RAD51 Inhibitor B02

RAD51 inhibitor B02 is an inhibitor of RAD51 recombinase (IC₅₀ = 27.4 µM in a FRET-based DNA strand exchange assay), which is often overexpressed in cancer cells.¹ It is selective for RAD51 over the E. coli homologue RecA at concentrations up to 250 µM and over RAD54 at concentrations up to 200 µM. RAD51 inhibitor B02 inhibits RAD51 binding to single-stranded DNA (ssDNA) and disrupts double-stranded DNA binding to the RAD51/ssDNA filament.² It inhibits irradiation-induced RAD51 foci formation in HEK293 cells at a concentration of 50 µM. RAD51 inhibitor B02 increases sensitivity to cisplatin (Item No. 13119) in mouse embryonic fibroblasts in vitro and in an MDA-MB-231 mouse xenograft model when used at a dose of 50 mg/kg.³

WARNING This product is not for human or veterinary use.

1. Huang, F., Motlekar, N.A., Burgwin, C.M., et al. Identification of specific inhibitors of human RAD51 recombinase using high-throughput screening. ACS Chem. Biol. 6(6), 628-635 (2011).

2. Huang, F., Mazina, O.M., Zentner, I.J., et al. Inhibition of homologous recombination in human cells by targeting RAD51 recombinase. J. Med. Chem. 55(7), 3011-3020 (2012).

3. Huang, F., and Mazin, A.V. A small molecule inhibitor of human RAD51 potentiates breast cancer cell killing by therapeutic agents in mouse xenografts. PLoS One 9(6), e100993 (2014).