ezh1

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).

Valemetostat (DS-3201) is an EZH1/2 inhibitor that can be used to study relapsed/refractory peripheral T-cell lymphoma.

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

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

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

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.

CPI-169 racemate (CPI 169) is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.

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.

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.

NSD2-IN-6 is a selective inhibitor of NSD2, with an IC50 of 3.8 nM for NSD2 and 274 nM for NSD1. It reduces H3K36me2 levels and reverses cellular plasticity by restoring androgen receptor (AR) signaling pathways. In organoid models, NSD2-IN-6 prompts a transition of cell states from cluster 2 and cluster 3 to cluster 1. In vivo, it exhibits antitumor activity by reversing tumor cell plasticity, inhibiting growth, and promoting apoptosis. NSD2-IN-6 is useful for research in prostate cancer.

EPZ011989 is a highly potent and selective oral EZH2 inhibitor with Ki value <3 nM.

(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.

EPZ005687, a potent and selective inhibitor of EZH2.

HH-2853 is a potent inhibitor targeting EZH1/2, demonstrating significant antitumor activity. Its IC50 values for both wild-type and mutant EZH2 range from 2.21-5.36 nM, comparable to tazemetostat. HH-2853 is more effective against EZH1, with an IC50 of 9.26 nM, notably lower than tazemetostat's 58.43 nM. However, at concentrations up to 10 μM, it exhibits minimal inhibitory activity on 36 types of histone-modifying enzymes. On the cellular level, HH-2853 effectively inhibits mono-, di-, and tri-methylation of H3K27 in various cancer cell lines with wild-type or mutant EZH2, without affecting other methylation types on histone H3 at concentrations up to 10 μM. Additionally, HH-2853 significantly reduces cell viability in multiple cancer cell lines carrying EZH2 GOF mutations or SWI/SNF complex alterations, and demonstrates superior antitumor effects compared to tazemetostat in several tumor xenograft models at equivalent doses.

METTL3-IN-11 is a highly selective METTL3 inhibitor (IC50 = 45.31 nM), demonstrating greater selectivity for METTL3 over DNMT1, EZH1, MLL1, and PRMT1. It reduces m6A levels in total RNA of MOLM-13 and SKOV3 cells, inducing apoptosis and inhibiting migration. METTL3-IN-11 also decreases expression of m6A downstream target genes (c-MYC and BCL2). It is applicable in ovarian cancer and acute myeloid leukemia research.

(R)-OR-S1 is a SAM-competitive, highly selective, orally bioavailable dual inhibitor of EZH1/2.

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. EZH2-IN-14 targets the histone methyltransferase EZH2, inhibiting its trimethylation of histone H3K27. In vitro, EZH2-IN-14 regulates gene expression in cancer cells, inhibits proliferation, and induces apoptosis, making it suitable for studying tumor epigenetic regulatory mechanisms and for potential drug development.