Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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 Ligand
PRMT5 ligand 3 (Compound S19) is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme involved in epigenetic regulation. This compound plays a crucial role in the development of PROTACs (Proteolysis Targeting Chimeras) aimed at targeting PRMT5 for degradation, thereby facilitating research into cancer and other diseases characterized by dysregulated methylation. PRMT5 ligand 3 is essential for studies focused on the therapeutic potential of targeted protein degradation strategies. -
Histone Methyltransferase
ZLD10A is a potent and selective inhibitor of the histone methyltransferase EZH2, effectively blocking H3K27 methylation. Demonstrating nanomolar potency against both wild-type and mutant forms of EZH2, ZLD10A exhibits over 1000-fold selectivity compared to other histone methyltransferases. Its ability to inhibit cell proliferation in diffuse large B-cell lymphoma (DLBCL) cell lines in a concentration- and time-dependent manner highlights its potential as an antiproliferative agent. ZLD10A serves as a valuable tool for investigating EZH2 mutant lymphomas. -
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. -
Histone Methyltransferase
JMV 236 is a potent histone methyltransferase inhibitor that modulates epigenetic regulation. It exhibits significant appetite-suppressing activity by antagonizing cholecystokinin, influencing the interaction between the intestinal peptide PrRP and the CCK1 receptor. This compound activates PrRP neurons in the nucleus of the solitary tract (NTS), enhancing its effects on food intake regulation, particularly in starvation conditions. JMV 236 is valuable in research applications focused on appetite control and metabolic disorders. -
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. -
G9a Inhibitor
CSV0C018875 hydrochloride is a selective inhibitor of G9a (EHMT2), effectively blocking its enzymatic activity in both enzyme and cell-based assays. This compound demonstrates a lower toxicity profile compared to the known G9a inhibitor BIX-01294, making it a valuable tool for research. CSV0C018875 binds tightly to the active site of G9a, enhancing the compound's inhibitory potency and prolonging its residence time. Its potential for improved ADME (absorption, distribution, metabolism, and excretion) and pharmacodynamic properties positions CSV0C018875 as a promising candidate for further biological studies. -
DOT1L Inhibitor
Dot1L-IN-7 is a potent inhibitor of DOT1L (disruptor of telomeric silencing 1-like protein) with an IC50 of 1.0 μM. This compound selectively induces cytotoxic effects in Mixed Lineage Leukemia (MLL)-AF9 cells while leaving E2A-HLF cells unaffected. It serves as a valuable tool for studying the roles of DOT1L in leukemogenesis and evaluating potential therapeutic strategies for MLL. -
PRMT5 Inhibitor
PRMT5-IN-39-d3 is a deuterated inhibitor targeting protein arginine methyltransferase 5 (PRMT5). This orally bioavailable compound is essential for investigating the role of PRMT5 in various cancer models. Its specific inhibition of PRMT5 provides insights into epigenetic regulation and potential therapeutic applications in oncology research. -
EZH2 Inhibitor
EZH2-IN-22 is a potent inhibitor of EZH2, exhibiting IC50 values of less than 0.00051 µM for the EZH2 (Y641N) and EZH2 (Y641F) mutants, and 0.00052 µM for wild-type EZH2. This compound demonstrates significant antiproliferative activity, making it a valuable tool for research in epigenetic regulation and cancer biology. Its application extends to studies of EZH2-related pathways and therapeutic approaches for tumors exhibiting EZH2 mutations. -
PRMT5 Inhibitor
PRMT5-IN-18 is a highly effective inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme implicated in various cancer pathways. This compound demonstrates strong selectivity and potency, making it a valuable tool for investigating the role of PRMT5 in oncogenesis. Its utility in biochemical assays and cellular studies provides insights into potential therapeutic strategies targeting PRMT5-related diseases. -
EZH2 Inhibitor
BBDDL2059 is a selective covalent inhibitor targeting the histone methyltransferase EZH2, demonstrating an IC50 of 1.5 nM against the EZH2-Y641F mutation. This compound effectively inhibits lymphoma cell proliferation at nanomolar concentrations, making it a valuable tool for anticancer research. BBDDL2059 is suitable for investigations into the mechanistic roles of EZH2 in cancer biology and therapeutic development. -
PRMT5 Inhibitor
PRMT5-IN-32 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It effectively reduces HCT116 cell proliferation, demonstrating an IC50 value of 0.13 μM. This compound is valuable for research investigating the role of PRMT5 in cancer biology and for assessing the therapeutic potential of PRMT5 inhibition in various malignancies. -
Histone Methyltransferase
Prospasmine hydrochloride is an anticholinergic agent that primarily targets histone methyltransferases, influencing gene expression through epigenetic modification. Its biological activity includes the inhibition of glandular secretions and the relaxation of smooth muscles, making it beneficial in the study of gastrointestinal disorders and smooth muscle spasm relief. Additionally, it demonstrates potential as an anesthetic adjuvant, providing a versatile tool for research in both analgesic and gastrointestinal pharmacology.
