -
METTL3 Inhibitor
METTL3-IN-5 is a selective inhibitor of METTL3, a key enzyme involved in N6-methyladenosine (m6A) methylation. This compound demonstrates potent inhibitory effects on the growth of MOLM-13 cells, with an IC50 of less than 2 μM. While exhibiting minimal hERG inhibitory activity (IC50 >30 μM), METTL3-IN-5 is a valuable tool for researching acute myeloid leukemia (AML) and m6A-related biological processes. -
METTL3 Inhibitor
METTL3-IN-13 is a selective inhibitor of the methyltransferase METTL3. This compound exhibits significant biological activity by disrupting RNA methylation, which plays a critical role in various cancer types including hypopharyngeal squamous cell carcinoma and non-small cell lung cancer. It serves as a valuable tool for investigating the role of METTL3 in oncogenic processes and may assist in the development of targeted therapies. -
miR-155 Inhibitor
Cobomarsen sodium is a targeted miR-155 inhibitor that modulates various signaling pathways, including JAK/STAT, MAPK/ERK, and PI3K/AKT, contributing to the regulation of cell survival. This oligonucleotide is primarily employed in research focused on B-cell lymphoma, enabling insights into the molecular mechanisms of this malignancy and potential therapeutic strategies. -
miR-155 Inhibitor
Cobomarsen is an oligonucleotide inhibitor targeting miR-155. This compound modulates various signaling pathways associated with cell survival, including the JAK/STAT, MAPK/ERK, and PI3K/AKT pathways. Cobomarsen is primarily utilized in research focused on B-cell lymphoma, providing insights into miRNA-mediated gene regulation and potential therapeutic approaches. -
TET Inhibitor
TETi76 is a potent inhibitor of TET family enzymes, demonstrating IC50 values of 1.5 μM for TET1, 9.4 μM for TET2, and 8.8 μM for TET3. By competitively binding to the active site of these enzymes, TETi76 effectively decreases cytosine hydroxymethylation and inhibits the clonal growth of TET2 mutant cells both in vitro and in vivo, while sparing normal hematopoietic precursor cells. This selective activity makes TETi76 a valuable tool for investigating leukemia and studying TET-related pathways in cancer research. -
TET1 Inhibitor
NSC-311068 is a potent inhibitor of TET1, targeting the enzyme's transcriptional activity and its role in modifying 5-hydroxymethylcytosine (5hmC). This compound effectively reduces TET1 expression levels and attenuates global 5hmC levels. NSC-311068 demonstrates significant cytotoxicity in acute myeloid leukemia (AML) cells characterized by elevated TET1 expression, making it a valuable tool for studying TET1-related pathways and potential therapeutic approaches in AML. -
WDR5 Inhibitor
WDR5-IN-5 is a selective inhibitor targeting the WIN site of the WD repeat domain 5 (WDR5). This compound demonstrates significant anti-proliferative activity against various cancer cell lines and possesses favorable pharmacokinetic properties in murine models. With a high binding affinity to WDR5, the Ki value is recorded at less than 0.02 nM, making it a valuable tool for research into cancer biology and potential therapeutic applications. -
WDR5 Inhibitor
WDR5-IN-6 is a selective inhibitor of WDR5, acting primarily at the WBM site. This compound demonstrates significant anti-tumor activity by inhibiting cell proliferation in neuroblastoma cell lines. Additionally, WDR5-IN-6 exhibits notable synergy with OICR-9429, another WDR5 inhibitor that targets the WIN site. This compound is valuable for research applications focused on neuroblastoma and related oncological studies. -
WDR5 Inhibitor
WM-586 is a covalent inhibitor of WDR5, effectively disrupting the interaction between WDR5 and MYC with an IC50 value of 101 nM. This compound demonstrates significant potential in cancer research, particularly in the study of neuroblastoma, breast cancer, bladder cancer, and colorectal cancer. Its ability to target the WDR5-MYC complex makes it a valuable tool for exploring therapeutic strategies in various malignancies. -
WDR5-MYC Interaction Inhibitor
WM-662 is an inhibitor targeting the WDR5-MYC interaction, exhibiting an IC50 of 18 μM. This compound is particularly relevant for investigations into cancer biology, aging processes, and neurodegenerative disorders. Its ability to disrupt the WDR5-MYC interaction positions WM-662 as a valuable tool in studying dysregulated gene expression associated with these conditions. -
WDR5-MYC Interaction Inhibitor
Anticancer agent 126 is a specific inhibitor of the WDR5-MYC interaction, targeting the critical role of this complex in oncogenic signaling. This compound effectively disrupts the binding of WDR5 to MYC, leading to a reduction in MYC target gene expression. It is suitable for research applications focused on elucidating the mechanisms of cancer biology and developing therapeutic strategies against MYC-driven malignancies. -
WDR5 Inhibitor
WDR5-IN-7 is a potent inhibitor of WD repeat domain 5 (WDR5), utilizing a benzoxazepinone structure. This compound exhibits significant anti-cancer activity and is particularly useful in the study of various tumor models. WDR5-IN-7 serves as a valuable tool for elucidating the role of WDR5 in oncogenic processes and for exploring therapeutic strategies in cancer research. -
WDR5-MLL1 Inhibitor
DDO-2213 is a potent inhibitor of the WDR5-MLL1 complex, exhibiting an IC50 of 29 nM and a Kd value of 72.9 nM for WDR5. This compound selectively targets MLL histone methyltransferase activity, effectively inhibiting the proliferation of cells containing MLL translocations. DDO-2213 is a valuable tool for research focused on MLL fusion leukemia and its underlying mechanisms. -
WDR5-MLL1 Inhibitor
WDR5-0102 is a selective inhibitor of the WDR5-MLL1 complex, exhibiting a dissociation constant (Kd) of 4 μM and a competitive inhibition constant (Kdis) of 7 μM. This compound effectively suppresses the H3K4 methyltransferase activity of MLL1 without affecting other human methyltransferases, including SETD7 and several others such as G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5. WDR5-0102 is a valuable tool for investigating the role of MLL1 in various biological processes and its implications in cancer research. -
MLL1-WDR5 PPI Inhibitor
DDO-2093 is a selective inhibitor of the MLL1-WDR5 protein-protein interaction, exhibiting a potent IC50 of 8.6 nM and a dissociation constant (Kd) of 11.6 nM. This compound demonstrates significant antitumor activity by selectively targeting and inhibiting the catalytic function of the MLL complex. DDO-2093 is useful in research focused on understanding MLL-related oncogenesis and potential therapeutic strategies in cancer treatment. -
PARP-1 Inhibitor
PARP-1-IN-32 is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1). This compound is utilized in cancer research to investigate the mechanisms of DNA repair and cellular response to genotoxic stress. Its ability to selectively inhibit PARP-1 makes it a valuable tool for studying the role of this enzyme in tumor biology and therapeutic resistance. -
SIRT6 Inhibitor
SIRT6-IN-6 is a selective inhibitor of SIRT6, demonstrating a potent IC50 of 4.93 μM and a Ki of approximately 10 μM. This compound shows significant selectivity against other histone deacetylases, including SIRT1-3 and HDAC1-11. Research findings indicate that SIRT6-IN-6 effectively elevates the expression of the glucose transporter GLUT-1, which contributes to the reduction of blood glucose levels in mouse models of type 2 diabetes. This reagent is valuable for studies focused on the mechanistic pathways associated with type 2 diabetes and metabolic regulation. -
Sirtuin Inhibitor
MC3482 is a selective inhibitor of sirtuin 5 (SIRT5), known for its role in mitochondrial metabolism and deacylation processes. This compound effectively modulates SIRT5 activity, making it valuable for studies examining the implications of SIRT5 in cellular energy regulation and metabolic disorders. Its use in research can contribute to understanding SIRT5's role in various physiological and pathological conditions, including cancer and neurodegeneration. -
SIRT5 Inhibitor
MC3138 is a selective SIRT5 inhibitor, demonstrating notable antitumor activity in human pancreatic ductal adenocarcinoma (PDAC) cells, with IC50 values ranging from 25.4 to 236.9 μM. In preclinical studies, MC3138 enhances the efficacy of Gemcitabine, significantly inhibiting tumor growth in murine models. This compound is valuable for research into targeted cancer therapies and the modulation of metabolic pathways related to SIRT5 activity. -
SIRT5 Inhibitor
Et-29 is a potent inhibitor of SIRT5, with a reported Ki value of 40 nM, demonstrating selectivity for this target. By modulating the activity of SIRT5, Et-29 plays a significant role in the study of metabolic processes and post-translational modifications. This reagent is ideal for research applications focused on the regulation of cellular metabolism and potential therapeutic strategies in metabolic diseases. -
SIRT6 Inhibitor
SIRT6-IN-2 is a selective and competitive inhibitor of SIRT6, exhibiting an IC50 of 34 μM. This compound enhances the acetylation of H3K9 and promotes glucose uptake in cultured cells. Additionally, SIRT6-IN-2 demonstrates the ability to reduce T cell proliferation, showcasing its immunosuppressive properties and potential chemosensitizing effects. Research applications include the study of metabolic regulation and immune response modulation. -
SIRT Inhibitor
SIRT-IN-3 is a selective inhibitor of SIRT1 with an IC50 of 17 μM. It demonstrates approximately 4-fold selectivity over SIRT2 and 14-fold selectivity over SIRT3, exhibiting IC50 values of 74 μM and 235 μM, respectively, for these isoforms. This compound is valuable for research applications investigating the role of SIRT1 in cellular processes, including aging, metabolism, and gene regulation. -
SIRT5 Inhibitor
SIRT5 Inhibitor 3 is a potent and competitive inhibitor of SIRT5, exhibiting an IC50 value of 5.9 μM. This compound effectively inhibits the desuccinylation activity of SIRT5, making it a valuable tool for studying the enzyme's role in various biological processes. SIRT5 Inhibitor 3 is applicable in research focused on cancer and neurodegenerative diseases, providing insights into potential therapeutic strategies. -
SIRT1 Inhibitor
SIRT1-IN-4 is a selective SIRT1 inhibitor that demonstrates an IC50 of 10.04 μM. This compound is utilized in research focused on cancer biology, providing valuable insights into the role of SIRT1 in tumorigenesis and potential therapeutic approaches. Further studies may explore its utility in modulating cellular processes regulated by SIRT1. -
SIRT1 Inhibitor
(S)-Selisistat is a selective inhibitor of SIRT1, demonstrating an IC50 value of 98 nM. This compound effectively modulates the activity of the sirtuin family of proteins, which are implicated in various cellular processes, including metabolism and aging. (S)-Selisistat is valuable for research exploring the role of SIRT1 in age-related diseases and metabolic disorders, making it a crucial tool for investigating therapeutic strategies in these areas. -
SIRT3 Inhibitor
SIRT3-IN-1 is a potent Sirtuin 3 (SIRT3) inhibitor with an IC50 value of 0.043 μM. This compound selectively inhibits SIRT3, making it a valuable tool for studying the role of SIRT3 in acute myeloid leukemia (AML) and other related conditions. Its specific action on SIRT3 allows for targeted investigations into cellular metabolism, oxidative stress response, and potential therapeutic strategies in AML research. -
SIRT7 Inhibitor
YZL-51N is a selective inhibitor of SIRT7, with an IC50 value of 12.71 μM. By occupying the NAD+ binding pocket, YZL-51N inhibits SIRT7 enzyme activity, thereby compromising DNA damage repair mechanisms and reducing cancer cell viability. Its demonstrated anti-tumor activity makes YZL-51N a valuable tool for cancer research applications. -
SIRT1 Inhibitor
SIRT1-IN-3 is a selective inhibitor of SIRT1, exhibiting an IC50 value of 4.2 μM. This compound effectively modulates SIRT1 activity, making it a valuable tool for studies investigating the role of SIRT1 in various biological processes. Research applications include the exploration of SIRT1's involvement in metabolism, aging, and stress response pathways. -
SIRT1 Inhibitor
SIRT1-IN-2 is a potent and selective inhibitor of SIRT1 (silent information regulator 1), demonstrating an IC50 value of 1.6 μM. This compound plays a critical role in research focused on understanding the regulation of cellular metabolism, aging, and stress response pathways. Its specific inhibition of SIRT1 makes it a valuable tool for studying related biological processes and therapeutic interventions. -
Sirt2 Inhibitor
Sirt2-IN-2 is a selective inhibitor of the Sirtuin 2 (Sirt2) enzyme, exhibiting an IC50 of 0.118 μM. This compound is instrumental in research aimed at studying the role of Sirt2 in cellular processes and its implications in neurodegenerative diseases. Its use facilitates investigations into the potential therapeutic effects of Sirt2 modulation. -
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. -
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. -
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. -
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. -
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.
