Histone Methyltransferase

Cat. No.

A23910

CAS No.

2225938-17-8

MS1943

MS1943 is an orally active, PROTAC-based selective degrader of EZH2 that effectively reduces cellular EZH2 levels. It exhibits strong anticancer activity, showing cytotoxic effects in various triple-negative breast cancer (TNBC) cell lines while sparing normal cells. MS1943 maintains high potency in inhibiting EZH2 methyltransferase activity (IC₅₀ = 120 nM) and demonstrates high selectivity for EZH2, making it a promising candidate for epigenetic and cancer research.

Cat. No.

A23911

CAS No.

2225938-86-1

MS177

MS177 is a fast-acting and effective PROTAC degrader targeting EZH2. It comprises a cereblon (CRBN) ligand, a linker, and the potent EZH2 enzymatic inhibitor C24 (IC₅₀: 12 nM). MS177 efficiently depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes, leading to inhibition of leukemia cell proliferation, induction of apoptosis, and cell cycle arrest. It is a valuable tool for epigenetic and cancer research.

Cat. No.

A23940

CAS No.

2641601-67-2

PROTAC EZH2 Degrader-1

PROTAC EZH2 Degrader-1 (Compound 150d) is a potent PROTAC molecule targeting EZH2, with an IC₅₀ of 2.7 nM for inhibition of its methyltransferase activity. By degrading EZH2, it provides a valuable tool for studying its role in tumorigenesis and cancer progression.

Cat. No.

A23944

CAS No.

2688842-08-0

UNC6852

UNC6852 is a selective PROTAC degrader of the polycomb repressive complex 2 (PRC2), incorporating ligands for EED (embryonic ectoderm development) and von Hippel-Lindau (VHL). It targets EED with an IC₅₀ of 247 nM, enabling PRC2 degradation and serving as a valuable tool for epigenetic and cancer research.

Cat. No.

A23964

CAS No.

3061315-33-8

LLC0424

LLC0424 is a potent and selective cereblon-based PROTAC that targets NSD2 for degradation. It induces NSD2 degradation in a cereblon- and proteasome-dependent manner, with a DC₅₀ of 20 nM in RPMI-8402 cells.

Cat. No.

A23982

CAS No.

3093642-32-8

PROTAC EZH2 Degrader-2

PROTAC EZH2 Degrader-2 (Compound E-3P-MDM2) is a PROTAC molecule designed by linking the EZH2 inhibitor Tazemetostat (EPZ6438) to an E3 ligase ligand. It induces dose-dependent degradation of EZH2 in SU-DHL-6 cells, suppresses H3K27me3 expression, and concurrently degrades PRC2 components EED and SUZ12 without altering their mRNA levels. PROTAC EZH2 Degrader-2 exhibits strong anti-cancer and anti-proliferative activity, making it a valuable tool for epigenetic and oncology research.

Cat. No.

A23985

MS9715

MS9715 is a potent and selective PROTAC degrader targeting NSD3, designed by conjugating the NSD3 PWWP1 domain binder BI-9321 to a von Hippel-Lindau (VHL) E3 ligase ligand. It effectively induces degradation of NSD3 and holds significant potential for research in NSD3-dependent cancers, offering a novel approach to target epigenetic drivers in oncology.

Cat. No.

A23986

CAS No.

3037165-65-1

MS181

MS181 (Compound 1) is a potent PROTAC degrader that targets components of the polycomb repressive complex 1 (PRC1) by recruiting cereblon (CRBN) and binding EED. It effectively reduces the expression of key PRC1 and PRC2 components, including EED, EZH2, SUZ12, BMI1, and RING1B. MS181 exhibits significant antiproliferative activity, making it a valuable tool for studying epigenetic regulation and potential cancer therapeutics.

Cat. No.

A23999

CAS No.

3060730-06-2

MS8709

MS8709 (compound 10) is a first-in-class PROTAC degrader targeting the histone methyltransferases G9a and GLP, with potential anticancer activity. Engineered from the G9a/GLP inhibitor UNC0642, MS8709 recruits the von Hippel–Lindau (VHL) E3 ubiquitin ligase to promote the selective ubiquitination and proteasomal degradation of G9a/GLP proteins. This targeted degradation approach offers a novel therapeutic strategy for disrupting epigenetic dysregulation in cancer.

Cat. No.

A24332

CAS No.

2929304-60-7

UNC8153

UNC8153 is a potent and selective degrader targeting nuclear receptor-binding SET domain-containing protein 2 (NSD2), with a binding affinity (Kd) of 24 nM. It induces proteasome-dependent degradation of NSD2 by incorporating a simple warhead, leading to a reduction in both NSD2 protein levels and the associated H3K36me2 chromatin mark in cells. UNC8153 is a valuable chemical tool for investigating NSD2 function and epigenetic regulation.

Cat. No.

A24692

CAS No.

2855085-25-3

MS8815

MS8815 is a selective enhancer of the enhancer of zeste homolog 2 (EZH2) and functions as a PROTAC degrader. With an IC50 value of 8.6 nM, MS8815 demonstrates potent inhibitory activity against EZH2. This compound is valuable for research applications focused on triple-negative breast cancer (TNBC) and other conditions influenced by EZH2 activity.

Cat. No.

A24699

CAS No.

2375432-47-4

MS4322

Synonyms: YS43-22

MS4322 is a selective PROTAC degrader targeting PRMT5, effectively reducing PRMT5 protein levels in MCF-7 cells with a DC50 of 1.1 μM. This compound inhibits the methyltransferase activity of PRMT5, exhibiting an IC50 value of 18 nM. MS4322 facilitates the ubiquitination and subsequent degradation of PRMT5, making it a valuable tool for research into breast cancer, lung cancer, and hepatocellular cancer.

Cat. No.

A24732

CAS No.

3004503-12-9

NUCC-0226272

NUCC-0226272 is a potent PROTAC that facilitates the targeted degradation of EZH2. This compound exhibits significant anti-proliferative effects, making it a valuable tool for investigating the role of EZH2 in cancer biology. Its application in cancer research provides insights into potential therapeutic strategies for malignancies associated with EZH2 dysregulation.

Cat. No.

A24819

CAS No.

2601727-80-2

MS4322 (isomer)

Synonyms: YS43-22 (isomer)

MS4322 (isomer) is a specific degrader of the protein arginine methyltransferase 5 (PRMT5), exhibiting a DC50 of 1.1 μM for reducing PRMT5 protein levels in MCF-7 cells. It inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM, facilitating ubiquitination and subsequent degradation of the target protein. This reagent is valuable for researching breast cancer, lung cancer, and hepatocellular carcinoma, allowing for exploration of PRMT5's role in tumorigenesis.

Cat. No.

A24828

CAS No.

3050872-59-5

MS8847

MS8847 is a powerful EZH2 PROTAC degrader that utilizes the E3 ligase von Hippel-Lindau (VHL) to promote the degradation of EZH2 through the ubiquitin-proteasome system. This compound demonstrates robust anti-proliferative effects in acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cell lines. MS8847 serves as a valuable tool for investigating the role of EZH2 in oncogenic signaling pathways and developing targeted therapies for EZH2-dependent malignancies.

Cat. No.

A24851

CAS No.

2639882-69-0

PROTAC EED degrader-2

PROTAC EED Degrader-2 is a von Hippel-Lindau-based PROTAC that selectively targets the embryonic ectoderm development (EED) subunit of the polycomb repressive complex 2 (PRC2), exhibiting a pKD of 9.27. This compound acts as an effective inhibitor, demonstrating a pIC50 of 8.11, facilitating the degradation of EED and providing valuable insights for research on PRC2-related epigenetic regulation and its implications in various biological processes. Applications include studies on gene expression regulation and potential therapeutic targets in cancer and developmental biology.

Cat. No.

A24859

CAS No.

2639882-72-5

PROTAC EED degrader-1

PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC that selectively targets EED with a pKD of 9.02. This compound functions as a polycomb repressive complex 2 (PRC2) inhibitor, exhibiting an inhibitory potency characterized by a pIC50 of 8.17. It serves as a valuable tool for researching the modulation of PRC2 activity and its implications in cancer biology and epigenetic regulation.

Cat. No.

A26609

CAS No.

3098718-46-5

PROTAC EZH2 Degrader-3

PROTAC EZH2 Degrader-3 (compound ZJ-20) specifically targets and degrades the EZH2 protein through a proteolysis-targeting chimera (PROTAC) mechanism. This compound demonstrates potent inhibition of EZH2 expression as well as a significant reduction in other PRC2 subunits and H3K27me3 levels. Additionally, PROTAC EZH2 Degrader-3 exhibits anti-proliferative effects, inducing cell cycle arrest in the G0-G1 phase and promoting apoptosis in cancer cells, making it valuable for research in cancer therapeutics and epigenetic regulation.

Cat. No.

A26611

CAS No.

2978620-84-5

PROTAC EZH2 Degrader-9

PROTAC EZH2 Degrader-9 is an orally active PROTAC that selectively degrades EZH2 via the ubiquitin-proteasome pathway. By downregulating PRC2 core subunits and inhibiting H3K27me3, it effectively reverses PRC2-mediated gene silencing and disrupts EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 demonstrates potent antiproliferative effects on various cancer cell lines, inducing cell cycle arrest and apoptosis. This reagent is valuable for research focused on leukemia, lymphoma, and non-small cell lung cancer.

Cat. No.

A26621

CAS No.

3032785-06-8

CARM1 degrader-2

CARM1 degrader-2 is a potent PROTAC that specifically targets co-activator associated arginine methyltransferase (CARM1) for degradation, exhibiting a DC50 of 8.8 nM. This compound facilitates the degradation of CARM1 through a VHL- and proteasome-dependent mechanism, leading to the inhibition of methylation of key substrates such as poly(A)-binding protein PABP1 and BAF155. Its ability to inhibit CARM1 function makes CARM1 degrader-2 a valuable tool in breast cancer research, particularly in studies focused on cancer cell migration.

Cat. No.

A26638

CAS No.

2855085-26-4

MS8815N

MS8815N serves as a negative control for the EZH2 PROTAC degrader MS8815, designed to lack the ability to recruit the VHL E3 ligase while preserving the EZH2 binding moiety and linker structure. This compound is particularly useful in research related to triple-negative breast cancer (TNBC), providing a reliable tool for elucidating the mechanisms of PROTAC-mediated degradation in experimental settings. Its application aids in validating the specificity and effectiveness of EZH2-targeted degradation strategies.

Cat. No.

A26724

CAS No.

3065966-31-3

SKLB-0124

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.

Cat. No.

A26737

CAS No.

3018914-66-1

IHMT-EZH2-426

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.

Cat. No.

A29009

CAS No.

3093642-25-9

PROTAC EZH2 Degrader-44

PROTAC EZH2 Degrader-44 is a selective degrader targeting the EZH2-PRC2 complex through the recruitment of the CRBN E3 ligase, facilitating proteasome-mediated degradation of EZH2, SUZ12, and EED. This process leads to a marked reduction in H3K27me3 and CARM1 levels, resulting in potent antiproliferative effects. It induces mitochondrial dysfunction and promotes apoptosis by modulating Bcl-2 family proteins, demonstrating minimal cytotoxicity in normal human mammary epithelial, liver, and kidney cells. PROTAC EZH2 Degrader-44 serves as an effective research tool for investigating targeted therapies in triple-negative breast cancer.

Cat. No.

A53787

CAS No.

3093642-41-9

PROTAC EZH2 Degrader-41

PROTAC EZH2 Degrader-41 is a PROTAC designed to target EZH2 by recruiting cIAP E3 ubiquitin ligase. This compound facilitates the ubiquitination and subsequent proteasomal degradation of EZH2, thereby exerting significant antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 is a valuable tool for investigating the role of EZH2 in lymphoma research and its potential as a therapeutic target.