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Bractoppin

Catalog No.GC62128

Bractoppin is a inhibitor of phosphopeptide recognition by the human BRCA1 tBRCT domain with IC50 of 74 nM.

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Bractoppin Chemical Structure

Cas No.: 2290527-07-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$149.00
In stock
5 mg
$135.00
In stock
10 mg
$225.00
In stock
25 mg
$495.00
In stock
50 mg
$765.00
In stock
100 mg
$1,215.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Preparation Method

For the direct binding assay, 10μl of labeled protein at a final concentration of 20nM was mixed with 10μl of test compound( Bractoppin ) and incubated on ice for 10 min. For the competitive assay, 10μl of labeled protein at a final concentration of 20nM was mixed with 2μM cognate peptide substrate at the EC80 concentration determined by prior titration using a 16-point serial dilution by direct-binding MST.

Reaction Conditions

0-105nM Bractoppin

Applications

Bractoppin is a 414-Da compound, with nanomolar potency in displacing cognate BACH1 phosphopeptide substrate from the BRCA1 tBRCT as measured by MST( IC50 0.074 μM). Its predicted binding mode to BRCA1 tBRCT reveals favorable hydrophobic interactions in the hydrophobic cavity, as well as a T-shaped, pi-pi stacking interaction with Phe1662, that together significantly contribute toward its activity. Indeed, substitution of the phenyl ring at R1 in Bractoppin with a 4-pyridyl group (CCBT2082) decreased activity by 5-fold by affecting the stacking interaction with Phe1662.

Cell experiment [2]:

Cell lines

HEK293 cells

Preparation Method

HEK293 cells stably harboring plasmids for Tet-inducible expression of tBRCT domains were seeded. Compound( Bractoppin )addition or inducible expression of BRCA1 tBRCT were performed as indicated, when cells were 30% confluent, before exposure to 1Gy irradiation.

Reaction Conditions

1-100uM Bractoppin for 7 days

Applications

In cells, 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.

References:

[1]. Periasamy J, Kurdekar V, et,al.Targeting Phosphopeptide Recognition by the Human BRCA1 Tandem BRCT Domain to Interrupt BRCA1-Dependent Signaling. Cell Chem Biol. 2018 Jun 21;25(6):677-690.e12. doi: 10.1016/j.chembiol.2018.02.012. Epub 2018 Mar 29. PMID: 29606576; PMCID: PMC6015222.

Background

Bractoppin is a tandem BRCT (tandem BRCT, BRCA1) delivered by human breast and ovarian cancer suppressor protein (BRCA1) tBRCT domain recognizes a drug-like inhibitor of phosphopeptide that selectively inhibits nanomolar activity of substrate binding in vitro with an IC50 of 0.074 µM[1].

Bractoppin has nanomolar potency in displacing cognate BACH1 phosphopeptide substrate from the BRCA1 tBRCT. Its predicted binding mode to BRCA1 tBRCT reveals favorable hydrophobic interactions in the hydrophobic cavity, as well as a T-shaped, pi-pi stacking interaction with Phe1662, that together significantly contribute toward its activity. Indeed, substitution of the phenyl ring at R1 in Bractoppin with a 4-pyridyl group (CCBT2082) decreased activity by 5-fold by affecting the stacking interaction with Phe1662[1].

In cells, 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[1].

References:
[1]. Periasamy J, Kurdekar V, et,al. Targeting Phosphopeptide Recognition by the Human BRCA1 Tandem BRCT Domain to Interrupt BRCA1-Dependent Signaling. Cell Chem Biol. 2018 Jun 21;25(6):677-690.e12. doi: 10.1016/j.chembiol.2018.02.012. Epub 2018 Mar 29. PMID: 29606576; PMCID: PMC6015222.

Chemical Properties

Cas No. 2290527-07-8 SDF
Formula C25H23FN4O M.Wt 414.47
Solubility DMSO : 250 mg/mL (603.18 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4127 mL 12.0636 mL 24.1272 mL
5 mM 0.4825 mL 2.4127 mL 4.8254 mL
10 mM 0.2413 mL 1.2064 mL 2.4127 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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