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GSK343

CAS No. : 1346704-33-3

MCE 站：GSK343

产品活性：GSK343 是一种高效,选择性的 EZH2 抑制剂，IC₅₀ 为 4 nM。

研究领域：Epigenetics  |  Autophagy

作用靶点：Histone Methyltransferase  |  Autophagy

In Vitro: GSK343, which contains an n-propyl group at the 4-position of the pyridone, has EZH2 K_i^app=1.2±0.2 nM. In this 6-day proliferation assay, among the cell lines evaluated in this study, the prostate cancer cell line LNCaP is the most sensitive to EZH2 inhibition, with growth IC₅₀ value of 2.9 μM for GSK343. GSK343 is found to have half maximal inhibitory concentration values of 13 μM in HeLa cells and 15 μM in SiHa cells.

In Vivo: Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels.

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