SU056

SU056 is a YB-1 inhibitor. SU056 induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. SU056 interacts with YB-1 and inhibits and its associated downstream proteins and pathways. SU056 can enhance the cytotoxic effects of Paclitaxel (HY-B0015)[1].

Research Areas >> Cancer

YB-1[1]

SU056 (约 0-10 μM，48 h) 抑制 OVCAR3/4/5/8、SKOV3 和 ID8 细胞的生长[1]。 SU056 (1 μM，5-8 天) 以剂量依赖性方式抑制 OVCAR-8 和 ID8 细胞集落形成[1]。 SU056 (1-5 μM，6 小时) 将 OVCAR8、SKOV3 和 ID8 细胞 阻滞在 sub-G1 期和 G1 期[1]。 SU056 (0-1 μM，12 小时) 抑制 OVCAR8、SKOV3 和 ID8 细胞的细胞迁移[1]。 SU056 (0-5 μM, 24 h) 在 OVCAR8、SKOV3 和 ID8 细胞中诱导细胞凋亡[1]。 SU056 (1-5 μM, 12 h) 抑制 OVCAR8 细胞中 YB-1、TMSB10、SUMO2 和 PMSB2 蛋白的表达[1]。 SU056 (0.1、0.5 和 1 μM，48 小时) 增强紫杉醇 (HY-B0015) (0.1、0.5 和 1 nM) 的细胞毒性作用[1]。 Cell Viability Assay[1] Cell Line: OVCAR3/4/5/8, SKOV3 and ID8 cells Concentration: 0-10 μM approximately Incubation Time: 48 h Result: Inhibited cell growth with IC50 values of 1.27, 6.8, 4.33, 3.18, 1.73, 3.75 μM. Cell Migration Assay [1] Cell Line: OVCAR8, SKOV3, and ID8 cells Concentration: 0, 0.5, 1 μM Incubation Time: 12 h Result: Dose-dependently inhibited cell migration. Western Blot Analysis[1] Cell Line: OVCAR8 cell Concentration: 1-5 μM Incubation Time: 12 h Result: Dose-dependently inhibited the YB-1, TMSB10, SUMO2, and PMSB2 proteins.

SU056 (20 mg/kg，腹腔注射) 抑制植入 ID8 细胞的小鼠体内的肿瘤生长[1]。 SU056 (10 mg/kg，腹腔注射，每日) 联合紫杉醇 (HY-B0015) (5 mg/kg，每周，腹腔注射) 抑制植入卵巢癌细胞 (OVCAR8) 的免疫缺陷小鼠的肿瘤生长，且比单独给药效果更明显[1]。 Animal Model: C57BL/6 mice implanted (s.c.) with luciferase-expressing ID8 cells[1] Dosage: 20 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Reduced the tumor weight by 2-fold, and is well-tolerated. Reduced the lung metastases. Inhibited YB-1 expression and downstream MDR1 (IHC assay of tumor sample).

[1]. Tailor D, et al. Y box binding protein 1 inhibition as a targeted therapy for ovarian cancer. Cell Chem Biol. 2021 Aug 19;28(8):1206-1220.e6.