Bractoppin|CAS 2290527-07-8|DC Chemicals

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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