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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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. -
WDR5 Degrader
MS33 is a potent WDR5 degrader that functions through E3 ligase VHL-mediated degradation. It exhibits binding affinities of 870 nM for VCB and 120 nM for WDR5, effectively targeting this protein for proteasomal degradation. MS33 is primarily utilized in research related to acute myeloid leukemia, aiding in the understanding of WDR5's role in cancer biology. -
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. -
JMJD1C Inhibitor
JMJD1C-IN-1 is a selective inhibitor of JMJD1C with an IC50 of 0.59 μM and a Kd of 1.96 μM. This compound effectively disrupts the binding of JMJD1C to the H3K9me2 peptide substrate as demonstrated in the HTRF assay, showing an IC50 of 1.47 μM. JMJD1C-IN-1 enhances tumor immunotherapy research by impairing intratumoral regulatory T (Treg) cell fitness through the accumulation of H3K9me2, which downregulates PD1 expression, and by reducing STAT3 demethylation, thereby promoting STAT3 activation. Furthermore, it exhibits dose-dependent antitumor efficacy across various mouse cancer models, including fibrosarcoma, melanoma, lung cancer, hepatocellular carcinoma, and colorectal cancer. -
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. -
HDAC Inhibitor
HDAC-IN-48 is a potent inhibitor of histone deacetylases (HDACs) that exhibits significant cytotoxicity, with a GI50 of approximately 20 nM. This hybrid molecule incorporates pharmacophores from SAHA and CETZOLE, effectively inducing ferroptosis while inhibiting HDAC activity. Additionally, HDAC-IN-48 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications in chemical biology and therapeutic research. -
HDAC11 Inhibitor
HDAC11-IN-3 is a selective inhibitor of HDAC11, exhibiting an IC50 of 4.1 nM. This compound demonstrates potent anti-acute myeloid leukemia (AML) activity against U937 and OCI-AML2 cell lines with an IC50 of 10 μM. It effectively induces apoptosis, cell cycle arrest, and differentiation while upregulating iron transporters transferrin (TF) and transferrin receptor (TFRC). Additionally, HDAC11-IN-3 activates the p62-Keap1-Nrf2-HMOX1 pathway, resulting in elevated intracellular iron levels and subsequent ferroptosis in AML cells. This reagent is suited for studies investigating the molecular mechanisms of AML and can be utilized alone or in combination with other therapeutic agents like Cytarabine. -
LSD1 Inhibitor
Higenamine hydrochloride is a selective inhibitor of LSD1, with an IC50 value of 1.47 μM. This compound exhibits anti-inflammatory and antibacterial properties, and has been shown to attenuate IL-1β-induced apoptosis via the ROS-mediated PI3K/Akt signaling pathway. Additionally, Higenamine hydrochloride protects brain cells from oxygen deprivation and promotes bone formation in osteoporosis through the SMAD2/3 pathway. Its versatile applications make it suitable for research in cancer, inflammation, cardiorenal syndrome, and related diseases. -
SIRT1/2 Inhibitor
Sirt1/2-IN-1 is a selective inhibitor of SIRT1 and SIRT2, exhibiting IC50 values of 1.81 and 2.10 µg/mL, respectively, while also inhibiting SIRT3 with an IC50 of 20.5 µg/mL. This compound induces hyperacetylation of α-tubulin, with an IC50 of 32.05 µg/mL, demonstrating its potential for modulating protein acetylation. Sirt1/2-IN-1 is particularly relevant in cancer research, showcasing significant anticancer activity that supports its use in investigating therapeutic strategies targeting sirtuin pathways. -
HDAC Inhibitor
HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma. -
Naa50 Inhibitor
Naa50-IN-1 is a potent inhibitor of N-alpha-acetyltransferase 50 (Naa50), exhibiting an IC50 of 7 nM against the human enzyme. This compound shows selectivity for related acetyltransferases, Naa10 and Naa60. Naa50-IN-1 interacts with the substrate-binding pocket of Naa50, with its binding affinity augmented by the presence of AcCoA, making it a valuable tool for investigating the biological roles of protein acetylation. Research applications include studies on gene regulation and enzyme activity related to Naa50 and its substrates. -
EZH2 Inhibitor
TDI-6118 is a potent inhibitor of the histone methyltransferase EZH2, known for its ability to penetrate the blood-brain barrier. This compound exhibits significant biological activity in targeting EZH2, making it a valuable tool for investigating central nervous system malignancies. Its application in research may contribute to a better understanding of the molecular mechanisms underlying various brain cancers. -
CARM1/HDAC2 inhibitor
CARM1/HDAC2-IN-1 is a dual inhibitor targeting both CARM1 and HDAC2, exhibiting IC50 values of 3.71 nM and 4.07 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. CARM1/HDAC2-IN-1 is suitable for studies investigating the role of these epigenetic regulators in tumor biology and therapeutic strategies. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-12 is a CRBN-recruiting PROTAC designed to selectively degrade the EZH2 protein, exhibiting an IC50 of 3.90 nM for EZH2 and an IC50 of 5.24 μM for EZH1. This compound facilitates targeted protein degradation, making it a valuable tool for research focused on epigenetic regulation and cancer biology. Its ability to modulate the expression of key oncogenic factors positions it as a significant reagent for therapeutic investigations targeting EZH2-dependent pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-24 is an innovative molecule designed to target EZH2 by utilizing a PROTAC-mediated degradation mechanism. This compound exhibits potent EZH2 methyltransferase inhibitory activity, facilitating the selective degradation of the EZH2 protein. Research applications include studies on epigenetic regulation and therapeutic strategies for cancers with aberrant EZH2 activity. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-30 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2) with an IC50 of 6.22 μM in SU-DHL-6 cells. This compound is instrumental in research applications focusing on diffuse large B-cell lymphoma by promoting the degradation of EZH2 and thereby modulating epigenetic regulation. The inclusion of ligands for both EZH2 and MDM2, coupled with a linker, facilitates targeted protein degradation and offers a valuable tool for investigating therapeutic strategies in cancer biology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-43 is a targeted PROTAC protein degrader that specifically degrades the EZH2 protein, exhibiting an IC50 of 21.73 μM in SU-DHL-6 cells. This compound is valuable for investigating the role of EZH2 in lymphoma research and understanding its mechanistic function in histone methylation. The dual ligand design incorporates a histone methyltransferase ligand and a VHL ligand, promoting efficient substrate recognition and recruitment for proteasomal degradation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-17 is a selective protein degrader that targets the enhancer of zeste homolog 2 (EZH2). This compound demonstrates significant antiproliferative activity, with an IC50 of 18.32 μM in lymphoma cell lines. PROTAC EZH2 Degrader-17 is a valuable tool for investigating EZH2-related pathologies and provides insights into the therapeutic potential of protein degradation in cancer research. -
EZH2 Ligand
EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies. -
EZH2 PROTAC
PROTAC EZH2 Degrader-26 is a targeted proteolysis-targeting chimera (PROTAC) designed to specifically degradation of the enhancer of zeste homolog 2 (EZH2). This compound demonstrates a potent inhibitory activity with an IC50 of 5.80 nM against EZH2, alongside micromolar-level activity against EZH1, with an IC50 of 0.06 μM. PROTAC EZH2 Degrader-26 is suitable for research applications involving epigenetic regulation, cancer biology, and studies aimed at understanding histone methylation processes. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-39 is a targeted PROTAC that effectively degrades the EZH2 protein, exhibiting an IC50 of 61.00 nM. This compound functionally inhibits the methyltransferase activity of EZH2, making it an important tool for studying the biological implications of EZH2 modulation. Its applications include cancer research and epigenetic regulation studies, contributing to advancements in targeted therapy development. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-15 is a targeted degrader that specifically interacts with the EZH2 protein via a proteolysis-targeting chimera (PROTAC) mechanism. This compound effectively inhibits the methyltransferase activity of EZH2, leading to its degradation and resulting in alterations to histone methylation patterns. It serves as a valuable tool for research applications focused on epigenetic regulation, cancer biology, and therapeutic strategies aimed at EZH2 modulated pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-10 is a Proteolysis Targeting Chimeras (PROTAC) compound designed to selectively degrade the enhancer of zeste homolog 2 (EZH2). By facilitating the ubiquitination and subsequent proteasomal degradation of EZH2, this compound exhibits potential as an innovative therapeutic approach for cancer research. Its mechanism involves a specific ligand for EZH2 and a cereblon ligand, linked together to enhance degradation efficiency, making it a valuable tool for investigating EZH2-related oncogenic pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-35 is a proteolysis-targeting chimera (PROTAC) specifically designed to degrade the Enhancer of Zeste Homolog 2 (EZH2) protein, exhibiting a binding affinity (Ka) of 16.19 nM. This compound demonstrates significant antiproliferative activity against triple-negative breast cancer cells while maintaining minimal cytotoxicity toward normal human epithelial, hepatic, and renal cells. PROTAC EZH2 Degrader-35 is a valuable tool for studying the role of EZH2 in cancer biology and has potential applications in therapeutic research focused on triple-negative breast cancer. -
EZH2 PROTAC
PROTAC EZH2 Degrader-27 is a potent EZH2 PROTAC inhibitor with an IC50 of 4.00 nM, specifically designed to target the SET domain of the EZH2 methyltransferase. By engaging in targeted protein degradation, this compound effectively inhibits methyltransferase activity, leading to downregulation of histone methylation. Research applications include studies on epigenetic regulation and potential therapeutic strategies targeting EZH2 in various cancers. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-13 is a targeted proteolysis-targeting chimera (PROTAC) designed to selectively degrade Enhancer of Zeste Homolog 2 (EZH2) with an IC50 of 2.70 nM. This compound exhibits potent antiproliferative effects in various cancer cell lines, making it a valuable tool in cancer research. PROTAC EZH2 Degrader-13 facilitates investigations into the role of EZH2 in tumorigenesis and therapeutic resistance, providing insights for the development of innovative cancer treatments. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-23 is a targeted protein degradant that specifically degrades EZH2 through a PROTAC mechanism. It acts by inhibiting the methyltransferase activity of EZH2 via binding to the SET domain, exhibiting a target IC50 of 30.00 nM. This compound is valuable for research applications focused on the modulation of gene silencing pathways and the exploration of EZH2's role in cancer biology. -
PRMT5/MEP50 complex Degrader
MS115 is a selective degrader targeting the PRMT5/MEP50 complex, demonstrating DC50 values of 17.4 nM and 11.3 nM for PRMT5 at 24 hours in MDAMB468 breast cancer cells. This compound effectively inhibits the proliferation of breast cancer cells, making it a valuable tool for studying PRMT5-mediated pathways and evaluating therapeutic strategies in cancer research. MS115's unique mechanism positions it as a significant reagent for investigating the roles of epigenetic regulators in tumor biology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-37 is a PROTAC compound designed to induce the degradation of the EZH2 protein, exhibiting a target IC50 of 144 nM. This reagent is valuable for research related to lymphomas and other conditions where dysregulation of histone methylation is implicated. Its mechanism harnesses the cellular degradation pathway, providing a potent tool for studying EZH2-dependent biological processes and developing therapeutic strategies against EZH2-driven malignancies. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-28 is a targeted PROTAC protein degrader designed to selectively degrade the EZH2 enzyme, demonstrating an IC50 of 16.2 μM in diffuse large B-cell lymphoma (DLBCL) cell lines. This compound is valuable for studying the role of EZH2 in lymphoma biology and therapeutic interventions. Its dual-ligand structure combines an EZH2 ligand with a VHL ligand, facilitating targeted protein degradation for advancing cancer research. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-20 is a small-molecule degrader specifically designed to target the EZH2 protein, utilizing the proteolysis targeting chimera (PROTAC) mechanism. It demonstrates potent antiproliferative effects with an IC50 of approximately 10 μM in lymphoma cell lines. This compound is ideal for research focused on understanding the role of EZH2 in lymphoma and exploring new therapeutic approaches for this malignancy. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-25 is a proteolysis-targeting chimera (PROTAC) designed to specifically degrade the EZH2 protein through targeted ubiquitination and proteasomal degradation. This compound is valuable for investigating the role of EZH2 in various lymphoma types, facilitating studies on its contribution to tumorigenesis. In addition, it illustrates the potential of PROTAC technology in modulating epigenetic regulators for therapeutic applications. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-16 is a targeted PROTAC protein degrader that specifically induces the degradation of EZH2, exhibiting an IC50 of 13.74 μM in SU-DHL-6 cells. This compound demonstrates significant antiproliferative activity against diffuse large B-cell lymphoma (DLBCL) cells, making it valuable for research focused on DLBCL. Its unique design incorporates a histone methyltransferase ligand and a Cereblon ligand linked via a proprietary linker, facilitating targeted degradation for therapeutic exploration. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-31 is a targeted protein degrader that effectively interacts with EZH2, promoting its degradation through the use of a PROTAC strategy. This compound demonstrates potent antiproliferative activity, with IC50 values of 3.63 μM in lSU-DHL-6 cells and 8.74 μM in HBL-1 cells. It is valuable for research focused on lymphoma, offering insights into EZH2-mediated pathways and potential therapeutic interventions. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-14 is an EZH2-targeting PROTAC degrader that selectively induces degradation of the EZH2 protein. With an IC50 of 18.21 μM, it effectively targets diffuse large B-cell lymphoma cells while showing no antiproliferative effects on non-target cells at concentrations up to 30.00 μM. This compound is valuable for research focused on the role of EZH2 in diffuse large B-cell lymphoma and provides a tool for exploring novel therapeutic strategies in oncology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-22 is a PROTAC (Proteolysis Targeting Chimera) designed to target and degrade the EZH2 protein. This compound effectively modulates EZH2 activity, leading to the inhibition of histone methylation and promoting cancer cell apoptosis. It is particularly valuable in cancer-related research, facilitating the study of epigenetic regulation and therapeutic interventions. -
DOT1L Inhibitor，PROTAC
DOT1L705 is a PROTAC degrader that selectively targets DOT1L, facilitating the recruitment of the VHL E3 ubiquitin ligase for proteasomal degradation of the protein. This leads to a significant reduction in H3K79 methylation levels, ultimately decreasing the viability of leukemia cells. DOT1L705 is particularly relevant for research focused on MLL-rearranged leukemia, making it a valuable tool for investigating the underlying mechanisms of disease progression. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-42 is a targeted degrader that specifically induces degradation of EZH2, a histone methyltransferase, via cIAP-mediated ubiquitination and subsequent proteasomal pathway. This compound exhibits antiproliferative activity and is particularly useful in the study of lymphoma. By modulating EZH2 levels, it provides a valuable tool for investigating epigenetic regulation and related therapeutic strategies in cancer research. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-36 is a targeted PROTAC designed to degrade the EZH2 protein, exhibiting a target IC50 of 16.00 nM. This compound is particularly relevant for research applications related to lymphoma, leveraging the selective degradation of EZH2 to investigate its role in cancer progression. The molecule consists of a histone methyltransferase ligand, a Cereblon ligand, and a linker, facilitating the ubiquitin-proteasome pathway for protein elimination.
