Catalog No.
Product Name
Application
Product Information
Citations
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PRMT5 Inhibitor
PRMT5-IN-41 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating potent enzymatic inhibition with oral bioavailability. In addition to its primary mechanism, PRMT5-IN-41 exhibits off-target inhibition of the hERG ion channel, with an IC50 value of 1.36 µM. This compound is valuable for research applications investigating the role of PRMT5 in various biological processes, including cancer progression and gene regulation. -
PRMT1 Inhibitor
DCPT1061 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), as well as PRMT6 and PRMT8. It demonstrates significant biological activity with a reduced effect on other PRMTs, such as PRMT3, PRMT4, and PRMT5, as well as other epigenetic enzymes. This compound exhibits antitumor effects, making it a valuable tool for research into cancer biology and epigenetic regulation. -
EZH2 Inhibitor
EZH2-IN-4 is a potent inhibitor of the EZH2 enzyme, exhibiting IC50 values of 0.923 nM for wild type EZH2 and 2.65 nM for mutant EZH2. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and epigenetic regulation. Its oral bioavailability enhances its potential for in vivo studies targeting EZH2-driven malignancies. -
EZH2/HSP90 Inhibitor
EZH2/HSP90-IN-29 is a dual inhibitor targeting both EZH2 and HSP90, exhibiting IC50 values of 6.29 nM for EZH2 and 60.1 nM for HSP90. This compound enhances the expression of apoptosis and necrosis-related genes, induces M-phase cell cycle arrest, and disrupts the reactive oxygen species catabolism pathway. Additionally, EZH2/HSP90-IN-29 has the capability to cross the blood-brain barrier, making it a valuable tool for research in cancer biology and neurodegenerative diseases. -
PRMT5-MTA Inhibitor
PRMT5-MTA-IN-7 is a selective inhibitor of the PRMT5-MTA complex, demonstrating a KD of 236 nM for PRMT5-MTA and 2.84 μM for PRMT5-SAM. It exhibits IC50 values of 4.08 μM and 13.6 μM for these targets, respectively. This compound selectively inhibits the proliferation of MTAP-deficient cancer cells, making it a valuable tool for research in colon cancer and related studies. -
EZH2/EZH1 Inhibitor
EZH2-IN-1 is a selective inhibitor targeting EZH2 and EZH1 through a SAM-competitive mechanism. It demonstrates potent inhibition with IC50 values of 32 nM for wild-type EZH2, 197 nM for the EZH2 Y641N mutant, and 213 nM for EZH1. This compound effectively reduces levels of bulk H3K27me3 and H3K27me2, highlighting its potential utility in research related to diffuse large B cell lymphoma. -
PRMT5 Inhibitor
PRMT5-IN-40 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits potent inhibition of PRMT5 enzymatic activity, which is critical for regulating various biological processes, including gene expression, cell proliferation, and apoptosis. This compound is valuable for researchers studying epigenetic modifications and the role of PRMT5 in cancer and other diseases. -
PRMT1 Inhibitor
Furamidine is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), exhibiting an IC50 of 9.4 μM, while maintaining a considerably lower affinity for PRMT5, PRMT6, and PRMT4. Additionally, Furamidine acts as a reversible, competitive inhibitor of tyrosyl-DNA phosphodiesterase 1 (TDP-1), demonstrating enhanced inhibition with duplex DNA substrates. This compound has applications in research focusing on methylation patterns and DNA repair mechanisms, as well as serving as an antiparasitic agent. -
EZH2 Inhibitor
EZH2-IN-16 is a potent inhibitor of the histone methyltransferase EZH2, targeting both the wild-type and the Y641F mutant forms with IC50 values of 37.6 nM and 79.1 nM, respectively. This compound effectively inhibits the proliferation of WSU-DLCL2 cells, demonstrating a GI50 of 0.2 μM. EZH2-IN-16 is valuable for research applications focused on epigenetic regulation and oncology, particularly in the context of EZH2-related pathways in cancer progression. -
PRMT5 Inhibitor
PRMT5-IN-36 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), which plays a critical role in regulating gene expression and cellular signaling. This compound demonstrates significant anticancer activity, making it a valuable tool in cancer research. Its oral bioavailability facilitates in vivo studies, allowing for deeper exploration of PRMT5's involvement in tumorigenesis and potential therapeutic applications in malignancies. -
PRMT5 Inhibitor
PRMT5-IN-34 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), which plays a critical role in gene expression and cellular signaling through the methylation of arginine residues on target proteins. This compound demonstrates significant biological activity by modulating PRMT5 activity, thereby influencing various cellular processes including cell proliferation and differentiation. PRMT5-IN-34 is invaluable for research applications aimed at understanding the role of arginine methylation in cancer and other diseases related to dysregulation of methyltransferases. -
EZH2/EED Interaction Inhibitor
SAH-EZH2 is an EZH2/EED interaction inhibitor designed to disrupt the binding between embryonic ectoderm development (EED) and the EZH1/EZH2 complex. This stable α-helical peptide selectively inhibits the trimethylation of histone H3 at lysine 27 (H3K27me3), providing a valuable tool for studying epigenetic regulation. SAH-EZH2 is applicable in research focused on developmental biology and the mechanisms of cancer progression related to the regulation of gene expression by histone modifications. -
EZH2 Inhibitor
Tanshindiol C is an EZH2 inhibitor that competes with S-adenosylmethionine, demonstrating an IC50 of 0.55 μM for inhibiting methyltransferase activity. It activates Nrf2 and Sirtuin 1 (Sirt1) in macrophages, suggesting potential roles in oxidative stress response. Tanshindiol C exhibits anti-cancer properties and may serve as a valuable tool in research related to atherosclerosis and epigenetic regulation. -
Histone Methyltransferase Inhibitor
PRMT5-IN-15 is a potent inhibitor of the histone methyltransferase PRMT5, exhibiting an IC50 value of 0.84 nM. This compound selectively targets PRMT5, disrupting its enzymatic activity and consequently influencing epigenetic regulation. PRMT5-IN-15 is valuable for research into gene expression, cellular differentiation, and cancer biology, particularly in studying the role of arginine methylation in various pathological conditions. -
PRMT5/MTA Complex Inhibitor
(S)-Navlimetostat is a selective inhibitor of the PRMT5/MTA complex, demonstrating an IC50 value of 7070 nM. This compound exhibits significant potential in modulating arginine methylation processes, making it a valuable tool for studying the role of PRMT5 in various biological pathways. It is particularly relevant for research applications in cancer, neurodegenerative diseases, and other conditions associated with dysregulated methylation. -
Histone Methyltransferase Inhibitor
CPI-1328 is a potent inhibitor of the histone methyltransferase EZH2, exhibiting a Ki value of 63 fM. This compound is primarily utilized in research to investigate the role of EZH2 in gene regulation, cancer progression, and epigenetic modifications. It is particularly relevant for studies exploring the therapeutic potential of targeting histone methylation pathways in various malignancies. -
G9a Inhibitor
DCG066 is a selective inhibitor of the lysine methyltransferase G9a, effectively binding to G9a and obstructing its methyltransferase activity in vitro. This compound has been shown to decrease di-methylation levels of histone H3 at lysine 9 (H3K9Me2), leading to inhibition of cell proliferation and induction of apoptosis. Additionally, DCG066 exhibits low cytotoxicity in leukemia cell lines characterized by elevated G9a expression, such as K562, making it a valuable tool for studying the role of G9a in oncogenesis and potential therapeutic applications. -
Histone Methyltransferase
HLCL-61 is a potent small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme involved in histone methylation. By selectively targeting PRMT5, HLCL-61 disrupts its activity, leading to alterations in gene expression and potential therapeutic effects in various cancers. This compound serves as a valuable tool for researching the role of arginine methylation in epigenetic regulation and the mechanistic pathways associated with PRMT5 in cancer biology. -
EZH2 Inhibitor
EZH2-IN-17 is a potent EZH2 inhibitor with an IC50 value of 0.95 nM, demonstrating significant selectivity and oral bioavailability. This compound exhibits robust anti-proliferative activity against various lymphoma cell lines, including WSU-DLCL2, Pfeiffer, and Karpas-422, with IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively. EZH2-IN-17 is useful for research focused on epigenetic modulation and the investigation of EZH2's role in cancer progression. -
PRMT Inhibitor
MS023 trihydrochloride is a potent and selective inhibitor of human type I protein arginine methyltransferases (PRMTs), demonstrating impressive IC50 values of 30 nM for PRMT1, 119 nM for PRMT3, 83 nM for PRMT4, 4 nM for PRMT6, and 5 nM for PRMT8. Its ability to effectively inhibit these enzymes makes it a valuable tool for research into the roles of PRMTs in various biological processes and disease states. This compound is suitable for studies involving cellular signaling, epigenetics, and post-translational modifications. -
EZH2 Inhibitor
(R)-HH2853 is a selective inhibitor of the EZH2 enzyme, specifically targeting the mutant EZH2-Y641F variant with an IC50 of less than 100 nM. This compound demonstrates potential in therapeutic applications related to cancer and autoimmune diseases, enabling researchers to investigate its effects on histone methylation and gene regulation. Its specificity for mutant EZH2 may provide insights into mechanisms of malignancy and contribute to the development of novel treatment strategies. -
PRMT4/PRMT6 Inhibitor
MS049 dihydrochloride is a selective inhibitor of protein arginine methyltransferases PRMT4 and PRMT6, demonstrating IC50 values of 34 nM and 43 nM, respectively. This compound effectively reduces the levels of dimethylated Med12 and H3R2 in HEK293 cells, making it valuable for studying the role of arginine methylation in cellular processes. MS049 dihydrochloride shows low toxicity and does not adversely affect cell proliferation, offering a reliable tool for research into epigenetic regulation and associated pathways. -
G9a Inhibitor
G9a-IN-1 is a targeted inhibitor of the G9a protein (EHMT2), a nuclear histone lysine methyltransferase responsible for the dimethylation of histone H3 at lysine 9 (H3K9me2), a modification linked to transcriptional repression. By inhibiting G9a, G9a-IN-1 plays a crucial role in unraveling the mechanisms of gene silencing associated with various pathological conditions. This compound is valuable for research in autoimmune disorders and cancer, offering insights into therapeutic strategies for these diseases. -
Histone Methyltransferase Inhibitor
PRT543 is a selective inhibitor of the histone methyltransferase PRMT5, targeting key epigenetic modifications associated with various cancers and hematological disorders. This compound demonstrates significant efficacy in inhibiting PRMT5 activity, leading to alterations in gene expression and cellular phenotypes relevant to cancer progression and disorders such as sickle cell disease and hereditary persistence of fetal hemoglobin (HPFH). PRT543 serves as a valuable tool for researchers investigating the role of PRMT5 in epigenetic regulation and its potential as a therapeutic target. -
PRMT6 Degrader
SKLB-0124 is a selective degrader of Protein Arginine Methyltransferase 6 (PRMT6) with an IC50 of 1.6 μM. This compound induces proteasome-dependent degradation of PRMT6, resulting in significant inhibition of cell proliferation and the induction of apoptosis and cell cycle arrest. SKLB-0124 has demonstrated DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells, making it a valuable reagent for researching lung and breast cancer. It does not degrade PRMT1 or PRMT8, ensuring specificity in studies involving PRMT6. -
Type I PRMT Inhibitor
GSK3368715 trihydrochloride is a highly selective inhibitor targeting type I protein arginine methyltransferases (PRMTs), demonstrating a remarkable capacity to inhibit PRMT1 (IC50 = 3.1 nM) and other isoforms such as PRMT6 and PRMT8. As an uncompetitive inhibitor of S-adenosyl-L-methionine, this compound significantly affects arginine methylation patterns and alters exon usage. GSK3368715 trihydrochloride has shown promising anti-cancer activity, making it a valuable tool for research into the role of PRMTs in disease mechanisms and therapeutic development. -
PRMT5 Inhibitor
PRMT5-IN-4 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), which plays a critical role in tumorigenesis. By blocking PRMT5 activity, this compound exhibits significant anti-tumor effects, making it a valuable tool in cancer research. PRMT5-IN-4 can be utilized in studies investigating the molecular mechanisms of cancer cell proliferation and survival, as well as potential therapeutic strategies targeting PRMT5 in various malignancies. -
DOT1L Inhibitor
Dot1L-IN-6 is a potent inhibitor of the DOT1L enzyme, demonstrating an IC50 value of 0.19 nM. This compound effectively disrupts the function of the telomeric silencing 1-like protein, making it a valuable tool for exploring the role of DOT1L in various biological processes. Researchers can utilize Dot1L-IN-6 in studies related to epigenetics, gene regulation, and the development of therapies for diseases associated with abnormal DOT1L activity. -
EZH2 Inhibitor
PF-06726304 acetate is a selective inhibitor of EZH2, a critical regulator of gene expression involved in epigenetic modifications. It effectively inhibits both wild-type and Y641N mutant forms of EZH2, exhibiting inhibition constants (Kis) of 0.7 nM and 3.0 nM, respectively. This compound demonstrates significant antitumor growth inhibition, making it a valuable tool for cancer research and therapeutic development targeting EZH2-related pathways. -
Histone Methyltransferase Inhibitor
PRMT5-IN-12 is a potent inhibitor of the histone methyltransferase PRMT5, which catalyzes the symmetrical dimethylation of arginine residues on histone proteins. This compound exhibits significant inhibitory activity, making it a valuable tool for investigating the role of PRMT5 in epigenetic regulation and gene expression. Research applications include studies of cancer biology and potential therapeutic strategies targeting PRMT5-mediated pathways. -
PRMT5 Inhibitor
CMP-5 hydrochloride is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating no activity against PRMT1, PRMT4, or PRMT7. This compound effectively blocks the methylation of histone H4 at arginine 3 (S2Me-H4R3) by inhibiting PRMT5 methyltransferase activity. CMP-5 hydrochloride has shown the ability to prevent transformation of EBV-driven B-lymphocytes while sparing normal B cells, making it a valuable tool for research in cancer biology and epigenetic modulation. -
SUV39H2 Inhibitor
OTS186935 trihydrochloride is a potent inhibitor of the protein methyltransferase SUV39H2, with an IC50 of 6.49 nM. This compound demonstrates significant anti-tumor efficacy in mouse xenograft models while exhibiting no detectable toxicity. OTS186935 trihydrochloride is also capable of modulating the production of γ-H2AX, making it a valuable tool for studying DNA damage response mechanisms in cancer research. -
PRMT5 Inhibitor
PRMT5-IN-46 is an inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting inhibitory activity with IC50 values in the range of 1-10 μM. PRMT5 plays a crucial role in methylation processes linked to various genetic alterations. This compound is suitable for research in the contexts of proliferative diseases, metabolic disorders, and hematological conditions. -
PRMT5 Inhibitor
PRMT5-MTA-IN-3 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating potent biological activity with an IC50 of 5 nM in inhibiting cell proliferation within the MTAP-deficient colorectal cancer cell line HCT-116. This compound is particularly relevant for research focused on cancers associated with MTAP deficiencies, including colorectal cancer, non-small cell lung cancer, and pancreatic cancer, making it a valuable tool for cancer biology studies aimed at targeting PRMT5. -
Histone Methyltransferase Inhibitor
PRMT5-IN-48 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 20.7 nM. This compound effectively inhibits the growth of various cancer cell lines while inducing apoptosis and causing cell cycle arrest at the G0/G1 phase. PRMT5-IN-48 is valuable for research focused on non-Hodgkin lymphoma and other malignancies associated with PRMT5 dysregulation. -
EZH2 Degrader
IHMT-EZH2-426 is a potent covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for wild-type EZH2 and 1.2 nM and 1.7-3.5 nM against the mutants EZH2-A687V and EZH2-Y641F/Y641N/Y641S, respectively. This compound effectively reduces levels of H3K27me3 and EZH2, exhibiting significant anti-proliferative activity in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines. It is a valuable tool for research aimed at understanding EZH2's role in oncogenesis and potential therapeutic interventions. -
PRMT5 Inhibitor
PRMT5-MTA-IN-1 is a selective inhibitor of protein arginine methyltransferase PRMT5, targeting its enzymatic activity. This compound effectively inhibits the proliferation of colorectal cancer cells, including HCT116 wildtype and MTAP del mutant strains, with an IC50 of 16 nM and 2.47 μM, respectively. Additionally, PRMT5-MTA-IN-1 shows favorable liver microsomal stability and membrane permeability, indicating potential for in vivo applications. Its promising pharmacokinetic profile was observed in CD-1 mice, supporting further research into its therapeutic efficacy. -
Histone Methyltransferase
Bisegliptin is a small molecule inhibitor targeting histone methyltransferases, primarily recognized for its antidiabetic properties. It undergoes metabolic conversion, predominantly transforming the cyano group into a carboxylic acid form, with DPP-4 contributing to its metabolism. The resultant carboxylic acid metabolite can be detected in both in vivo and in vitro settings. Research indicates that co-administration with other DPP inhibitors influences the plasma concentration of this metabolite, highlighting the complexity of its metabolic dynamics. Additionally, the amide intermediate demonstrates a significantly faster conversion rate than the parent compound in the presence of DPP-4, underscoring its relevance in metabolic studies. -
EZH2/LSD1 Inhibitor
ML234 is a dual inhibitor targeting EZH2 and LSD1, exhibiting IC50 values of 0.09 μM and 0.12 μM, respectively. This compound demonstrates significant antiproliferative effects in prostate cancer cell lines, including LNCAP, PC3, and 22RV1. In vivo studies reveal that ML234 effectively suppresses tumor growth in the 22RV1 xenograft mouse model, making it a valuable tool for research focused on anticancer therapies in prostate cancer. -
PRMT6 Covalent Inhibitor
MS117 is a potent and irreversible covalent inhibitor of protein arginine methyltransferase 6 (PRMT6), demonstrating an IC50 of 18 nM. This compound effectively modulates PRMT6 activity, making it a valuable tool for investigating the role of arginine methylation in various biological processes. MS117 is suitable for research applications focused on epigenetics, gene expression regulation, and potential therapeutic strategies in related diseases. -
Histone Methyltransferase Inhibitor
CARM1-IN-1 is a potent and selective inhibitor of the histone methyltransferase CARM1, with an IC50 value of 8.6 μM and minimal activity against PRMT1 and SET7 (IC50 >667 μM). This compound effectively reduces the methylation activity of CARM1 on various substrates, including PABP1, CA150, SmB, and histone H3. Additionally, CARM1-IN-1 has been shown to suppress the promoter activity of prostate-specific antigen (PSA) while displaying low cytotoxicity, making it a valuable tool for studying epigenetic regulation and prostate cancer biology. -
ASH1L Inhibitor
AS-85 is a potent inhibitor of the ASH1L histone methyltransferase, exhibiting an IC50 value of 0.6 μM. It demonstrates significant anti-leukemic activity through strong binding to the ASH1L SET domain, with a Kd value of 0.78 μM. This compound is useful in research focused on understanding the role of ASH1L in leukemia and other related disorders. -
EZH2 Inhibitor
EZH2-IN-15 is an EZH2 inhibitor that primarily targets the EZH2 methyltransferase enzyme. This compound exhibits notable anti-tumor activity and is applicable in research focused on H3K27me3-dependent tumors. It provides a valuable tool for investigating the role of EZH2 in oncogenesis and may aid in the development of therapeutic strategies targeting specific malignancies. -
EZH2 Inhibitor
ZLD1039 is a highly selective and orally bioavailable inhibitor of the EZH2 enzyme, targeting its role in the polycomb repressive complex 2 (PRC2). This compound demonstrates potent inhibition of PRC2 enzymatic activity against both wild-type and mutant EZH2 variants, with IC50 values of 5.6 nM for wild-type, 15 nM for Y641F, and 4.0 nM for A677G. ZLD1039 has been shown to inhibit breast tumor growth and metastasis, making it a valuable tool for research in cancer biology and therapeutic exploration. -
PRMT7/9 Inhibitor
EML734 is a selective inhibitor of protein arginine methyltransferases PRMT7 and PRMT9, exhibiting IC50 values of 315 nM and 0.89 μM, respectively. This compound is essential for investigating the roles of PRMT7 and PRMT9 in cellular processes, making it valuable for studies related to epigenetics and gene regulation. Researchers can utilize EML734 to better understand the implications of arginine methylation in various biological contexts and disease models. -
G9a/DNMT Inhibitor
CM-579 trihydrochloride is a reversible dual inhibitor targeting G9a and DNMT, demonstrating IC50 values of 16 nM and 32 nM, respectively. This compound exhibits significant in vitro cellular activity across various cancer cell types, making it a valuable tool for epigenetic research and cancer therapeutics. Its ability to modulate histone methylation and DNA methylation positions CM-579 trihydrochloride as a key reagent for studies investigating the role of these enzymes in oncogenesis and potential treatment strategies. -
SUV39H2 Inhibitor
OTS193320 is an imidazo[1,2-a]pyridine compound that acts as a selective inhibitor of the SUV39H2 methyltransferase. It effectively reduces global histone H3 lysine 9 tri-methylation levels in breast cancer cells, leading to apoptosis. Additionally, the combination of OTS193320 with Doxorubicin has been shown to significantly decrease γ-H2AX levels and enhance the reduction in cancer cell viability compared to the use of either compound alone. This makes OTS193320 a valuable tool for understanding the role of histone modifications in cancer therapy. -
DOT1L Inhibitor
Dot1L-IN-5 is a highly potent inhibitor of the telomeric silencing 1-like protein (DOT1L), exhibiting an IC50 of 0.17 nM. This compound is essential for investigating the role of DOT1L in epigenetic regulation and its implications in various cancers and developmental disorders. It serves as a valuable tool for researchers exploring the therapeutic potential of DOT1L modulation in disease models. -
PRMT9 Inhibitor
PRMT9-IN-1 is a selective inhibitor of protein arginine methyltransferase 9 (PRMT9). This compound plays a critical role in the regulation of gene expression and has been linked to various hematological cancers. PRMT9-IN-1 is utilized in research studies to elucidate the mechanisms of action in cancer biology and to explore potential therapeutic strategies targeting PRMT9-mediated pathways. -
G9a/GLP Inhibitor
BIX-01294 trihydrochloride is a reversible and selective inhibitor of G9a and GLP histone methyltransferases, with reported IC50 values of 1.7 μM and 0.9 μM, respectively. It functions by competing for binding at the N-terminal site of substrate lysine residues, thereby inhibiting methylation processes. BIX-01294 trihydrochloride has been shown to induce necroptosis and autophagy, demonstrating antitumor activity particularly in recurrent tumor cells. Its utilization in research may further elucidate the roles of histone methylation in cancer biology and potential therapeutic strategies.
