We use analytics and advertising cookies, which you can accept or reject; see our privacy policy.

Current choice:

Histone Methyltransferase

Histone methyltransferase inhibitors target the enzymes that methylate lysine residues on histone tails. Lysine methyltransferases transfer methyl groups from S-adenosylmethionine to defined lysines, most often on histone H3. Methylation of lysine 27 of histone H3 (H3K27) by enhancer of zeste homolog 2 (EZH2) is linked to Polycomb gene silencing, while H3K9 methylation marks heterochromatin. Most compounds here target EZH2, including GSK126, GSK343 and tazemetostat, which compete with S-adenosylmethionine. UNC0642 inhibits G9a and G9a-like protein (GLP), pinometostat targets the H3K79 methyltransferase disruptor of telomeric silencing 1-like (DOT1L), and chaetocin acts on suppressor of variegation 3-9 homolog (SUV39H) enzymes. Inhibitors of arginine-directed enzymes are listed under Protein Arginine Methyltransferases.

Items 51-57 of 57

  • PROTAC EZH2 Degrader-36
    Cat. No.
    A57778
    CAS No.
    2653338-72-6

    PROTAC EZH2 Degrader-36

    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.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC EZH2 Degrader-19
    Cat. No.
    A57779
    CAS No.
    2653338-65-7

    PROTAC EZH2 Degrader-19

    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.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC EZH2 Degrader-34
    Cat. No.
    A57780
    CAS No.
    2653338-71-5

    PROTAC EZH2 Degrader-34

    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.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC EZH2 Degrader-11
    Cat. No.
    A57781
    CAS No.
    2653338-61-3

    PROTAC EZH2 Degrader-11

    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.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC EZH2 Degrader-45
    Cat. No.
    A57782
    CAS No.
    3093642-26-0

    PROTAC EZH2 Degrader-45

    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.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC EZH2 Degrader-40
    Cat. No.
    A57783
    CAS No.
    3093642-40-8

    PROTAC EZH2 Degrader-40

    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.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC EZH2 Degrader-29
    Cat. No.
    A57784
    CAS No.
    3093642-30-6

    PROTAC EZH2 Degrader-29

    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.

    View Details

    Out of stock

    All 3 sizes

Items 51-57 of 57

Added to your cart

View Cart Checkout

    Loading...