ezh2

PROTAC EZH2 Degrader-1 (Compound 150d), a potent inhibitor, effectively suppresses EZH2 methyltransferase activity, demonstrating an IC50 of 2.7 nM. EZH2 is crucial in various tumorigenesis and development processes [1].

EZH2-IN-5 is a highly effective inhibitor of EZH2, displaying remarkable potency against both wild-type and mutant Tyr641 EZH2, with IC50 values of 1.52 nM and 4.07 nM, respectively.

EZH2-IN-12 (Compound 5) is a potent inhibitor of EZH2, which has potential for studies of CNS malignancies.

EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity.

EZH2-IN-7, a potent inhibitor of EZH2, addresses overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) that cause an abnormal increase in H3K27me3, contributing to the proliferation of various tumors, including breast cancer, prostate cancer, and leukemia. It shows promise for cancer research applications.

PARP/EZH2-IN-1 is a novel compound that functions as a dual inhibitor for both PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for the treatment of triple-negative breast cancer with wild-type BRCA.

EZH2-IN-13 is a potent EZH2 inhibitor with potential anticancer activity.EZH2-IN-13 may be used to study diseases associated with EZH2 activity.

EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.

EZH2-IN-8 is a potent inhibitor of EZH2. EZH2-IN-8 has the potential to be used in the study of cancer diseases.

EZH2-IN-15 is a specific inhibitor of histone modifier enhancer of zeste 2 (EZH2). EZH2 is aberrantly overexpressed in a number of human cancers that controls the adaptive response via regulation of Treg activity. Intratumoral EZH2 expression has also been shown to control the innate immunity

IHMT-EZH2-426 (compound 38) is a potent, covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM for EZH2-Y641F/Y641N/Y641S mutants. The compound effectively inhibits proliferation in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines, attributed to its capacity to diminish H3K27me3 and EZH2 levels [1].

EZH2-IN-3 is an inhibitor of EZH2 and EZH1 with selective impact on diffuse large B cell lymphoma cell growth.

EZH2-IN-14 is a selective inhibitor of EZH2 (Histone Methyltransferase), demonstrating potent inhibition with an IC50 value of 12 nM. It specifically targets the methyltransferase activity of EZH2/PRC2, effectively reducing H3K27me3 levels. Moreover, EZH2-IN-14 exhibits more than 200-fold selectivity for EZH2 over the closely related H3K27 methyltransferase, EZH1.

EZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.

EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activity of EZH2 has been demonstrated in numerous studies in a variety of different cancer types and EZH2-IN-11 has shown research potential for cancer diseases.

EZH2-IN-9 is a potent inhibitor of EZH2, whose overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) cause abnormal elevations in H3K27me3 and contribute to the growth and development of many tumours (e.g. breast cancer, prostate cancer, leukaemia, etc.). EZH2-IN-9 has shown potential for cancer research.

GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).

EI1 (Ezh2 inhibitor) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

(S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, inhibiting EZH2_Y641F with an IC50 of <100 nM.(S)-HH2853 has potential antitumor activity and can be used in the study of autoimmune diseases.

(R)-HH2853 is a potent EZH2 inhibitor with an IC50 <100 nM for EZH2-Y641F.(R)-HH2853 has anticancer and antitumor activity and can be used in autoimmune diseases.

ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis.

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.

UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).

EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.

EPZ005687 is a potent and selective inhibitor of EZH2.

Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity.

GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases.

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].

Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo

Boc-NH-C4-acid is a PROTAC linker belonging to the Alkyl/ether class, which can be used for the synthesis of PROTAC1 and can degrade EED, EZH2, and SUZ12 in PRC2.

MS8815, a selective proteolysis targeting chimera (PROTAC) degrader of enhancer of zeste homolog 2 (EZH2), exhibits inhibitory activity with an IC50 value of 8.6 nM. It is utilized in the research of triple-negative breast cancer (TNBC) [1].

UNC2399, a biotinylated version of UNC1999, functions as a selective degrader of EZH2 and exhibits strong in vitro efficacy against EZH2, demonstrated by its IC 50 value of 17 nM.

Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for therapeutic intervention of atherosclerosis.It possesses a unique anti-cancer activity whose mechani

YM281, a potent EZH2 inhibitor, promotes cell apoptosis and induces cell cycle arrest at the G0/G1 phase, demonstrating antitumor effects in vivo. This compound holds promise for lymphoma research [1].

Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information for designing a new class of potent EZH2 inhibitors. It also possesses the anti-angiogenic act

BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant. It demonstrates potency in inhibiting lymphoma cell proliferation at nanomolar concentrations, proving its utility in anticancer research [1].

GSK926 is a selective, SAM-competitive, and cell-active EZH2 inhibitor.

ZLD10A is a highly potent and selective small molecule inhibitor of EZH2.

MC4343, a potent dual inhibitor targeting both EZH2 and histone deacetylase, presents promising potential for cancer research applications.

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.

DM-01 is a potent and selective inhibitor of EZH2. DM-01 can be used to study diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL) and SNF5/INI-1/SMARCB1 gene-associated solid tumours.

Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor.Tulmimetostat has antitumor activity and is used in the study of ovarian cancer and advanced solid tumors.

DCE_42 is a novel EZH2 inhibitor, it also displays significant anti-proliferation activity against lymphoma cell lines.

Tazemetostat de(methyl morpholine)-COOH (compound 7), a PROTAC ligand for EZH2, facilitates the synthesis of PROTACs that target this enzyme. These EZH2 degraders exhibit potent inhibition of cell viability in diffuse large B-cell lymphoma (DLBCL) and other lymphoma subtypes [1].

GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.

CPI-905 is a potent and selective EZH2 inhibitor with IC50 value of 39.5 nM.