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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Histone Methyltransferases Inhibitor
TM2-115 is a potent inhibitor of histone methyltransferases in malaria parasites. By targeting these essential enzymes, TM2-115 leads to rapid and irreversible lethality in the parasites. This compound is crucial for studies aimed at understanding the epigenetic regulation of malaria and provides valuable insights into potential therapeutic strategies for combatting malaria infections. -
SMYD2 Inhibitor
EPZ033294 is a potent inhibitor of SMYD2, exhibiting an IC50 value of 3.9 nM. SMYD2 is a histone methyltransferase responsible for the methylation of lysine residues, notably converting BTF3 to BTF3me1. This compound effectively prevents the methylation process, as demonstrated by a concentration-dependent inhibitory effect observed in 293T cells. EPZ033294 is valuable for research applications focused on epigenetic regulation and the role of SMYD2 in various cellular processes. -
PRMT5 Inhibitor
PRMT5-IN-37 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme involved in epigenetic regulation and gene expression. This compound exhibits significant biological activity in blocking PRMT5 function, resulting in the inhibition of cellular proliferation in various cancer models. PRMT5-IN-37 is particularly useful for research applications focused on cancer biology and the development of targeted therapies. -
SETD7 Inhibitor
(S)-PFI-2 hydrochloride selectively inhibits the lysine methyltransferase SETD7, demonstrating approximately 500-fold higher potency compared to its (R) enantiomer. This compound operates via a unique mechanism that alters the catalytic functionality of SETD7, influencing the binding dynamics with substrate peptides and cofactor interactions. Its targeted inhibition positions (S)-PFI-2 as a valuable tool for investigating SETD7's role in various biological processes, including epigenetic regulation and cellular signaling pathways. This compound is particularly relevant for research applications focused on methylation dynamics and related therapeutics. -
Histone Methyltransferase Inhibitor
UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3), effectively disrupting its enzymatic activity. This compound plays a significant role in regulating histone methylation, thus influencing gene expression and chromatin dynamics. UNC2327 is utilized in research applications focused on epigenetic modifications and the functional study of PRMT3 in various biological contexts. -
EZH2/PRC2 Inhibitor
NPD13668 is an inhibitor of EZH2, targeting the polycomb repressive complex 2 (PRC2) to modulate gene silencing. This compound effectively disrupts EZH2 activity, leading to the reactivation of silenced H3K27me3 target genes and subsequent depletion of the H3K27me3 modification. NPD13668 is applicable in studies focused on prostate and ovarian cancer, providing insights into epigenetic regulation and potential therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-7 is a potent inhibitor of Enhancer of Zeste Homolog 2 (EZH2), targeting the enzyme involved in histone methylation. This compound effectively reduces the abnormal levels of H3K27 methylation associated with EZH2 overexpression and mutations, which contribute to the progression of various cancers, including breast cancer, prostate cancer, and leukemia. EZH2-IN-7 serves as a valuable tool for cancer research, particularly in understanding the role of EZH2 in tumor development and exploring potential therapeutic strategies. -
Histone Methyltransferase
WAY-260022 is a selective inhibitor targeting norepinephrine reuptake, exhibiting potent activity against norepinephrine transporters. This compound demonstrates significant selectivity for serotonin and dopamine reuptake inhibition, making it a valuable tool in neuropharmacological research. WAY-260022 has also shown oral efficacy in preclinical studies, particularly in models of thermoregulatory dysfunction, highlighting its potential applications in understanding neurochemical pathways. -
PRMT5 Inhibitor
PRMT5-IN-49 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound exhibits significant antitumor activity by disrupting PRMT5-mediated methylation processes, which are critical for oncogenic signaling and cell proliferation. PRMT5-IN-49 is instrumental in cancer research and the investigation of epigenetic regulatory mechanisms in various malignancies. -
Histone Methyltransferase Inhibitor
PRMT5-IN-11 is a selective inhibitor of the protein methyltransferase complex PRMT5:MEP50, designed to disrupt histone methylation. With its structure-dependent activity in the (sub)micromolar range, this compound serves as a valuable tool for studying epigenetic regulation. It is ideally suited for research applications involving cancer biology and chromatin modifications. -
PRMT5 Inhibitor
PRMT5-IN-50 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting oral activity and favorable metabolic stability. This compound effectively inhibits symmetric dimethylarginine (SDMA) methylation in both MTAP-deleted and MTAP-wild type HCT116 cell lines, with IC50 values of 1.0 nM and 536 nM, respectively. Additionally, PRMT5-IN-50 demonstrates robust anti-proliferative effects, showing IC50 values of 19 nM and 1620 nM for tumor cell growth inhibition. In vivo studies indicate that PRMT5-IN-50 significantly suppresses tumor growth in mouse models, supporting its potential utility in cancer research. -
PRMT1 Inhibitor
PRMT1-IN-1 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), which plays a crucial role in regulating gene expression and cellular signaling through arginine methylation. This compound exhibits potent inhibitory activity against PRMT1 and has applications in cancer research and investigations into epigenetic modulation. Its ability to selectively target PRMT1 makes it a valuable tool for elucidating the biological functions of this enzyme in various cellular processes. -
Histone Methyltransferase Inhibitor
PRMT5-IN-10 is a selective inhibitor of the protein methyltransferase complex PRMT5:MEP50. It demonstrates structure-dependent inhibition, affecting its ability to catalyze the methylation of histones. This compound is useful in investigating the role of PRMT5 in various biological processes, including gene expression regulation and epigenetic modifications, making it a valuable tool for research in cancer biology and epigenetics. -
PRMT5 inhibitor
PRMT5-IN-33 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating a competitive binding mechanism with an IC50 of 10.9 nM. This compound effectively induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cell lines, highlighting its potential as a therapeutic agent. PRMT5-IN-33 exhibits significant antitumor activity, making it a valuable tool for cancer research and drug development. -
Histone Methyltransferase
D595 is a phenylethylamine derivative that functions primarily as a histone methyltransferase inhibitor. This compound exhibits significant biological activity by inhibiting the uptake of monoamine neurotransmitters, displaying a high affinity for the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). Structural modifications, particularly alterations in hydroxyl stereochemistry, can influence its binding interactions with these transporters, demonstrating a specific stereoselectivity. D595 is suitable for studies involving neuropharmacology and epigenetic regulation. -
SMYD3 Inhibitor
EPZ028862 is a selective inhibitor of SMYD3, a histone methyltransferase involved in the regulation of gene expression. By targeting SMYD3, EPZ028862 disrupts cellular proliferation and oncogenic signaling pathways, demonstrating significant potential in cancer research applications. Its specificity makes it a valuable tool for studying the role of SMYD3 in tumor biology and for exploring therapeutic strategies against various cancers. -
Histone Methyltransferase Inhibitor
GSK2807 is a potent and selective histone methyltransferase inhibitor that competitively inhibits SAM binding to SMYD3, with a Ki value of 14 nM. This compound is valuable for cancer research, as it effectively prevents the methylation of MEKK2, thereby potentially influencing cell proliferation and tumor progression. GSK2807 is a promising tool for studying the role of SMYD3 in cancer biology and for evaluating therapeutic strategies targeting histone methylation. -
PRMT5 Inhibitor
PRMT5-IN-21 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), a crucial enzyme involved in the regulation of gene expression and cellular signaling. This compound effectively suppresses PRMT5 activity, leading to alterations in histone and non-histone protein methylation. PRMT5-IN-21 is valuable for research applications aimed at investigating the role of PRMT5 in various biological processes, including cancer progression and cellular differentiation. -
PRMT5 Inhibitor
PRMT5-IN-36-d3 is a deuterated derivative of the PRMT5 inhibitor PRMT5-IN-36. This compound serves as an orally bioavailable inhibitor of protein arginine methyltransferase 5 (PRMT5), a target of interest in cancer research. PRMT5-IN-36-d3 is utilized to study the role of PRMT5 in tumorigenesis and its potential as a therapeutic target in various malignancies. -
EZH2 Inhibitor
EZH2-IN-19 is a potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of 0.32 nM. This compound is primarily utilized in cancer research to investigate the epigenetic regulation of gene expression mediated by EZH2. Its specific inhibition of EZH2 makes it a valuable tool for studying various malignancies associated with dysregulated histone methylation. -
DOT1L Inhibitor
EPZ-4777 is a selective inhibitor of DOT1L, targeting the methylation of histone H3 at lysine 79 (H3K79) in cancer cells. This compound effectively blocks the expression of genes associated with leukemia and selectively induces cell death in translocated cells, making it a valuable tool in cancer research. Its specificity for DOT1L-related pathways positions EPZ-4777 as a significant reagent for studying leukemogenesis and potential therapeutic interventions. -
PRMT5 Inhibitor
PRMT5-IN-53 is a potent, orally bioavailable inhibitor of PRMT5, exhibiting pIC50 values of ≥ 9.7 against both human and mouse PRMT5. It demonstrates high affinity for the PRMT5:MEP50 complex with a KD of 11.3 pM. This compound effectively inhibits PRMT5 in the intestines of murine models, leading to a significant reduction in the number and size of polyps while minimizing systemic hematological toxicity. PRMT5-IN-53 is particularly valuable for research in colorectal cancer, especially in the context of familial adenomatous polyposis (FAP). -
EZH2 Inhibitor
SKLB-03220 is a selective covalent inhibitor of EZH2, exhibiting an IC50 of 1.72 nM for EZH2MUT. This compound demonstrates minimal activity against other histone methyltransferases and kinases, ensuring its specificity. SKLB-03220 has shown significant potency in ovarian cancer cell lines, inducing apoptotic processes, and effectively inhibits tumor growth in the PA-1 xenograft model. It is an important tool for research focused on ovarian cancer pathways and treatments. -
PRMT5 Inhibitor
PRMT5-IN-51 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits potent antiproliferative activity in various cancer cell lines, making it a valuable tool for investigating the role of PRMT5 in tumorigenesis. This compound is useful for research applications focused on understanding the molecular mechanisms of cancer and the therapeutic potential of PRMT5 inhibition. -
PRMT5 Ligand
PRMT5 ligand 1 is a specific ligand for the enzyme PRMT5, which plays a crucial role in the regulation of various cellular processes through protein arginine methylation. This compound serves as a valuable tool in the development of proteolysis-targeting chimeras (PROTACs), particularly in synthesizing the degrader MS4322. Its application in research facilitates the investigation of PRMT5's biological functions and its potential as a therapeutic target in cancer and other diseases. -
EZH2 Ligand
EZH2 ligand-1 is a small molecule that specifically binds to the Enhancer of Zeste Homolog 2 (EZH2), a key component of the PRC2 complexes involved in epigenetic regulation through histone methylation. This compound serves as a valuable tool for synthesizing PROTACs aimed at targeted protein degradation and is relevant for studying oncogenic processes linked to EZH2 dysregulation. Its application in research contributes to the understanding of cancer biology and the development of novel therapeutic strategies. -
EZH2 Degrader
PROTAC EZH2 Degrader-3 (compound ZJ-20) specifically targets and degrades the EZH2 protein through a proteolysis-targeting chimera (PROTAC) mechanism. This compound demonstrates potent inhibition of EZH2 expression as well as a significant reduction in other PRC2 subunits and H3K27me3 levels. Additionally, PROTAC EZH2 Degrader-3 exhibits anti-proliferative effects, inducing cell cycle arrest in the G0-G1 phase and promoting apoptosis in cancer cells, making it valuable for research in cancer therapeutics and epigenetic regulation. -
G9a Inhibitor
G9a-IN-2 is a potent inhibitor of the histone methyltransferase G9a, exhibiting an IC50 of 0.024 μM. This compound effectively reduces levels of H3K9me2 and promotes the mRNA expression of γ-globin. G9a-IN-2 holds potential for therapeutic applications in ameliorating sickle cell disease (SCD) through its modulation of epigenetic mechanisms. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-9 is an orally active PROTAC that selectively degrades EZH2 via the ubiquitin-proteasome pathway. By downregulating PRC2 core subunits and inhibiting H3K27me3, it effectively reverses PRC2-mediated gene silencing and disrupts EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 demonstrates potent antiproliferative effects on various cancer cell lines, inducing cell cycle arrest and apoptosis. This reagent is valuable for research focused on leukemia, lymphoma, and non-small cell lung cancer. -
EZH2 Inhibitor
YM281 is a potent inhibitor of the EZH2 enzyme, a key component of the polycomb repressive complex involved in histone methylation. This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase, demonstrating significant antitumor activity in vivo. YM281 holds promise for research applications focused on lymphoma and may contribute to the development of targeted therapies in epigenetic regulation studies. -
PRMT5 Inhibitor
PRMT5-IN-28 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound targets the enzyme responsible for the arginine methylation of various proteins, which plays a crucial role in gene expression regulation, mRNA splicing, and cellular signaling pathways. Inhibition of PRMT5 has been shown to impede cancer cell proliferation and promote apoptosis, making it valuable for research applications in cancer biology and therapeutic development. Additionally, targeting PRMT5 may provide insights into mechanisms of immune evasion in tumors. -
Histone Methyltransferase
Lobelane hydrochloride selectively inhibits the vesicular monoamine transporter-2 (VMAT2). This compound demonstrates an affinity for VMAT2 with a K(i) value of 630 nM, while exhibiting low interaction with nicotinic acetylcholine receptors (nAChR). The unique mechanism of action of lobelane hydrochloride makes it a valuable tool for studying neurotransmitter dynamics and offers potential in the development of therapeutic agents aimed at addressing methamphetamine abuse. Its structural analogs may further expand its applications in neuropharmacological research. -
PRMT5 Inhibitor
PRMT5-IN-52 is a potent non-nucleoside inhibitor of Protein Arginine Methyltransferase 5 (PRMT5), demonstrating an inhibitory rate of 20.2% at a concentration of 10 μM. This compound exhibits significant antitumor activity, making it a valuable tool for research in various cancer types, including lung, prostate, and colorectal carcinoma. It provides a promising avenue for investigating the role of PRMT5 in cancer biology and therapeutic development. -
G9a Inhibitor
CSV0C018875 is a quinoline-based inhibitor targeting the G9a protein (EHMT2). This compound demonstrates reduced cytotoxicity compared to other G9a inhibitors, making it a valuable tool for studies related to epigenetic regulation. Its selective inhibition of G9a can facilitate research into the roles of histone methylation in gene expression and various diseases, providing insights into potential therapeutic strategies. -
Histone Methyltransferase
JNJ-7925476 is a selective inhibitor of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT), targeting histone methyltransferase activity. This compound demonstrates rapid absorption, resulting in a brain concentration that is seven times greater than that in plasma. In vivo studies reveal a dose-dependent increase in extracellular levels of serotonin, norepinephrine, and dopamine in the rat cerebral cortex. Additionally, JNJ-7925476 exhibits significant antidepressant-like effects in behavioral assays, highlighting its potential for application in depression research and neuropharmacology. -
PRMT5 Inhibitor
AZ-PRMT5i-1 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating potent inhibitory activity while targeting MTAP-deficient cancers. This compound exhibits both in vitro and in vivo antitumor properties and shows cooperativity with methylthioadenosine (MTA). AZ-PRMT5i-1 is useful for research applications focused on the therapeutic potential of disrupting aberrant PRMT5 activity in cancer models. -
Histone Methyltransferase Inhibitor
PRMT6-IN-2 is a potent inhibitor of the histone methyltransferases PRMT6 and CARM1, exhibiting an IC50 value of 30 nM. This compound targets PRMT6, which is frequently overexpressed in various cancer cell types, and demonstrates promising potential for anticancer therapeutic development. Its dual inhibition mechanism makes PRMT6-IN-2 an important tool for investigating the role of arginine methylation in cancer progression. -
Histone Methyltransferase Inhibitor
(R)-BAY-6035 is a selective inhibitor of histone methyltransferase, specifically targeting the methylation of MAP3K2 by SMYD3. This compound exhibits nanomolar potency and offers high specificity against various kinases and protein lysine methyltransferases. It is suitable for research applications exploring gene regulation, epigenetic modifications, and signaling pathways related to cancer and other diseases. -
Histone Methyltransferase
Aclantate is a selective inhibitor of histone methyltransferases, which plays a crucial role in the regulation of gene expression through epigenetic modifications. This compound exhibits significant anti-inflammatory and analgesic activity, making it valuable in studies related to pain management and inflammatory diseases. Aclantate is particularly relevant for research focused on autoimmune conditions such as rheumatoid arthritis, providing insights into therapeutic strategies for alleviating inflammation and associated pain. -
G9a/GLP Inhibitor
DS79932728 is a potent inhibitor of G9a and GLP, demonstrating IC50 values of 12.6 nM and 75.7 nM, respectively. This compound effectively induces the endogenous production of γ-globin, leading to elevated levels of fetal hemoglobin (HbF) and an increase in the proportion of F-reticulocytes. Its favorable oral absorption properties have been validated in cynomolgus monkey models, making it a valuable tool for research on hematological disorders and therapeutic strategies aimed at enhancing HbF synthesis. -
Histone Methyltransferase Control
(R)-OR-S1 is a potent inhibitor of histone methyltransferases EZH1 and EZH2, exhibiting selective dual activity against both enzymes. This reagent has demonstrated the capacity to induce cell differentiation and apoptosis in acute myeloid leukemia (AML) cells, suggesting its potential application in targeted therapy. Notably, (R)-OR-S1 does not lead to significant myelosuppression, allowing for normal hematopoiesis to persist post-treatment, especially when combined with cytarabine. These properties highlight (R)-OR-S1’s promise as a clinically tolerable option for patients undergoing PRC2-targeted treatment in AML. -
PRMT5 Inhibitor
PRMT5-IN-47 is a selective, orally bioavailable inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 15 nM. This compound demonstrates significant antiproliferative effects and is recognized for its potential anticancer activity. PRMT5-IN-47 serves as a valuable tool in cancer research, enabling studies on cellular proliferation and the therapeutic targeting of PRMT5 in various malignancies. -
SETD7 Inhibitor
DC-S238 is a highly selective inhibitor of the histone methyltransferase SETD7 (SETD7) with an IC50 of 4.88 μM. This compound is effective in modulating histone methylation and is valuable for investigating its role in cancer, diabetes, and inflammatory disease research. Its oral bioavailability and specificity make it a useful tool for elucidating the biological functions associated with SETD7. -
PRMT5 Inhibitor
PRMT5-IN-17 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme involved in epigenetic regulation. This compound demonstrates significant anti-tumor activity, making it a promising candidate for cancer research. PRMT5's role in modulating gene expression through arginine methylation highlights the relevance of PRMT5-IN-17 in studies aimed at understanding cancer progression and developing novel therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-18 is a potent inhibitor of enhancer of zeste homologue 2 (EZH2) with an IC50 of 1.01 nM. This compound effectively inhibits cell proliferation and induces apoptosis in tumor cells. EZH2-IN-18 is utilized in research applications focusing on cancer biology and epigenetic regulation, making it a valuable tool for studies on EZH2-related pathways and therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2), demonstrating significant anticancer activity. It acts competitively with the cofactor S-adenosylmethionine (SAM) and non-competitively with peptide or nucleosome substrates. This compound is instrumental in research applications focused on targeted cancer therapies and understanding the epigenetic regulation of gene expression. -
PRMT5 Inhibitor
PRMT5-IN-19 is a selective non-nucleoside inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating IC50 values of 23.9 nM in radioactive biochemical assays and 47 nM in AlphaLISA assays. This compound effectively occupies the SAM-binding pocket of PRMT5, inhibiting its methyltransferase activity with notable selectivity for PRMT5 over other PRMTs and protein lysine methyltransferases (PKMTs). PRMT5-IN-19 has been shown to inhibit cell proliferation through the induction of apoptosis, making it useful for research in cancer biology and therapeutic development. -
PRMT5-MTA complex Inhibitor
PRMT5-MTA-IN-8 is a potent inhibitor of the PRMT5-MTA complex, with an IC50 value of 4.4 nM. This compound effectively reduces the intracellular levels of symmetric dimethylarginine (SDMA) and inhibits the proliferation of MTAP-deficient cells. Research has demonstrated its antitumor activity, particularly in mouse models of triple-negative breast cancer, by promoting tumor cell apoptosis through PRMT5 inhibition. PRMT5-MTA-IN-8 is suitable for investigations into cancer biology and therapeutic strategies targeting PRMT5-related pathways. -
EZH2 Inhibitor
DCE_254 is an EZH2 inhibitor with an IC50 value of 11 μM, demonstrating significant antiproliferative activity against lymphoma cell lines. It interferes with the SAM-mediated methyl transfer process, thereby inhibiting the development of hypermethylation-related cancers, with an IC50 of 10.3 μM. This compound is valuable for research into targeted therapies for cancers influenced by epigenetic modifications. -
EZH2 Inhibitor
EZH2-IN-5 is a highly potent inhibitor of the EZH2 enzyme, exhibiting IC50 values of 1.52 nM for wild-type EZH2 and 4.07 nM for the mutant variant Tyr641. This compound effectively interferes with the methyltransferase activity of EZH2, leading to a reduction in histone methylation. EZH2-IN-5 is utilized in research focused on cancer biology, particularly in hematological malignancies and solid tumors characterized by aberrant EZH2 activity.
