2. Epigenetics GPCR/G Protein Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Autophagy Apoptosis
  3. Histone Methyltransferase GLP Receptor Reactive Oxygen Species (ROS) Autophagy Apoptosis
  4. G9a-IN-4

G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer.

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G9a-IN-4

G9a-IN-4 Chemical Structure

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G9a-IN-4 Related Antibodies

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View All Histone Methyltransferase Isoform Specific Products:

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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

G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer[1].

In Vitro

G9a-IN-4 (Compound 31) is a specific G9a/GLP inhibitor (IC50 = 0.2 nM; IC50 = 0.43 nM) with high selectivity for other tested epigenetic targets in AlphaLISA[1].
G9a-IN-4 (72 h) displays more potent suppressing effects against all tested cancer cells, including hematological cancer cells: RPMI8226 (IC50 = 0.85 μM), MV-4-11 (IC50 = 0.49 μM), Jeko-1 (IC50 = 0.7 μM), Molt4 (IC50 = 1.34 μM), and solid tumor cells: HeLa (IC50 = 1.55 μM), U2OS (IC50 = 3 μM), CT26 (IC50 = 3.31 μM)[1].
G9a-IN-4 (1.25-2.5 μM, 72 h) induces a marked reduction in the dimethylation of H3K9 in CT26 cells in a dose-dependent manner[1].
G9a-IN-4 (2.5-5 μM, 48 h) significantly induces the ROS accumulation in CT26 cells in a dose-dependent manner[1].
G9a-IN-4 (2.5-10 μM, 12 h) significantly decreases LC3-I expression at 10 μM and increases the LC3-II level at all tested concentrations, thus leading to an increased ratio of LC3-II to LC3-I in a dose-dependent manner, effectively induce autophagy in CT26 cells[1].
G9a-IN-4 (2.5-10 μM, 24 h) can increase the proportion of apoptotic cells dose-dependently to 91.37 % from 5.48 % in CT26 cells[1].
G9a-IN-4 (2.5-5 μM for 24 h ) induces G0/G1 phase arrest in CT26 cells[1].

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

G9a-IN-4 Related Antibodies

Western Blot Analysis[1]

Cell Line: CT26 cells
Concentration: 1.25 μM, 2.5 μM
Incubation Time: 72 h
Result: Induced a marked reduction in the dimethylation of H3K9 in CT26 cells in a dose-dependent manner.

Cell Autophagy Assay[1]

Cell Line: CT26 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Significantly decreased LC3-I expression at 10 μM and increased the LC3-II level at all tested concentrations, thus leading to an increased ratio of LC3-II to LC3-I in a dose-dependent manner.
Effectively induced autophagy in CT26 cells.

Cell Cycle Analysis[1]

Cell Line: CT26 cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 24 h
Result: Induced a marked reduction in the dimethylation of H3K9 in CT26 cells in a dose-dependent manner.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-∞ Vz CL MRT0-t
Mice 1 mg/kg i.v. 29.6 h 32 ng/mL 465 ng·h/mL 129045 mL/kg 4101 mL/h/kg 11.2 h
In Vivo

G9a-IN-4 (10 mg/kg, I.p., once every two days for two weeks) effectively inhibits tumors in the colon cancer mice model without causing significant weight loss or death[1].

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

Animal Model: CT26 cells (5 × 105 cells/mouse) were subcutaneously implanted into the right armpit of female BALB/c mice (6 weeks)[1].
Dosage: 10 mg/kg
Administration: I.p., once every two days for two weeks
Result: Significantly suppressed tumor growth with a 45.1 % (TGI) reduction in tumor weight.
Exhibited a negligible impact on the body weight of mice without mortality during the 14-day treatment.
Molecular Weight

616.79

Formula

C35H48N6O4
SMILES

COC1=CC2=C(N=C(N=C2NC3CCN(CC3)C(C)C)N4CCC5=C(C4C)C=C6OCOC6=C5)C=C1OCCCN7CCCC7
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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G9a-IN-4 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:

G9a-IN-4Histone MethyltransferaseGLP ReceptorReactive Oxygen Species (ROS)AutophagyApoptosisAntitumorG9a inhibitorLysine methyltransferaseStructural optimizationTetrahydroisoquinolineInhibitorinhibitorinhibit

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