| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
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 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 Forster resonance energy transfer, and diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. |
| 产品描述 | 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: |
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