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Cat. No. M21649
Bractoppin Structure
Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 270  USD270 In stock
25mg USD 580  USD580 In stock
50mg USD 880  USD880 In stock
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Quality Control & Documentation
Biological Activity

Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain with IC50 of 74 nM. Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin (100 μM) selectively inhibits damage-induced BRCA1 foci formation, but has little effect on the radiation-induced accumulation of MDC1 at sites of DNA damage. Similarly, Bractoppin has little effect on the radiation-induced recruitment of TOPBP1.

Chemical Information
Molecular Weight 414.47
Formula C25H23FN4O
CAS Number 2290527-07-8
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Yicong Wan, et al. Biochem Biophys Res Commun. Bractoppin, a BRCA1 carboxy-terminal domain (BRCT) inhibitor, suppresses tumor progression in ovarian borderline tumor organoids

[2] Vadiraj Kurdekar, et al. ChemMedChem. Structure-Guided Synthesis and Evaluation of Small-Molecule Inhibitors Targeting Protein-Protein Interactions of BRCA1 tBRCT Domain

[3] Jayaprakash Periasamy, et al. Cell Chem Biol. Targeting Phosphopeptide Recognition by the Human BRCA1 Tandem BRCT Domain to Interrupt BRCA1-Dependent Signaling

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