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.

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).

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.

(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.

(2R,4S)-Azalanstat (Iso-Azalansta) is a selective heme oxygenase (HO) inhibitor that is used in the study of cardiovascular disease.

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

EPZ005687, a potent and selective inhibitor of EZH2.

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

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

3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.

3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.

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.

JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 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

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.

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-22 (example 92) is a potent EZH2 inhibitor, exhibiting IC50 values of <0.00051 µM for EZH2(Y641N) and EZH2(Y641F), and 0.00052 µM for EZH2 (wt). Additionally, EZH2-IN-22 demonstrates antiproliferative activity.

CDK9/EZH2-IN-1 is a dual-target inhibitor of CDK9 and EZH2 with IC50 values of 83.9 nM and 108.6 nM, respectively. It induces apoptosis and causes DNA double-strand breaks (DSB). Additionally, CDK9/EZH2-IN-1 inhibits the proliferation of MKN45, MDA-MB-453, and SW620 cancer cells, with respective IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM.

EZH2/HSP90-IN-29 is a potent dual inhibitor of EZH2 and HSP90, with IC50 values of 6.29 nM and 60.1 nM, respectively. It induces cell cycle arrest at the M phase, promotes the expression of genes related to apoptosis/necrosis, and inhibits reactive oxygen species (ROS) catabolism. This compound can cross the blood-brain barrier, making it a promising and easily manageable candidate for glioblastoma (GBM) research.

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

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.