Catalog No.
Product Name
Application
Product Information
Citations
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PRMT5 Inhibitor
EPZ015666 is a potent inhibitor of the protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 22 nM. This compound is utilized in research focused on epigenetic regulation and has potential applications in the study of cancer and other diseases associated with aberrant PRMT5 activity. Its selective mode of action makes it a valuable tool for understanding the role of arginine methylation in various biological processes. -
LSD1/HDAC Inhibitor
LSD1/HDAC-IN-1 is a potent inhibitor of histone deacetylases (HDACs) and lysine-specific demethylase 1 (LSD1), demonstrating impressive inhibitory activity with IC50 values of 0.125 nM for HDAC1, 0.373 nM for HDAC2, 0.0118 nM for HDAC6, 0.103 nM for HDAC8, and 0.571 μM for LSD1. This compound is significant in cancer research, as it influences gene expression and histone modification, making it a valuable tool for studies addressing epigenetic regulation and potential therapeutic interventions. -
LSD1/HDAC6 Inhibitor
LSD1/HDAC6-IN-1 is a dual inhibitor targeting lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6), demonstrating significant anti-tumor activity. This compound is particularly relevant for research into multiple myeloma (MM), providing insights into epigenetic regulation and potential therapeutic strategies. Its oral bioavailability makes it suitable for in vivo studies in cancer research. -
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. -
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. -
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. -
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.
