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Results for "

EZH2 methyltransferase activity

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Natural
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147525
    PROTAC EZH2 Degrader-1
    1 Publications Verification

    		 PROTACs Histone Methyltransferase Cancer
    PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .
    PROTAC EZH2 Degrader-1
  • HY-148458
    EZH2-IN-14

    		Histone Methyltransferase Cancer
    EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .
    EZH2-IN-14
  • HY-133129
    MS1943
    1 Publications Verification

    		 PROTACs Histone Methyltransferase Apoptosis Cancer
    MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)) .
    MS1943
  • HY-10442
    3-Deazaneplanocin A
    Maximum Cited Publications
    26 Publications Verification

    DZNep; 3-Deazaneplanocin

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .
    3-Deazaneplanocin A
  • HY-122936
    Tanshindiol C

    		Histone Methyltransferase Keap1-Nrf2 Sirtuin Cardiovascular Disease Cancer
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
    Tanshindiol C
  • HY-12186
    3-Deazaneplanocin A hydrochloride
    Maximum Cited Publications
    26 Publications Verification

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor . 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .
    3-Deazaneplanocin A hydrochloride
  • HY-121093
    DC-S239

    		Histone Methyltransferase Cancer
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .
    DC-S239
  • HY-113786
    EZH2-IN-21

    		Histone Methyltransferase Cancer
    EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates .
    EZH2-IN-21
  • HY-117540
    ZLD10A

    		Histone Methyltransferase Cancer
    ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
    ZLD10A
  • HY-164500
    MC3629

    		Apoptosis Histone Methyltransferase Cancer
    MC3629 is an inhibitor of histone methyltransferase (EZH2) with anti-tumor activity. MC3629 inhibits SHH MB cancer cell proliferation and self-renewal and induces apoptosis. MC3629 can be used to study drug resistance in tumor aggressiveness .
    MC3629
  • HY-117947
    (R)-OR-S1

    		Histone Methyltransferase Cancer
    (R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
    (R)-OR-S1

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