CD147 degrader 1

CD147 degrader 1 is a PROTAC targets CD147 with an DC50 value of 6.72 µM. CD147 degrader 1 inhibits cell proliferation, migration and invasion. CD147 degrader 1 decreases the expression of CD147, MMP9, and p-STAT3 protein. CD147 degrader 1 shows anti-cancer acyivity[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

Signaling Pathways >> PROTAC >> PROTAC

CD147 degrader 1 (compound 6a) (2.5, 10 µM; 0, 24, 48 h) 抑制 Sk-Mel-28 细胞的迁移和侵袭[1]。 CD147 degrader 1 (0, 2.5, 5, 10 µM) 以剂量依赖性方式降低 CD147、MMP9 和 p-STAT3 蛋白的表达[1]。 Cell Cytotoxicity Assay[1] Cell Line: Sk-Mel-28 cells Concentration: 0-40 µM Incubation Time: 48 h Result: Exhibited cytotoxicity with an IC50 value of 6.23 µM. Western Blot Analysis[1] Cell Line: Sk-Mel-28, SK-Mel-5 cells Concentration: 0, 2.5, 5, 10 µM Incubation Time: 6 h Result: Decreased the expression of CD147, MMP9, p-STAT3 protein in a dose-dependent manner.

CD147 degrader 1 (20 mg/kg；腹腔注射；每两天一次，持续 17 天) 在小鼠体内显示出抗癌活性[1]。 Animal Model: 6-8 weeks, BALB/c female nude mice (Sk-Mel-5 cells)[1] Dosage: 20 mg/kg Administration: I.p.; every two days for 17 days Result: Significantly reduced volume and weight of tumors, and there was no noticeable weight loss.

[1]. Zhou Z, et al. Targeted degradation of CD147 proteins in melanoma. Bioorg Chem. 2020 Dec;105:104453.