EZH1

EZH1 is a PRC2 catalytic homolog that methylates histone H3 lysine 27 and supports transcriptional repression in chromatin regulation^[1]. Mechanistically, EZH1 colocalizes with H3K27me3 and preserves this mark on development-related genes when EZH2 is absent, linking EZH1 to embryonic stem cell identity and pluripotency execution^[1]. In adult models, EZH1 maintains hematopoietic stem cells in a slow-cycling, undifferentiated state and protects them from senescence-like cell-cycle arrest^[2]. Compared with EZH2, EZH1 forms similar PRC2 complexes but represses chromatin through a distinct mechanism, because PRC2-EZH2 strongly catalyzes H3K27me2/3 whereas PRC2-EZH1 more directly compacts chromatin^[3]. Functional redundancy is context-dependent, as EZH1 and EZH2 jointly sustain H3K27 trimethylation in mouse skin, where double targeting abolishes H3K27me3 and disrupts hair follicle homeostasis and wound repair^[4]. In cancer research, EZH1/2 dual inhibitors provide experimental tools to test whether simultaneous EZH1 and EZH2 blockade suppresses H3K27me3 more effectively than EZH2-selective inhibition^[5]. Valemetostat studies further support EZH1/2 inhibition as a translational model in relapsed or refractory adult T-cell leukemia/lymphoma^[6].

References:

[1]. Shen X, et al. EZH1 mediates methylation on histone H3 lysine 27 and complements EZH2 in maintaining stem cell identity and executing pluripotency. Mol Cell. 2008 Nov 21;32(4):491-502. [Content Brief]

[2]. Hidalgo I, et al. Ezh1 is required for hematopoietic stem cell maintenance and prevents senescence-like cell cycle arrest. Cell Stem Cell. 2012 Nov 2;11(5):649-62. [Content Brief]

[3]. Margueron R, et al. Ezh1 and Ezh2 maintain repressive chromatin through different mechanisms. Mol Cell. 2008 Nov 21;32(4):503-18. [Content Brief]

[4]. Ezhkova E, et al. EZH1 and EZH2 cogovern histone H3K27 trimethylation and are essential for hair follicle homeostasis and wound repair. Genes Dev. 2011 Mar 1;25(5):485-98. [Content Brief]

[5]. Sato T, et al. c-Jun N-terminal kinase in pancreatic tumor stroma augments tumor development in mice. Cancer Sci. 2017 Nov;108(11):2156-2165. [Content Brief]

[6]. Izutsu K, et al. An open-label, single-arm phase 2 trial of valemetostat for relapsed or refractory adult T-cell leukemia/lymphoma. Blood. 2023 Mar 9;141(10):1159-1168. [Content Brief]

EZH1 Related Products (10):

By Type:	Selective (2)
By Effects:	Inhibitors (6) Degraders (3)

Cat. No.	Product Name	Effect	Purity

HY-109108

Valemetostat	Inhibitor	99.84%
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

HY-15646

UNC1999	Inhibitor	99.87%
UNC1999, a chemical probe, is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC₅₀s of <10 nM and 45 nM, repectively.

HY-109108A

Valemetostat tosylate	Inhibitor	99.84%
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

HY-145602

Tulmimetostat	Inhibitor	99.79%
Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies.

HY-141877

MS4322	Degrader	99.14%
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC₅₀ of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC₅₀ of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).

HY-180553

NSD2-IN-6	Inhibitor
NSD2-IN-6 is a selective and orally active ^NSD2 inhibitor with IC₅₀s of 3.8 and 274 nM for ^NSD2 and ^NSD1 respectively. NSD2-IN-6 reduces H3K36me2 levels, reverses cell plasticity by restoring the androgen receptor (^AR) signaling pathway. NSD2-IN-6 reduces a shift from cluster 2 and 3 states towards the cluster 1 state in organoids. NSD2-IN-6 exerts antitumor activity by reversing tumor cell plasticity, suppressing growth, and promoting ^apoptosis in vivo. NSD2-IN-6 can be used for prostate cancer research.

HY-181327

PROTAC EZH2 Degrader-26	Degrader
PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC₅₀ of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC₅₀ of 0.06 μM.

HY-181308

PROTAC EZH2 Degrader-13	Degrader
PROTAC EZH2 Degrader-13 is an EZH2-targeting PROTAC with an IC₅₀ of 2.70 nM. PROTAC EZH2 Degrader-13 exerts antiproliferative effects in cancer cells. PROTAC EZH2 Degrader-13 can be used for the research of cancer.

HY-141877B

MS4322 (isomer)		99.87%
MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC₅₀ of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC₅₀ of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).

HY-144881

(S)-HH2853	Inhibitor
(S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC₅₀ of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases.

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