Bractoppin

Chemical Structure : Bractoppin

CAS No.: 2290527-07-8

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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 tumor-suppressor breast cancer 1 (BRCA1) tBRCT domain with binding IC50 of 74 nM.

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5 mg	￥880	In stock
10 mg	￥1280	In stock
25 mg	￥1980	In stock
50 mg	￥3480	In stock
100 mg		Get quote

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生物&药学活性

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.

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.

Bractoppin

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Bractoppin

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