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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[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Autophagy; GLP Receptor; Histone Methyltransferase; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; Autophagy; Epigenetics; GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Field of Research

Cancer

Smiles

COC1=CC2=C(N=C(N=C2NC3CCN(CC3)C(C)C)N4CCC5=C(C4C)C=C6OCOC6=C5)C=C1OCCCN7CCCC7

Molecular Formula

C35H48N6O4

Molecular Weight

616.79

References & Citations

[1]Shao M, et al. Discovery of 2-tetrahydroisoquinoline-substituted quinazoline derivatives as lysine methyltransferase G9a inhibitors with in vivo antitumor efficacy. Eur J Med Chem. 2025 Dec 15;300:118113.

Shipping Conditions

Room temperature

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-178378/

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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