Epigenetics
Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.
- DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
- HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
- Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
- RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
- Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.
Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.
3 key components involved in the regulation of epigenetic modifications
Epigenetics Writer
Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).
Epigenetics Reader
Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.
Epigenetics Eraser
Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.
Catalog No.
Product Name
Application
Product Information
Citations
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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. -
SIRT1 Activator
BML-278 is a potent SIRT1 activator with an effective concentration (EC150) of 1 μM. It enhances histone modifications by increasing H3K9 methylation and inhibiting H3K9 acetylation, which contributes to improved early embryonic development. Additionally, BML-278 induces G1/S phase cell cycle arrest and reduces senescence in primary human mesenchymal cells. In U937 cells, this compound reduces tubulin acetylation while promoting increased mitochondrial density in murine C2C12 myoblasts, highlighting its versatility in cellular and developmental research applications. -
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. -
PRMT5 Inhibitor
PR5-LL-CM01 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 7.5 μM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. It can be employed to explore the role of PRMT5 in tumorigenesis and may aid in the development of targeted therapies. -
PRMT5 Inhibitor
PRMT5-IN-30 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), with an IC50 of 0.33 μM and a Kd of 0.987 μM. This compound demonstrates broad selectivity against various other methyltransferases, making it a valuable tool in biochemical research. PRMT5-IN-30 effectively inhibits the methylation of SmD3 mediated by PRMT5, providing a means to study the functional roles of PRMT5 in cellular processes and disease pathways. -
G9a/GLP Inhibitor
MS8511 hydrochloride is a selective irreversible inhibitor of G9a and GLP, targeting cysteine residues within the substrate binding site. It exhibits IC50 values of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM and 46 nM, respectively. MS8511 hydrochloride effectively reduces cellular H3K9me2 levels and enhances antiproliferative activity. This compound is applicable in cancer research, particularly in studies involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as in investigations of neurodegenerative diseases such as Alzheimer’s disease and genetic disorders like Prader−Willi syndrome. -
PRMT7 Inhibitor
PRMT7-IN-1 is a selective inhibitor of protein arginine methyltransferase 7 (PRMT7), exhibiting an IC50 value of 2.1 μM. This compound demonstrates significant anticancer activity against various cancer cell lines, making it a valuable tool for studies on PRMT7's role in cancer biology. Its application extends to investigating PRMT7-mediated signaling pathways and potential therapeutic strategies in oncology. -
EZH2 Inhibitor
EZH2-IN-13 is a potent inhibitor of the Enhancer of Zeste Homolog 2 (EZH2), a critical regulator of gene expression involved in epigenetic modification. This compound is primarily utilized in research applications focused on cancers and precancerous lesions that exhibit aberrant EZH2 activity. Investigating EZH2-IN-13 can provide insights into the role of EZH2 in tumorigenesis and potential therapeutic strategies for EZH2-dependent malignancies. -
PRMT5:MEP50 PPI Inhibitor
PRMT5:MEP50 PPI inhibitor is designed to target and disrupt the interaction between PRMT5 and MEP50, key components in cellular signaling pathways. This compound exhibits significant anti-tumor and anti-proliferative effects on lung and prostate cancer cells. Its application in cancer research aids in understanding the role of methyltransferase complexes in tumorigenesis. -
HOTAIR-EZH2 Inhibitor
AC1Q3QWB is an inhibitor of the HOTAIR-EZH2 interaction, which leads to the upregulation of CDKN1A and SOX17. This compound enhances the efficacy of Tazemetostat in the context of endometrial cancer, making it a valuable tool for researchers investigating therapeutic strategies targeting the EZH2 pathway. Its role in modulating gene expression through disruption of oncogenic interactions supports its application in cancer research. -
Histone Methyltransferase Inhibitor
EED ligand 1 is a selective inhibitor of the EED subunit of the polycomb repressive complex 2 (PRC2), a histone methyltransferase. It exhibits potent efficacy in disrupting PRC2-mediated methylation processes, making it valuable for studies investigating gene expression regulation and epigenetic modifications. This compound is applicable in research on cancer biology, developmental processes, and therapeutic approaches targeting PRC2 activity. -
G9a/ GLP Inhibitor
MS8511 is a selective, irreversible inhibitor of G9a and GLP that covalently targets a cysteine residue within the substrate binding site. It demonstrates IC50 values of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM and 46 nM, respectively. MS8511 effectively decreases cellular levels of H3K9me2 and enhances antiproliferative activity, making it a valuable tool for researching various cancers, including brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as conditions such as Alzheimer’s disease, sickle cell disease, and Prader−Willi syndrome. -
SMYD2 Inhibitor
AZ506 is a potent inhibitor of the methyltransferase enzyme SMYD2, exhibiting an IC50 of 17 nM. By targeting SMYD2, AZ506 effectively reduces SMYD2-mediated methylation within cellular environments. This compound is suitable for research applications focused on elucidating the role of SMYD2 in various disease pathways and exploring its potential as a therapeutic target. -
PRMT6 Inhibitor
PRMT6-IN-3 is a selective inhibitor of protein arginine methyltransferase 6 (PRMT6), exhibiting an IC50 value of 192 nM. This compound has been shown to induce apoptosis in various cancer cell lines, highlighting its potential as an anticancer agent. PRMT6-IN-3 is a valuable tool for research applications focused on understanding PRMT6's role in tumor biology and exploring novel cancer therapeutic strategies. -
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.
