h3k27me3

MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively.

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3 me2 demethylases JMJD3 KDM6B and UTX KDM6A (IC50=8.6 6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

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

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.

UNC4976 TFA, a positive allosteric modulator (PAM) peptidomimetic of the CBX7 chromodomain, promotes binding to nucleic acids. It concurrently inhibits the H3K27me3-specific recruitment of CBX7 to target genes and enhances non-specific interaction with DNA and RNA [1].

HDM-IN-1 (Compound A4) is an inhibitor of fungal histone demethylase (HDM) that inhibits H3K27me3 in Cryptococcus neoformans and Candida auris, with IC50 values of 134 nM and 12 nM, respectively. It demonstrates inhibitory activity against these fungi by preventing biofilm and capsule formation, with an MIC80 of 0.5-2 μg mL. Additionally, HDM-IN-1 exhibits antifungal activity in ICR mouse models.

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

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.

GSK-J1 lithium salt is an effective inhibitor of H3K27me3 me2-demethylases JMJD3 KDM6B and UTX KDM6A, with an IC 50 of 60 nM for KDM6B.

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

MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM).

PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).

WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.

GSK-J2 sodium, the sodium form of GSK-J2, is an isomer of GSK-J1 and lacks specific activity. GSK-J1 is a potent inhibitor of H3K27me3 me2-demethylases JMJD3 KDM6B and UTX KDM6A [1].

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.

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

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 due to its capacity to diminish H3K27me3 and EZH2 levels [1].