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Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain with IC50 of 74 nM. Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin (100 μM) selectively inhibits damage-induced BRCA1 foci formation, but has little effect on the radiation-induced accumulation of MDC1 at sites of DNA damage. Similarly, Bractoppin has little effect on the radiation-induced recruitment of TOPBP1.
Molecular Weight | 414.47 |
Formula | C25H23FN4O |
CAS Number | 2290527-07-8 |
Solubility (25°C) | DMSO ≥ 90 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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