Bractoppin |
رقم الكتالوجGC62128 |
Bractoppin هو مثبط قوي وانتقائي شبيه بالعقاقير للتعرف على الفوسفوببتيد من خلال مجال BRCA1 الترادفي (t) BRCT (ملزم IC50: 74 نانومتر)يقلل Bractoppin من تجنيد BRCA1 لكسر الحمض النووي ، مما يؤدي بدوره إلى قمع توقيف G2 الناجم عن التلف وتجميع إنزيم recombinase ، RAD51يثبط Bractoppin بشكل تفضيلي الخطوات المعتمدة على BRCA1 tBRCT في استجابة تلف الحمض النووي
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Cas No.: 2290527-07-8
Sample solution is provided at 25 µL, 10mM.
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.
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