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Catalog No.
Product Name
Application
Product Information
Citations
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Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) oxalate is an orally active and highly selective inhibitor of the menin–KMT2A (MLL) interaction, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits tumor cell proliferation and induces apoptosis and differentiation, particularly in cancers driven by KMT2A rearrangements. Bleximenib oxalate is a promising candidate for research in leukemia and other menin–KMT2A-dependent malignancies. -
G9a inhibitor
RK-701 is a highly selective and non-genotoxic inhibitor of G9a histone methyltransferase, with an IC₅₀ of 23–27 nM. It selectively upregulates fetal hemoglobin (HbF), γ-globin, and *BGLT3* expression, while downregulating H3K9me2 levels. RK-701 also exhibits inhibitory effects on the transcriptional repressors BCL11A and ZBTB7A, making it a promising candidate for the treatment of hemoglobinopathies such as sickle cell disease and β-thalassemia. -
PRMT4 inhibitor
TP-064 is a potent and selective inhibitor of protein arginine methyltransferase 4 (PRMT4/CARM1), with an IC50 of less than 10 nM. It effectively inhibits the dimethylation of BAF155 and MED12 with IC50 values of 340 nM and 43 nM, respectively. TP-064 shows minimal activity against other PRMT family members, except for PRMT6 (IC50 = 1.3 μM). It exhibits anticancer activity, making it a valuable tool for studying PRMT4-related epigenetic regulation and cancer therapy. -
PRMT5 inhibitor
AM-9747 (PRMT5-IN-25) is a highly potent PRMT5 inhibitor with a Ki value of 0.06 nM. It exhibits strong antiproliferative activity, making it a valuable candidate for research in PRMT5-driven cancers and epigenetic regulation. -
PRMT5 inhibitor
CMP-5 is a potent and highly selective inhibitor of PRMT5, exhibiting no inhibitory activity against related enzymes PRMT1, PRMT4, or PRMT7. It specifically blocks the symmetric dimethylation of histone H4 at arginine 3 (H4R3me2s) by targeting PRMT5-mediated methyltransferase activity. CMP-5 effectively prevents Epstein-Barr virus (EBV)-induced transformation of B lymphocytes while sparing normal B cells, highlighting its potential as a selective epigenetic modulator in virus-associated malignancies. -
SETD2 inhibitor
EZM0414 is a potent, selective, and orally bioavailable inhibitor of the histone methyltransferase SETD2, exhibiting an IC₅₀ of 18 nM in biochemical assays and 34 nM in cellular assays. It is being investigated for its therapeutic potential in relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma (DLBCL), making it a valuable tool for studying SETD2-mediated epigenetic regulation in hematologic malignancies. -
PRMT5 inhibitor
TNG-462 is an orally active and selective inhibitor of PRMT5, designed to exploit vulnerabilities in cancers characterized by methylthioadenosine phosphorylase (MTAP) deficiency and/or elevated methylthioadenosine (MTA) levels. By targeting MTA-sensitized PRMT5 activity, TNG-462 demonstrates potent antitumor efficacy in preclinical models of MTAP-deleted cancers. -
PRMT5 inhibitor
AMG 193 is an orally bioavailable, MTA-cooperative inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting potent antitumor activity. By leveraging the accumulation of methylthioadenosine (MTA) in MTAP-deficient cells, AMG 193 selectively inhibits PRMT5 with an IC₅₀ of 0.107 μM, leading to preferential suppression of tumor cell growth while sparing normal cells with intact MTAP function. -
Histone methyltransferase inhibitor
SGC3027 is a potent, selective, and cell-permeable inhibitor of the protein arginine methyltransferase PRMT7, serving as the first validated chemical probe for this target. As a histone methyltransferase inhibitor, SGC3027 enables the functional study of PRMT7-mediated arginine methylation and its role in epigenetic regulation. -
SUV39H1 methyltransferase inhibitor
F5446 (Compound 1) is a selective small-molecule inhibitor of the histone methyltransferase SUV39H1. By reducing H3K9 trimethylation (H3K9me3) at the Fas promoter, F5446 upregulates Fas expression and enhances the sensitivity of colorectal carcinoma cells to Fas ligand (FasL)-induced apoptosis in vitro. In vivo, F5446 effectively suppresses the growth of human colorectal tumor xenografts, highlighting its potential as an epigenetic therapeutic agent in cancer treatment. -
PRDM9 inhibitor
MRK-740 is a potent and selective small-molecule inhibitor of the histone methyltransferase PRDM9, acting in a substrate-competitive manner with an IC₅₀ of 80 nM. It exhibits high selectivity for PRDM9 over other histone methyltransferases and non-epigenetic targets. MRK-740 effectively inhibits PRDM9-mediated trimethylation of histone H3 at lysine 4 (H3K4me3), with an IC₅₀ of 0.8 µM in cellular assays. -
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. -
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 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. -
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. -
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 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. -
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. -
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.
