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Catalog No.
Product Name
Application
Product Information
Citations
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EZH2 Inhibitor
EZH2-IN-2 is a potent inhibitor of the EZH2 enzyme, exhibiting an IC50 of 64 nM and a TR-FRET IC50 of 20 nM. This compound facilitates research into the dysregulation of EZH2 activity, which is implicated in various cancer and precancerous conditions. EZH2-IN-2 serves as a valuable tool for studying the mechanisms of tumorigenesis and exploring therapeutic strategies targeting EZH2 pathways. -
CDK9/EZH2 Dual-target Inhibitor
CDK9/EZH2-IN-1 is a dual-target inhibitor designed to inhibit both CDK9 and EZH2, exhibiting IC50 values of 83.9 nM and 108.6 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing DNA double-strand breaks (DSBs). It effectively inhibits the proliferation of various cancer cell lines, including MKN45, MDA-MB-453, and SW620, with IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM, respectively. CDK9/EZH2-IN-1 is suitable for research applications in understanding cancer cell biology and therapeutic development. -
Histone Methyltransferase Inhibitor
UNC2399, a selective inhibitor of the histone methyltransferase EZH2, exhibits high in vitro potency with an IC50 of 17 nM. This biotinylated compound facilitates the study of EZH2-mediated pathways by enabling researchers to probe histone methylation dynamics. UNC2399 is valuable for investigations into cancer biology, epigenetics, and therapeutic development targeting methyltransferases. -
G9a Inhibitor
MS0124 is a selective inhibitor of G9a-like protein (GLP) with a reported IC50 of 13±4 nM for GLP and 440±63 nM for G9a. This compound plays a significant role in epigenetic regulation by inhibiting histone methylation, which is critical in various biological processes, including gene expression and cell differentiation. MS0124 is valuable for research applications exploring the mechanisms of histone modification and its implications in disease states. -
PRMT5 Inhibitor
PRMT5-IN-20 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), targeting the methylation of arginine residues on histones and non-histone proteins. This compound exhibits significant anti-tumor activity, making it a valuable tool for cancer research. PRMT5-IN-20 is suitable for studies investigating the role of arginine methylation in various malignancies and the therapeutic potential of targeting PRMT5 in cancer biology. -
EZH2 Inhibitor
DM-01 is a potent and selective inhibitor of EZH2, a key regulator of histone methylation. It demonstrates significant biological activity in the context of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and genetically defined solid tumors associated with SNF5/INI-1/SMARCB1 alterations. This compound facilitates research into the molecular mechanisms driving these malignancies and offers potential therapeutic insights for targeted cancer treatment. -
PRMT5 Inhibitor
PRMT5-IN-39 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), targeting the enzymatic activity involved in arginine methylation. This compound exhibits significant anti-cancer properties, making it a valuable tool for studying the role of PRMT5 in tumorigenesis and cellular signaling pathways. Researchers can utilize PRMT5-IN-39 to investigate its therapeutic potential in various cancer models and assess its effects on cell growth and proliferation. -
PRMT7 Inhibitor
PRMT7-IN-2 is a selective inhibitor of Protein Arginine Methyltransferase 7 (PRMT7) with an IC50 value of 0.50 μM. This compound effectively arrests the cell cycle at the G0/G1 phase and promotes apoptosis, leading to inhibition of cell growth both in vivo and in vitro. PRMT7-IN-2 decreases monomethylarginine levels associated with PRMT7 activity and modulates epithelial and mesenchymal marker expression, enhancing the levels of E-cadherin while reducing those of N-cadherin, Vimentin, and ZEB2. Such properties make it a valuable tool for studying cancer biology and cellular transformation mechanisms. -
HIF-1α/EZH2 Inhibitor
DYB-03 is an orally active inhibitor of HIF-1α and EZH2. It effectively suppresses migration, invasion, and angiogenesis in lung cancer cells as well as human umbilical vein endothelial cells (HUVECs), demonstrated both in vitro and in vivo. Additionally, DYB-03 induces apoptosis in A549 and H460 cells that are resistant to 2-ME2 and GSK126, highlighting its potential in overcoming resistance in lung cancer therapies. -
PRMT6 Allosteric Inhibitor
SGC6870 is a selective allosteric inhibitor of the protein arginine methyltransferase 6 (PRMT6), exhibiting an IC50 of 77 nM. This compound functions by modulating PRMT6 activity, thereby influencing cellular processes such as gene expression and signal transduction. SGC6870 is useful for research focused on epigenetic regulation and the role of PRMTs in various diseases, including cancer and neurodegenerative disorders. -
Histone Methyltransferase Inhibitor
RL5a is an inhibitor of the histone methyltransferase SETD8. It effectively disrupts the methylation of lysine 27 on histone H3, playing a crucial role in the regulation of gene expression. This compound is utilized in research focused on epigenetics and the modulation of cellular processes, making it a valuable tool for studies on cancer biology and developmental processes. -
PRMT5 Inhibitor
(R)-AMG-193 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), functioning as a methionine adenosine transferase (MTA)-cooperative inhibitor. This compound demonstrates significant antitumor activity, particularly in MTAP-deficient tumor cells, with an IC50 value of 0.107 μM. It effectively inhibits PRMT5, allowing for the preferential targeting of tumor cells while sparing normal cells with intact MTAP. (R)-AMG-193 is a valuable tool for research into cancer biology and therapeutic strategies involving PRMT5 inhibition. -
EZH2 Inhibitor
EPZ011989 trifluoroacetate is a selective inhibitor of the enzyme EZH2, exhibiting a Ki value of less than 3 nM. This compound is notable for its ability to effectively inhibit histone methylation, thereby demonstrating significant anti-tumor activity. EPZ011989 trifluoroacetate is applicable in cancer research, providing insights into the role of EZH2 in tumorigenesis. Additionally, it features an alkyne group that facilitates click chemistry applications, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with compatible azide-containing molecules. -
EZH1/2 Inhibitor
(S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, specifically targeting the EZH2_Y641F variant with an IC50 of less than 100 nM. This pyridine-based compound demonstrates significant biological activity, making it a valuable tool for research in anti-tumor and autoimmune disease pathways. Its ability to modulate histone methylation presents opportunities for exploring epigenetic regulation in various therapeutic contexts. -
PRMT5 Inhibitor
PRMT5-IN-1 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 11 nM for the PRMT5/MEP50 complex. This hemiaminal compound can be metabolized to aldehydes, allowing it to form covalent adducts with C449 under physiological conditions. PRMT5-IN-1 is valuable for investigating the role of PRMT5 in various biological processes, including gene regulation and oncogenesis, making it a useful tool for cancer research and other studies involving protein methylation. -
ASH1L Inhibitor
AS-99 free base is a potent and selective inhibitor of the ASH1L histone methyltransferase, with an IC50 of 0.79 µM and a dissociation constant (Kd) of 0.89 µM. It demonstrates significant anti-leukemic activity by inhibiting cell proliferation, inducing apoptosis and differentiation, and downregulating MLL fusion target genes. AS-99 effectively reduces leukemia burden in vivo, making it a valuable tool for research into targeted therapies for leukemia and other ASH1L-related malignancies. -
Histone Methyltransferase Inhibitor
EML741 is a selective inhibitor of the histone methyltransferases G9a and GLP, characterized by an IC50 value of 23 nM for G9a and a Kd of 1.13 μM. Additionally, EML741 inhibits DNMT1 with an IC50 of 3.1 μM while demonstrating no significant effect on DNMT3a or DNMT3b. This compound exhibits low cytotoxicity, is membrane permeable, and is capable of crossing the blood-brain barrier, making it a valuable tool for epigenetic research and potential therapeutic applications. -
EZH2 Inhibitor
EPZ011989 hydrochloride is a potent inhibitor of the Zeste Homolog 2 (EZH2) enzyme, demonstrating a Ki value of less than 3 nM. This compound exhibits notable anti-tumor activity, making it a valuable tool in cancer research. Additionally, EPZ011989 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating various biochemical applications. -
Histone Methyltransferase Inhibitor
Igermetostat is a potent inhibitor of histone methyltransferase EZH2, which plays a crucial role in gene silencing and epigenetic regulation. This compound exhibits significant activity in both in vivo and in vitro models, making it valuable for cancer research. Its application in studies of tumor biology and potential therapeutic strategies underscores its importance in exploring epigenetic modulation in various malignancies. -
DOT1L Inhibitor
S-N6-Methyladenosylhomocysteine is a potent inhibitor of the histone methyltransferase DOT1L, exhibiting an IC50 value of 0.29 μM. By selectively targeting DOT1L, this compound plays a crucial role in cancer research, particularly in studies investigating the epigenetic regulation and its implications in oncogenesis. It serves as a valuable tool for understanding the biochemical pathways associated with methylation-driven cancers and may facilitate the development of therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-14 is a highly selective inhibitor of EZH2, a histone methyltransferase, with an IC50 of 12 nM. By specifically targeting and inhibiting the methyltransferase activity of EZH2 within the PRC2 complex, EZH2-IN-14 effectively reduces levels of H3K27me3. This compound exhibits over 200-fold selectivity for EZH2 compared to the closely related EZH1, making it a valuable tool for research into epigenetic regulation and cancer biology. -
SETD2 Inhibitor
EZM0414 TFA is a potent and selective inhibitor of SETD2, exhibiting an IC50 of 18 nM in biochemical assays and 34 nM in cellular assays. This orally active reagent is suitable for investigating its effects on relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma. EZM0414 TFA facilitates valuable research into the role of SETD2 in cancer biology and therapeutic development. -
SETD7 Inhibitor
PFI-2 hydrochloride is a potent and selective inhibitor of SET domain containing lysine methyltransferase 7 (SETD7). It exhibits significant inhibitory activity with an IC50 value of 2.0 nM, making it an essential tool for studying the role of SETD7 in various biological processes. PFI-2 hydrochloride is valuable for investigating mechanisms underlying chronic kidney disease and inflammation, particularly in the context of renal fibrosis research. -
SETDB1-TTD Inhibitor
SETDB1-TTD-IN-1 is a selective inhibitor targeting the tandem Tudor domain of the SET domain bifurcated protein 1 (SETDB1-TTD), exhibiting a binding affinity (Kd) of 88 nM. This compound enhances the methyltransferase activity of SETDB1, making it a valuable tool for investigating the biological roles and disease associations of SETDB1-TTD in epigenetic regulation and cellular processes. Researchers can utilize SETDB1-TTD-IN-1 to explore its implications in various biological contexts. -
PRMT5 Inhibitor
PF-06939999 is a potent, orally active inhibitor of protein arginine methyltransferase 5 (PRMT5), functioning as a S-adenosylmethionine (SAM) competitive antagonist. It effectively suppresses the expression of symmetric dimethylarginine (SDMA) protein, with an IC50 value of 1.1 nM in A427 cells. Due to its ability to inhibit PRMT5 activity, PF-06939999 demonstrates significant antitumor effects, making it valuable for cancer research focused on epigenetic regulation and methylation pathways. -
PRMT1 Inhibitor
Furamidine dihydrochloride is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), exhibiting an IC50 of 9.4 μM. This compound demonstrates significant selectivity for PRMT1 over PRMT5, PRMT6, and PRMT4, making it an essential tool for studying PRMT-related biological processes. In addition, Furamidine dihydrochloride inhibits tyrosyl-DNA phosphodiesterase 1 (TDP-1) competitively and reversibly, showing enhanced activity with duplex DNA substrates. Furthermore, it possesses antiparasitic properties, expanding its potential applications in chemical and biological research. -
SETD2 Inhibitor
EPZ-719 is a selective inhibitor of the SETD2 enzyme, exhibiting an IC50 value of 0.005 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. EPZ-719 may be utilized to explore the role of SETD2 in tumorigenesis and to evaluate potential treatment strategies targeting this pathway. -
DOT1L Inhibitor
Dot1L-IN-4 is a potent inhibitor of the DOT1L enzyme, exhibiting an IC50 of 0.11 nM. It effectively disrupts the activity of the telomeric silencing 1-like protein, making it a valuable tool for research into epigenetic regulation and gene expression modulation. Its application extends to studies on leukemia and other cancer types where DOT1L is implicated, facilitating investigations into therapeutic approaches targeting this pathway. -
Dot1L inhibitor
Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM. -
Menin-MLL interaction inhibitor
MI-2 (Menin-MLL inhibitor 2) specifically binds to Menin and inhibits Menin??s interaction with MLL fusion proteins in cells. It can effectively reverse MLL fusion protein?Cmediated leukemic transformation by downregulating the expression of target genes downstream of MLL fusion protein oncogenic activity. MI-2 is a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of Menin as an oncogenic cofactor of MLL fusion proteins. -
SMYD2 inhibitor
AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM). -
EZH2 inhibitor
3-deazaneplanocin A, also known as DZNep, is a well-known histone methyltransferase inhibitor, which disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma.
