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EZH2 SET domain

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histone Methyltransferase (5) PROTACs (3)
By Research Areas:	Cancer (3)

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Targets Recommended: Discoidin Domain Receptor Epigenetic Reader Domain EHD Protein WDR5 YTHDF PASK/STK37 VISTA SHP1 PIKfyve BCL6 PNPLA3

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N5024

Gambogenic acid 2 Publications Verification	Histone Methyltransferase	Cancer
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of *EZH2, specifically and covalently binds to Cys668 within the EZH2-SET* domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer .

HY-101508

GNA002	Histone Methyltransferase	Cancer
GNA002 is a highly potent, specific and covalent *EZH2* (Enhancer of zeste homolog 2) inhibitor with an IC₅₀ of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .

HY-181324

PROTAC EZH2 Degrader-23	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-23 (compound 8) is a PROTAC protein degrader targeting *EZH2* with a target IC₅₀ of 30.00 nM. PROTAC EZH2 Degrader-23 inhibits *EZH2* methyltransferase activity via interaction with the *EZH2* SET domain .

HY-181331

PROTAC EZH2 Degrader-27	PROTACs Histone Methyltransferase	Others
PROTAC EZH2 Degrader-27 is a *EZH2* PROTAC inhibitor with an IC₅₀ of 4.00 nM against *EZH2. PROTAC EZH2* Degrader-27 inhibits methyltransferase activity by interacting with the SET domain of *EZH2* .

HY-181333

PROTAC EZH2 Degrader-38	PROTACs Histone Methyltransferase	Others
PROTAC EZH2 Degrader-38 (Compound 17) is a *EZH2* PROTAC degrader with an IC₅₀ of 165.00 nM. PROTAC EZH2 Degrader-38 functionally inhibits the methyltransferase activity of *EZH2* and competitively binds to the SAM-binding pocket of the *EZH2* SET domain .

Gambogenic acid 2 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Guttiferae Phenols Polyphenols Plants Garcinia hanburyi Hook. f. Disease Research Fields Cancer Source Classification	Histone Methyltransferase
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of *EZH2, specifically and covalently binds to Cys668 within the EZH2-SET* domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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EZH2 SET domain

Inhibitors & Agonists

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