IBR2 is a potent and specific RAD51 inhibitor that inhibits RAD51-mediated repair of DNA double-strand breaks. IBR2 disrupts RAD51 multimerisation, accelerates proteasome-mediated degradation of RAD51 proteins, inhibits cancer cell growth, and induces apoptosis[1][2].In IBR2-treated cancer cells, RAD51 is rapidly degraded and homologous recombination repair is impaired, leading to cell death. For most of the cancer cell lines tested, the IC50 value for the IBR2 prodrug ranged from 12-20 μM. IBR2 inhibited the growth of MBA-MD-468 with an IC50 value of 14.8 μM[1].
IBR2 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
20 μM
32 hours
IBR2 significantly reduced HR frequency, while B6 had no effect
EMBO Mol Med. 2013 Mar;5(3):353-65
HSC2-R cells
10 µM
24 hours
To evaluate the cytotoxicity of IBR2 on HSC2-R cells and its effect on radiosensitivity. Results showed that IBR2 at 10 µM significantly reduced the surviving fraction of HSC2-R cells and promoted apoptosis.
Biomed Rep. 2023 Feb 24;18(4):28
HSC2 cells
10 µM
24 hours
To evaluate the cytotoxicity of IBR2 on HSC2 cells and its effect on radiosensitivity. Results showed that IBR2 at 10 µM slightly affected the surviving fraction of HSC2 cells but did not significantly affect colony formation.
Biomed Rep. 2023 Feb 24;18(4):28
T315I-Ba/F3 cells
20 μM
36 hours
IBR2 dose-dependently reduced Rad51 levels and induced apoptosis
EMBO Mol Med. 2013 Mar;5(3):353-65
MCF7 cells
20 μM
8 hours
IBR2 significantly reduced IR-induced RAD51 foci formation but did not affect γ-H2AX foci
EMBO Mol Med. 2013 Mar;5(3):353-65
IBR2 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/SCID mice
T315I Bcr-abl mutant model
Intraperitoneal injection
100 mg/kg
Once daily for 20 days
IBR2 significantly prolonged animal survival, while imatinib had no effect
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