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RAD51 inhibitors and modulators act on the recombinase at the center of homologous recombination repair. RAD51 is the human counterpart of bacterial recombination protein A (RecA) and repairs DNA double-strand breaks by copying an intact template. It coats single-stranded DNA as a helical filament, and purified human RAD51 carries out ATP-dependent homologous pairing and strand exchange. Breast cancer susceptibility protein 2 (BRCA2) loads RAD51 onto DNA through eight short repeat motifs. RAD51 Inhibitor B02 came from a high-throughput screen for compounds that block RAD51 strand exchange. RI-1 and IBR2 are further RAD51 inhibitors, while CAM833 disrupts the BRCA2-RAD51 interaction. RS-1 works in the opposite direction and stimulates the recombination activity of RAD51.