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Bractoppin

Chemical Structure : Bractoppin

CAS No.: 2290527-07-8

Bractoppin

货号: PC-63244Not For Human Use, Lab Use Only.

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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
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.

物理化学性质&存储条件

分子量 414.484
分子式 C25H23FN4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(4-(2-fluorobenzyl)piperazin-1-yl)(2-phenyl-1H-benzo[d]imidazol-5-yl)methanone

参考文献

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

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