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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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 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. -
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. -
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. -
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. -
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. -
PRMT5 Inhibitor
PRMT5-IN-16 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), which plays a crucial role in epigenetic regulation. This compound exhibits significant anti-tumor activity, making it a valuable tool for studying cancer biology and epigenetic modifications. PRMT5-IN-16 is suitable for research applications aimed at exploring the therapeutic potential of PRMT5 inhibition in various cancer models. -
PRMT5 Inhibitor
PRMT5-MTA-IN-4 is a potent irreversible inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating an IC50 of 8 nM. This compound effectively blocks arginine methylation, leading to the inhibition of ribosomal RNA processing and the expression of cell cycle-related proteins. PRMT5-MTA-IN-4 exhibits significant antiproliferative effects across various tumor cell lines, with an IC50 of 0.3 μM in DLD-1 cells. This reagent is an important tool for investigating hematological malignancies, including acute myeloid leukemia and diffuse large B-cell lymphoma. -
EZH2-EED interaction Inhibitor
DC-PRC2in-01 is a potent inhibitor of the EZH2-EED interaction, exhibiting an IC50 of 4.21 μM and a dissociation constant (Kd) of 4.56 μM. This compound disrupts the EZH2-EED complex, leading to degradation of PRC2 core components and a reduction in H3K27me3 levels. Consequently, DC-PRC2in-01 effectively inhibits PRC2-driven proliferation of lymphoma cells and induces cell cycle arrest. It is particularly valuable for studying PRC2-related malignancies, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL). -
G9a/GLP Inhibitor
Antitumor agent-101 is a selective covalent inhibitor of the lysine methyltransferases G9a and GLP, exhibiting IC50 values of 8.5 nM and 5.5 nM, respectively. This compound demonstrates significant antitumor efficacy in the PANC-1 xenograft model, making it a valuable tool for studying the role of G9a and GLP in cancer biology. Its mechanism of action provides insights into potential therapeutic strategies for targeting malignant cells through epigenetic modulation. -
PRMT5 inhibitor
PRMT5-IN-54 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound plays a critical role in modulating gene expression through arginine methylation. PRMT5-IN-54 is particularly useful for investigating its potential therapeutic effects in autoimmune diseases and other conditions where PRMT5 activity is implicated. By inhibiting PRMT5, this reagent may contribute to unraveling the molecular mechanisms underlying various pathological states. -
PRMT Inhibitor
GSK3368715 hydrochloride is a reversible, orally active inhibitor targeting type I protein arginine methyltransferases (PRMTs). It demonstrates potent inhibitory activity with IC50 values of 3.1 nM for PRMT1, 48 nM for PRMT3, 5.7 nM for PRMT6, and 1.7 nM for PRMT8, while exhibiting weaker activity against PRMT4 (IC50 1148 nM). This compound effectively induces changes in arginine methylation states, modifies exon usage, and exhibits significant anticancer effects, making it valuable for research in cancer biology and epigenetic regulation. -
Histone Methyltransferase Inhibitor
PRMT5-IN-13 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), which plays a crucial role in histone methylation. By inhibiting PRMT5, this compound facilitates the study of epigenetic regulation and its impact on gene expression. PRMT5-IN-13 is valuable for research applications involving cancer biology, as well as investigations into the roles of arginine methylation in cellular processes. -
Histone Methyltransferase Inhibitor
PRMT5-IN-55 is a selective inhibitor of the histone methyltransferase PRMT5, demonstrating a pIC50 value of 9.6 at a concentration of 10 nM. This compound plays a crucial role in modulating epigenetic processes by inhibiting arginine methylation, which can influence gene expression and cellular differentiation. PRMT5-IN-55 is valuable for research applications focused on cancer biology, epigenetics, and the therapeutic exploration of PRMT5 in various diseases. -
PRMT1 Inhibitor
PRMT1-IN-3 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), demonstrating an IC50 of 4.11 μM. In addition to its primary activity against PRMT1, it also inhibits PRMT6 and PRMT8 with IC50 values of 23.3 and 30.1 μM, respectively. PRMT1-IN-3 effectively reduces asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells, leading to cell cycle arrest, apoptosis, and decreased migration and colony formation in MDA-MB-231 cells. This compound serves as a potential chemotherapeutic sensitizer for Paclitaxel and is valuable for research concerning TNBC. -
GSK-3β/G9a Inhibitor
GSK-3β/G9a-IN-1 is a selective inhibitor of GSK-3β and G9a, acting through competitive mechanisms with IC50 values of 0.8 μM and 1.1 μM, respectively. This compound is effective in lowering tau phosphorylation and reducing Aβ aggregation, making it relevant for Alzheimer's disease research. Additionally, GSK-3β/G9a-IN-1 influences chromatin dynamics by inhibiting H3K9me2 and modulating members of the SAGA complex. Its ability to improve memory and restore social behaviors highlights its potential as a therapeutic agent in neurodegenerative conditions. -
PRMT5 Inhibitor
PRMT5-IN-29 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 1.5 μM. This compound demonstrates significant biological activity and is suitable for advancing research in cancer biology, particularly in the context of targeted therapies. Its potency and oral bioavailability make it a valuable tool for investigating the role of PRMT5 in various malignancies. -
EZH2 Inhibitor
EZH2-IN-23 is a selective inhibitor of the EZH2 enzyme, exhibiting potent inhibition of the PRC2 complex with an IC50 of 0.8 nM. It effectively reduces H3K27 trimethylation in cellular assays with an IC50 of 40 nM, making it a valuable tool for studying epigenetic regulation. Additionally, EZH2-IN-23 demonstrates favorable pharmacokinetic properties in rat models, featuring 100% oral bioavailability, which enhances its potential for in vivo research applications. -
PRMT5 Inhibitor
PRMT5-IN-43 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound exhibits significant biological activity by disrupting PRMT5-mediated methylation processes, which play a crucial role in cancer cell proliferation and survival. Its application in cancer research makes it a valuable tool for investigating the mechanisms of oncogenesis and potential therapeutic interventions targeting PRMT5. -
PRMT5•MTA Inhibitor
PRMT5-MTA-IN-5 is an irreversible inhibitor targeting the PRMT5•MTA complex, with an IC50 value of 1.15 nM. This compound effectively inhibits arginine methylation, disrupting ribosomal RNA processing and affecting the expression of proteins associated with the cell cycle. PRMT5-MTA-IN-5 demonstrates potent antiproliferative effects in MTAP-deficient tumor cells, making it a valuable tool for research on MTAP-deficient solid tumors, including liver, breast, and pancreatic cancers. -
SETD8 Inhibitor
[Nle20] H4 peptide (16−23) is a potent inhibitor of the histone methyltransferase SETD8, exhibiting a Kd of 0.14 μM. This peptide competes with histone H4 for binding to the substrate site of SETD8, effectively blocking its methylation activity. As a result, [Nle20] H4 peptide (16−23) serves as a valuable tool in cancer research, offering potential applications in the development of therapeutic strategies targeting epigenetic modulation. -
PRMT5 Inhibitor
PRMT5-IN-44 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound exhibits significant anti-proliferative effects in various cancer cell lines, making it a valuable tool for studying the role of PRMT5 in tumorigenesis. PRMT5-IN-44 is particularly relevant for research applications focused on cancer biology and therapeutic development targeting PRMT5-mediated pathways. -
LSD1/G9a Inhibitor
LSD1-IN-20 is a potent dual non-covalent inhibitor of lysine-specific demethylase 1 (LSD1) and G9a, exhibiting Ki values of 0.44 and 0.68 μM, respectively. This compound demonstrates significant antiproliferative effects in THP-1 leukemia and MDA-MB-231 breast cancer cell lines, with IC50 values of 0.51 and 1.60 μM over 72 hours. LSD1-IN-20 serves as a valuable tool for research focused on epigenetic regulation and its implications in cancer biology. -
PRMT3 Inhibitor
PRMT3-IN-5 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with an IC50 value of 291 nM. This compound is valuable for studying the biological roles of PRMT3 and its implications in various diseases. Its specificity and potency make PRMT3-IN-5 a useful tool in epigenetic research and therapeutic investigations. -
Histone Methyltransferase Inhibitor
PRMT5-IN-9 is an inhibitor specifically targeting protein arginine methyltransferase 5 (PRMT5). This compound exhibits potent inhibitory activity with an IC50 of 0.01 μM, making it a valuable tool for cancer research. PRMT5-IN-9 can be utilized to study the role of arginine methylation in gene expression, cellular signaling, and tumor progression, thereby aiding in the exploration of novel therapeutic strategies.
