Bractoppin |
Catalog No.GC62128
One-Click Copy Product Info
|
Bractoppin is a drug-like inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain with an IC50 value of 74nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2290527-07-8
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Bractoppin is a drug-like inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain with an IC50 value of 74nM [1]. Bractoppin binds to the tBRCT residues of pSer and the adjacent pocket, which can block the BRCA1 tBRCT-dependent cellular signaling induced by DNA damage [2]. Bractoppin has been widely used to inhibit the cell cycle and DNA damage repair[3].
In vitro, Bractoppin treatment (10μM) for 24 hours significantly enhanced the sensitivity of 5637R cells to oxaliplatin and decreased cell viability[4]. Treatment with Bractoppin (100μM) for 3 hours inhibited the DNA replication mediated by double-strand breaks in oocyte DNA induced by bleomycin[5]. Treatment with 40μM Bractoppin for 48 hours significantly induced apoptosis in SKOV3 cells, accompanied by an increase in the expression of Bax-xl, and a decrease in the expression of proliferation-related proteins cyclin D1 and cyclin D2[6].
References:
[1] Kurdekar V, Giridharan S, Subbarao J, et al. Structure‐Guided synthesis and evaluation of small‐molecule inhibitors targeting protein–protein interactions of BRCA1 tBRCT domain[J]. ChemMedChem, 2019, 14(18): 1620-1632.
[2] Peña-Guerrero J, Fernández-Rubio C, García-Sosa A T, et al. BRCT domains: structure, functions, and implications in disease—new therapeutic targets for innovative drug discovery against infections[J]. Pharmaceutics, 2023, 15(7): 1839.
[3] Periasamy J, Kurdekar V, Jasti S, et al. Targeting phosphopeptide recognition by the human BRCA1 tandem BRCT domain to interrupt BRCA1-dependent signaling[J]. Cell chemical biology, 2018, 25(6): 677-690. e12.
[4] Yan Y, Zhang H, Jia C, et al. Elevated NDRG1 Expression Drives Oxaliplatin Chemoresistance in Bladder Cancer Cells by Promoting Homologous Recombination Repair and Inhibiting G2/M Arrest[J]. Cell Biochemistry and Biophysics, 2026, 84(1): 1433-1448.
[5] Xia T J, Xie F Y, Chen J, et al. CDK1 mediates the metabolic regulation of DNA double-strand break repair in metaphase II oocytes[J]. BMC biology, 2025, 23(1): 37.
[6] Wan Y, Zhang Y, Meng H, et al. Bractoppin, a BRCA1 carboxy-terminal domain (BRCT) inhibitor, suppresses tumor progression in ovarian borderline tumor organoids[J]. Biochemical and biophysical research communications, 2023, 638: 76-83.
| Cell experiment [1]: | |
Cell lines | SKOV3 cells |
Preparation Method | SKOV3 cells were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), and 0.1% (w/v) antibiotics (100U/ml penicillin, and 100mg/ml streptomycin) at 37°C in 5% CO2/atmosphere. Cells were seeded at a density of 5×103 cells/ml in the 96-well plates and allowed to adhere in a 5% CO2 incubator at 37°C for 24h. The cells were treated with different concentrations of Bractoppin (0, 5, 10, 20, 30, and 40μM) for 48h. The cell viability was evaluated. |
Reaction Conditions | 0, 5, 10, 20, 30, and 40μM; 48h |
Applications | Bractoppin treatment significantly reduced cell viability of SKOV3 cells in a dose-dependent manner. |
References: | |
| 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 |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4127 mL | 12.0636 mL | 24.1272 mL |
| 5 mM | 482.5 μL | 2.4127 mL | 4.8254 mL |
| 10 mM | 241.3 μL | 1.2064 mL | 2.4127 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)