RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.
RK-33 demonstrates the ability to inhibit a variety of cancer cell types, with IC50 values ranging between 3-6 µM. However, the PC3 cell line exhibits a much lower sensitivity to RK-33, with an IC50 exceeding 12 µM. Treatment with RK-33 leads to a notable increase in the G1 phase population in DU145 and LNCaP cell lines. In contrast, 22Rv1 cells show only a slight increase in the G1 phase upon RK-33 treatment, along with a significant decrease in the G2 phase population. Additionally, RK-33 induces a moderate elevation in the G1 phase in 22Rv1 cells[1].
RK-33 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
A549 cells
Cytotoxicity assay
72 h
Cytotoxicity against human A549 cells after 72 hrs by WST1 assay, IC50=2.5 μM
21572541
A549 cells
Cytotoxicity assay
72 h
Cytotoxicity against human A549 cells after 72 hrs by WST1 assay, IC50=2.56 μM
23290252
H460 cells
Cytotoxicity assay
72 h
Cytotoxicity against human H460 cells after 72 hrs by WST1 assay, IC50=2.8 μM
21572541
MCF7 cells
Cytotoxicity assay
72 h
Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay, IC50=7.5 μM
21572541
RK-33 动物研究
Animal study
The combination of RK-33 and radiation in mice leads to increased cell death, characterized by pyknotic or condensed nuclei, mixed with fibrin and interstitial edema, in tumors compared to those treated with control or single treatments. This combined treatment approach shows superiority in diminishing tumor proliferation[1]. In mice that received RK-33-PLGA treatment, RK-33 was present in the plasma at a concentration of 34 μg/mL and in the liver at 28 μg/g, while no RK-33 was detected in the lungs[2].
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