EZM8266
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.24%
- CAS No.: 2140164-84-5
- Formula: C19H27N5O3
- Molecular Weight:373.45
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Histone Methyltransferase Isoforms
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Biological Activity
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G9a 1 pM (IC50) |
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.
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Cell Line:human HuH7 HCC cells
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Concentration:1 μM; 2.5 μM; 5 μM
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Incubation Time:24 h
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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.
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Cell Line:murine PM299L HCC cells
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Concentration:5 μM
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Incubation Time:24 h (pre-treatment); 48 h (treatment)
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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.
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Cell Line:murine PM299L and human HuH7 HCC cells
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Concentration:1 μM
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Incubation Time:24 h (pre-treatment); 48 h (treatment)
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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.
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Cell Line:murine and human HCC cells
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Concentration:5 mM
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Incubation Time:24 h (pre-treatment); 48 h (treatment)
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Result:Significantly increased intracellular dsRNA accumulation, with mean fluorescence per cell ~3-fold higher compared to DMSO-treated controls.
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.
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Animal Model:C57BL/6J (male, 6-8 weeks old, orthotopic implantation of PM299L murine HCC tumor fragments)[1]
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Dosage:300 mg/kg
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Administration:p.o.; daily
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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).
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Animal Model:C57BL/6J (male, 6-8 weeks old, intrahepatic injection of PM299L murine HCC cells)[1]
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Dosage:300 mg/kg; 300 mg/kg plus 100 μg/mouse anti-PD1
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Administration:p.o.; 5 days per week; 4 weeks
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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.
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Animal Model:C57BL/6J (male, 4 weeks old, hydrodynamic tail vein injection of MYC/CTNNB1-Δ90 transposon vectors)[1]
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Dosage:300 mg/kg; 300 mg/kg plus 100 μg/mouse anti-PD1
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Administration:p.o.; 5 days per week; 4 weeks
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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
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CAS No. 2140164-84-5
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Appearance Solid
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Molecular Weight 373.45
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Formula C19H27N5O3
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Color White to off-white
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SMILES
CNC1=NC(NC2=CC(OC[C@@H](CN3CCC3)O)=C(C=C2)OC)=NC(C)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 KB)
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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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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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