In vitro: B02 is a specific inhibitor of human RAD51 recombinase, blocks HR repair in human embryonic kidney (HEK) and breast cancer cells and increases their sensitivity to a wide range of DNA damaging agents. Also, B02 enhances DNA damage and apoptosis induced by decitabine in MM cells. B02 shows high specificity for RAD51 and does not significantly inhibit RAD54 in the range of concentrations from 0 to 200 μM. B02 shows biological effect in human and mouse cells. In human embryonic kidney (HEK) cells, B02 disrupts RAD51 foci formation in response to DNA damage and inhibited DSB repair and DSB-dependent HR. B02 can also increase the sensitivity of cancer cells to chemotherapeutic DNA damaging agents. In vivo: B02 significantly increases the anti-tumor activity of cisplatin in vivo. B02 is tolerated by mice at doses up to 50 mg/kg without obvious body weight loss. No detectable morphological changes induced by B02 in kidneys and livers, main organs for detoxification are found.
|Cell lines||The human MM cell lines NCI-H929 (H929), RPMI 8226, ARP-1, U266 and MM.1S cells|
|Preparation method||Proliferation of MM-cell lines is monitored by the WST-1 colorimetric cell-count assay. MM cell lines are seeded in 96-well plates at ~8000 cells/well. The cells are treated with or without B02 (10 μM) for 1 h, followed by treatment with vehicle (DMSO) or DOX (20-160 nM) for 72 h. WST-1 reagent is added to the culture medium in each well at a 1:10 ratio, and incubation continues at 37°C for 4 h. Relative cell number is estimated from absorbance at 450 nm using a spectrophotometer.|
|Incubation time||1 h|
|Animal models||NCR nude mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||67 mg/mL in DMSO|
A Small-Molecule Inhibitor of RAD51 Reduces Homologous Recombination and Sensitizes Multiple Myeloma Cells to Doxorubicin.
Alagpulinsa DA, et al. Front Oncol. 2014 Oct 30;4:289. PMID: 25401086.
A small molecule inhibitor of human RAD51 potentiates breast cancer cell killing by therapeutic agents in mouse xenografts.
Huang F, et al, PLoS One. 2014 Jun 27;9(6):e100993. PMID: 24971740.
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