ezh2

EZH2-IN-13, a potent EZH2 inhibitor, exhibits potential anticancer activity and may be utilized to study diseases associated with EZH2 activity.

EZH2-IN-15 (SHR2554) is a specific inhibitor of the zeste 2 histone modification enhancer (EZH2).EZH2 is aberrantly overexpressed in many human cancers and controls adaptive responses by regulating Treg activity. EZH2 expression in tumors has also been shown to control innate immunity.

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.

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

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.

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

PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.

EZH2-IN-17 (compound 28), an orally active and potent inhibitor of EZH2, demonstrates an IC50 value of 0.95 nM. It shows significant anti-proliferation effects on various lymphoma cell lines including WSU-DLCL2, Pfeiffer, and Karpas-422, with IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively [1].

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

HDACs EZH2-IN-1 (Compound 22a) is a dual inhibitor of HDACs and EZH2, exhibiting potent inhibitory activity, with EZH2 Y641N being suppressed by 98% at 50 nM. It selectively targets HDAC1 and HDAC6, with IC50 values of 0.23 μM and 0.07 μM, respectively. HDACs EZH2-IN-1 effectively inhibits the proliferation of diffuse large B-cell lymphoma cells harboring EZH2 mutations and various acute myeloid leukemia cells. Additionally, this compound has the capability to induce cellular differentiation and apoptosis (Apoptosis).

EZH2-IN-18 (compound 9e) serves as a potent inhibitor of enhancer of zeste homologue 2 (EZH2 WT), exhibiting an IC50 of 1.01 nM. It effectively inhibits proliferation and induces apoptosis in tumor cells [1].

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

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

PARP EZH2-IN-1 is a novel dual inhibitor targeting PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for treating triple-negative breast cancer with wild-type BRCA.

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.

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-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-8 is a potent inhibitor of EZH2 with potential applications in cancer disease research.

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-19 (compound N40) is a potent inhibitor of the wild-type enhancer of zeste homolog 2 (EZH2), with an IC50 of 0.32 nM. It plays a significant role in cancer research.

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) with an IC50 value of 12 nM, targeting the methyltransferase activity of EZH2 PRC2 and reducing H3K27me3 levels. It exhibits more than 200-fold selectivity for EZH2 over the closely related H3K27 methyltransferase, EZH1.