E235

E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

Activates transcription factor 4, ATF4[1]

E235 (1 µM；2、4、8、16 或 24 h) 以时间依赖性方式下调了 HT1080 细胞中 XBP-1s mRNA 的水平[1]。 E235 (0.1-10 µM；4 d 或 5 d) 对 HT1080、RPMI-8226、B16F10、4T1、HT1080 shNT 和 HT1080 shATF4 细胞具有抗增殖活性[1]。 E235 (0、1、5 和 10 µM；4 h) 以剂量依赖性方式增加了 AG1522 细胞中 p53 的表达。 E235 (1 µM；2 h) 增加了 AG1522 细胞中 p-Chk2 的表达[1]。 E235 (0、1、5 和 10 µM；2 h) 增加了 AG1522 和 HT1080 细胞中 p-p53 的表达[1]。 E235 (0、0.5、1、5 和 10 µM；0.5 h) 以剂量依赖性方式增加了 HT1080 细胞中 γ-H2AX 的表达[1]。 Western Blot Analysis[1] Cell Line: HT1080, B16F10 and AG1522 cells. Concentration: 0, 1, 5 and 10 µM. Incubation Time: 4 h. Result: Increased the expression of ATF4 with dose-dependent manner. Western Blot Analysis[1] Cell Line: HT1080 cells. Concentration: 0, 0.5, 1, 5 or 10 µM. Incubation Time: 2, 4 or 8 h. Result: Increased the expression of p-elF2α with time and dose dependent manner. Cell Proliferation Assay[1] Cell Line: HT1080 or RPMI-8226 cells. Concentration: 1 µM. Incubation Time: 0, 8, 16 and 24 h. Result: Exhibited anti-proliferative activity. Cell Viability Assay[1] Cell Line: AG1522 cells. Concentration: 0, 0.1, 0.5, 1 and 10 µM. Incubation Time: 4 d. Result: Inhibited cell viability with dose-dependent manner. Cell Cycle Analysis[1] Cell Line: HT1080 cells and B16F10 cells. Concentration: 1 µM. Incubation Time: 8, 16 and 24 h. Result: Caused cell arrest during G2/M phase.

[1]. Sayers CM, et al. Identification and characterization of a potent activator of p53-independent cellular senescence via a small-molecule screen for modifiers of the integrated stress response. Mol Pharmacol. 2013 Mar;83(3):594-604.