G9a-IN-4

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.