Histone Methyltransferase

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

PROTAC EZH2 Degrader-19 is a potent PROTAC compound that targets the enhancing zeste homolog 2 (EZH2) with an IC50 of 15.00 nM. This reagent effectively induces degradation of all Polycomb Repressive Complex 2 (PRC2) subunits, including EZH2, SUZ12, EED, and RbAp48, in a concentration- and time-dependent manner. PROTAC EZH2 Degrader-19 demonstrates significant antiproliferative effects in cancer cell lines, making it a valuable tool for cancer research and therapeutic applications.

PROTAC EZH2 Degrader-34 is a targeted degrader of EZH2, exhibiting an IC50 of 6.30 μM in human EZH2 inhibition. This compound is designed to selectively induce the degradation of EZH2, a key enzyme involved in histone methylation. Its applications are primarily in the study of malignancies such as Pfeiffer and prostate cancer, facilitating investigations into the molecular mechanisms of oncogenesis and potential therapeutic interventions.

PROTAC EZH2 Degrader-11 is a targeted protein degrader designed to selectively degrade the EZH2 protein through a PROTAC mechanism. This compound effectively reduces tumor size and viability in three-dimensional spheroid models, demonstrating potential for cancer research applications. The technology leverages a dual-ligand system, incorporating an EZH2 ligand and a Cereblon ligand, connected by a linker to facilitate the targeted degradation process.

PROTAC EZH2 Degrader-45 is a specialized PROTAC protein degrader designed to target EZH2, exhibiting an IC50 of 22.97 μM in SU-DHL-6 cells. This compound is primarily utilized in research focused on diffuse large B-cell lymphoma, providing insights into epigenetic regulation through targeted protein degradation. The product includes a histone methyltransferase ligand and a VHL ligand, linked for enhanced efficacy in cellular studies.

PROTAC EZH2 Degrader-40 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2), exhibiting an IC50 value of 15.35 μM in SU-DHL-6 cells. This compound is valuable for researching diffuse large B-cell lymphoma and related epigenetic mechanisms. Its structure consists of a histone methyltransferase ligand, an aminopeptidase ligand, and a linker, facilitating targeted degradation of EZH2 to explore therapeutic potential in cancer treatment.

PROTAC EZH2 Degrader-29 is a targeted protein degrader that specifically engages the EZH2 protein, exhibiting an IC50 of 24.53 μM in diffuse large B-cell lymphoma cells. This compound serves as a valuable tool for investigating the degradation of EZH2 in both basic and translational research settings related to diffuse large B-cell lymphoma and other malignancies.