| Cas No.: | 2290527-07-8 |
| Chemical Name: | (4-(2-fluorobenzyl)piperazin-1-yl)(2-phenyl-1H-benzo[d]imidazol-5-yl)methanone |
| SMILES: | O=C(C1C=C2C(NC(=N2)C2C=CC=CC=2)=CC=1)N1CCN(CC2C(F)=CC=CC=2)CC1 |
| Formula: | C25H23FN4O |
| M.Wt: | 414.474 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Publication: | 1. Periasamy J, et al. Cell Chem Biol. 2018 Mar 9. pii: S2451-9456(18)30076-X. |
| Description: | Bractoppin is a potent, small-molecule chemical inhibitor that specific selectively blocks phosphopeptide recognition by the BRCA1 tBRCT domain with binding IC50 of 74 nM; shows no inhibition for recognition of cognate biotinylated phosphopeptides to the TOPBP1 tBRCT 7/8, or GRB2 SH2 proteins; engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket; 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; selectively interrupts BRCA1 tBRCT-dependent signals evoked by DNA damage. |

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