YL93

YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> MDM-2/p53

YL93 (0.078-2.5 μM; 24 h) 增加 p53、p21、MDM2 的蛋白质水平[1]。 YL93 (0.02-2.5 μM; 24 h) 使细胞周期停滞在 G1[1]。 YL93 (6.25-25 μM; 48 h) 增加凋亡 RKO 细胞[1]。 YL93 (2.5 μM；48 小时) 增加 MDM4 过表达细胞系 H460、MCF-7 和 U-2 OS 中 p53 靶向基因 MDM2、p21 和 PUMA 的转录[1]。 Western Blot Analysis[1] Cell Line: HCT-116 cells Concentration: 0.078125 μM, 0.15625 μM, 0.3125 μM, 0.625 μM, 1.25 μM, and 2.5 μM Incubation Time: 24 hours Result: Significantly increased the protein level of p53, p21, MDM2. Cell Cycle Analysis[1] Cell Line: HCT-116 cells Concentration: 0.02 μM, 0.1 μM, 0.5 μM, 2.5 μM Incubation Time: 24 hours Result: Arrested cell cycle at G1 phase.

[1]. Zhang S, et al. Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells. J Med Chem. 2022 Apr 28;65(8):6207-6230.