Art. -Nr.: HY-183058

EZM8266

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EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC₅₀ of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.24%
CAS. Nr.: 2140164-84-5
Formel: C₁₉H₂₇N₅O₃
Molecular Weight:373.45

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

EZM8266 Chemical Structure

CAS. Nr.: 2140164-84-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

G9a

1 pM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

EZM8266 (Compound 5R) (0.5-10 μM; ~15 days) potently inhibits colony formation of human PLC/PRF/5 HCC cells^[1].
EZM8266 (0.5-10 μM; 3 weeks) dose-dependently inhibits anchorage-independent growth of human PLC/PRF/5 HCC cells^[1].
EZM8266 (1-5 μM; 24 h) dose-dependently inhibits migration of human HuH7 HCC cells^[1].
EZM8266 (1-5 μM; 24 h) dose-dependently inhibits invasion of human HuH7 HCC cells^[1].
EZM8266 (compound 5a) (5 μM; 48 h) induces broad transcriptional reprogramming in human PLC/PRF/5 HCC cells, upregulating immune-related pathways including innate immune response, interferon signaling, and dsRNA processing^[1].
EZM8266 (5 mM; 24 h pre-treatment, 48 h single agent treatment) enhances IFN-γ-mediated upregulation of immune-related genes (including chemokines, MHC class I components, and interferon response genes) in murine PM299L HCC cells when used alone or in combination with IFN-γ^[1].
EZM8266 (1 μM); 24 h pre-treatment, 48 h single agent treatment) synergizes with IFN-γ to significantly increase CXCL10 secretion in murine PM299L and human HuH7 HCC cells when used in combination^[1].
EZM8266 (5 mM; 24 h pre-treatment, 48 h single agent treatment) enhances IFN-γ-mediated upregulation of MHC class I surface expression in murine PM299L and human HuH7 HCC cells when used alone or in combination with IFN-γ^[1].
EZM8266 (48 h) induces significant accumulation of intracellular double-stranded RNA in murine and human HCC cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Invasion Assay^[1]

Cell Line:

human HuH7 HCC cells
Concentration:

1 μM; 2.5 μM; 5 μM
Incubation Time:

24 h
Result:

Significantly reduced cell invasion in a dose-dependent manner, with ~60%, ~80%, and ~90% reductions at 1, 2.5, and 5 μM respectively, compared to control.

Real Time qPCR^[1]

Cell Line:

murine PM299L HCC cells
Concentration:

5 μM
Incubation Time:

24 h (pre-treatment); 48 h (treatment)
Result:

Upregulated expression of Cxcl9, Cxcl10, B2m, Hla-a, Nlrc5, Mda5, Stat1, Rigi, Casp1, Lgals3bp, Tap1, and Irgm2 when used alone.
Produced a synergistic increase in expression of all these genes when combined with IFN-γ compared to either treatment alone.

ELISA Assay^[1]

Cell Line:

murine PM299L and human HuH7 HCC cells
Concentration:

1 μM
Incubation Time:

24 h (pre-treatment); 48 h (treatment)
Result:

Slightly increased CXCL10 secretion when used alone, while IFN-γ alone induced a moderate increase.
Produced a synergistic, significant increase in CXCL10 secretion when combined with IFN-γ compared to either treatment alone in both PM299L and HuH7 cells.

Immunofluorescence^[1]

Cell Line:

murine and human HCC cells
Concentration:

5 mM
Incubation Time:

24 h (pre-treatment); 48 h (treatment)
Result:

Significantly increased intracellular dsRNA accumulation, with mean fluorescence per cell ~3-fold higher compared to DMSO-treated controls.

In Vivo

EZM8266 (Compound 5R) (300 mg/kg; p.o.; daily) significantly reduces tumor growth and increases intratumoral CD8⁺ and CD4⁺ T cell infiltration in an orthotopic murine HCC model^[1].
EZM8266 (300 mg/kg; p.o.; 5 days per week; 4 weeks) monotherapy significantly reduces tumor burden and incidence in an orthotopic murine HCC model, and combination with anti-PD1 further enhances antitumor efficacy, normalizes serum liver enzyme levels, and increases intratumoral CD8⁺ and CD4⁺ T cell infiltration^[1].
EZM8266 (300 mg/kg; p.o.; 5 days per week; 4 weeks) monotherapy significantly reduces tumor burden in a MYC/β-catenin-driven murine HCC model, and combination with anti-PD1 enhances antitumor efficacy and reshapes the tumor microenvironment to a less immunosuppressive state^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J (male, 6-8 weeks old, orthotopic implantation of PM299L murine HCC tumor fragments)^[1]
Dosage:

300 mg/kg
Administration:

p.o.; daily
Result:

Significantly reduced tumor growth compared to vehicle controls.
Significantly lowered final tumor weights compared to vehicle controls.
Increased tumor-infiltrating CD8+ T cell counts to a mean of ~100 cells/mm² (from vehicle mean ~30 cells/mm²).
Increased CD4+ T cell counts to a mean of ~100 cells/mm² (from vehicle mean ~30 cells/mm²).

Animal Model:

C57BL/6J (male, 6-8 weeks old, intrahepatic injection of PM299L murine HCC cells)^[1]
Dosage:

300 mg/kg; 300 mg/kg plus 100 μg/mouse anti-PD1
Administration:

p.o.; 5 days per week; 4 weeks
Result:

Reduced liver index (tumor burden) from a vehicle mean of ~18% to ~7% with monotherapy.
Reduced tumor incidence from 100% to 80% with monotherapy.
Further reduced liver index to ~3% with combination therapy.
Further reduced tumor incidence to 50% with combination therapy.
Reduced serum alanine transaminase (ALT), aspartate transaminase (AST), and lactate dehydrogenase (LDH) levels to levels comparable to age-matched normal mice.
Increased tumor-infiltrating CD8+ T cell counts to a mean of ~6000 cells/mm² with monotherapy, and to ~8000 cells/mm² with combination therapy (from vehicle mean ~1000 cells/mm²).
Increased CD4+ T cell counts to a mean of ~15000 cells/mm² with combination therapy (from vehicle mean ~5000 cells/mm²).
Reduced tumor area from a vehicle mean of ~80 μm² to ~20 μm² with monotherapy, and to ~5 μm² with combination therapy.

Animal Model:

C57BL/6J (male, 4 weeks old, hydrodynamic tail vein injection of MYC/CTNNB1-Δ90 transposon vectors)^[1]
Dosage:

300 mg/kg; 300 mg/kg plus 100 μg/mouse anti-PD1
Administration:

p.o.; 5 days per week; 4 weeks
Result:

Elicited a significant antitumor response with monotherapy.
Resulted in a pronounced reduction in tumor burden with combination therapy.
Increased infiltration of CD8+ and CD4+ T lymphocytes with combination therapy.
Decreased CD4+:CD8+ ratio with combination therapy.
Reduced regulatory T cells with combination therapy.
Preserved effector memory subsets without overt T cell exhaustion with combination therapy.

Chemical Information

CAS. Nr. 2140164-84-5
Appearance Solid
Molecular Weight 373.45
Formel C₁₉H₂₇N₅O₃
Color White to off-white
SMILES

CNC1=NC(NC2=CC(OC[C@@H](CN3CCC3)O)=C(C=C2)OC)=NC(C)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 104 mg/mL (278.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6777 mL

13.3887 mL

26.7773 mL

5 mM

0.5355 mL

2.6777 mL

5.3555 mL

10 mM

0.2678 mL

1.3389 mL

2.6777 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Adan-Villaescusa E, et al. Histone methyl-transferase G9a inhibition boosts the efficacy of immune checkpoint inhibitors in experimental hepatocellular carcinoma. Cell Rep Med. 2026;7(4):102717. [Content Brief]

[2]. Campbell JE, et al. Amine-substituted heterocyclic compounds as ehmt2 inhibitors, salts thereof, and methods of synthesis thereof. United States, WO2019079540 A. 2017-10-18.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6777 mL	13.3887 mL	26.7773 mL	66.9434 mL
	5 mM	0.5355 mL	2.6777 mL	5.3555 mL	13.3887 mL
	10 mM	0.2678 mL	1.3389 mL	2.6777 mL	6.6943 mL
	15 mM	0.1785 mL	0.8926 mL	1.7852 mL	4.4629 mL
	20 mM	0.1339 mL	0.6694 mL	1.3389 mL	3.3472 mL
	25 mM	0.1071 mL	0.5355 mL	1.0711 mL	2.6777 mL
	30 mM	0.0893 mL	0.4463 mL	0.8926 mL	2.2314 mL
	40 mM	0.0669 mL	0.3347 mL	0.6694 mL	1.6736 mL
	50 mM	0.0536 mL	0.2678 mL	0.5355 mL	1.3389 mL
	60 mM	0.0446 mL	0.2231 mL	0.4463 mL	1.1157 mL
	80 mM	0.0335 mL	0.1674 mL	0.3347 mL	0.8368 mL
	100 mM	0.0268 mL	0.1339 mL	0.2678 mL	0.6694 mL

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EZM8266

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Chemokine Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EZM8266

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Chemokine Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EZM8266 Related Classifications

HY-183058 Related Classifications