Catalog No.: PC-63244Not For Human Use, Lab Use Only.
Bractoppin is a potent, small-molecule chemical inhibitor that specific selectively blocks phosphopeptide recognition by tumor-suppressor breast cancer 1 (BRCA1) tBRCT domain with binding IC50 of 74 nM.
Bractoppin is a potent, small-molecule chemical inhibitor that specific selectively blocks phosphopeptide recognition by tumor-suppressor breast cancer 1 (BRCA1) tBRCT domain with binding IC50 of 74 nM.
Bractoppin shows no inhibition for recognition of cognate biotinylated phosphopeptides to the TOPBP1 tBRCT 7/8, or GRB2 SH2 proteins.
Bractoppin engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket.
Bractoppin inhibits substrate recognition detected by Förster resonance energy transfer, and diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51.
Bractoppin selectively interrupts BRCA1 tBRCT-dependent signals evoked by DNA damage.
