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COA of Bractoppin

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.

Chemical Information

Catalog Featured products
Purity of current batch >98%
CAS 2290527-07-8
Molecular Weight (MW) 414.474
Molecular Formula C25H23FN4O
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Handling:

Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

Reference:

1. Periasamy J, et al. Cell Chem Biol. 2018 Mar 9. pii: S2451-9456(18)30076-X.