2. Epigenetics
  3. Histone Methyltransferase
  4. EZM8266

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.

EZM8266

EZM8266 Chemical Structure

CAS No. : 2140164-84-5

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EZM8266 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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[1][2].

IC50 & Target[1]

G9a

1 pM (IC50)

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.

EZM8266 Related Antibodies

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.
Molecular Weight

373.45

Formula

C19H27N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Purity & Documentation
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EZM8266 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EZM82662140164-84-5EZM 8266EZM-8266Histone MethyltransferasePLC/PRF/5 HCC cellsH3K9me2CD8+ T cellG9ahepatocellular carcinomaCD4+ T cellPM299L HCC cellsHuH7 HCC cellsEHMT2histone methyltransferaseInhibitorinhibitorinhibit

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