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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 |
| Related DNA/RNA Synthesis Products |
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| Capecitabine
Capecitabine is an orally-administered chemotherapeutic agent. Capecitabine is a precursor, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. Capecitabine may inhibit cytochrome CYP2C9 enzyme, and therefore increase levels of substrates such as phenytoin and other substrates of CYP2C9. |
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