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CAS No. : 2290527-07-8
MCE 国际站:Bractoppin
产品活性:Bractoppin 是一种有效的 BRCA1 (t)BRCT domain 识别磷酸肽的选择性抑制剂 (IC50: 74 nM)。Bractoppin 减少 BRCA1 对 DNA 断裂片段的招募,进而抑制损伤诱导的 G2 期阻滞和重组酶 RAD51 的组装。Bractoppin 优先抑制 BRCA1 -tBRCT 依赖的 DNA 损伤。
研究领域:Cell Cycle/DNA Damage
作用靶点:DNA/RNA Synthesis | RAD51
In Vitro: In a MST assay, Bractoppin exhibits nanomolar potency in displacing cognate BACH1 phosphopeptide substrate from the BRCA1 tBRCT, the binding IC50 value is 74 nM.In a selectivity profile by competitive MST assay, Bractoppin (0-100 μM) does not detectably bind to fluorescently labeled tBRCT domains from MCPH1, TOPBP1 7/8, ECT2, or TOPBP1 1/2.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 (a protein containing multiple, structurally related tBRCT domains).Bractoppin (10-100 μM; 0.5 hr before radiation (32 hours)) inhibits 4Gy radiation induced G2 arrest in a dose-dependent manner. The percentage of G2 arrest cell is 64%, 42% and 25% for 10 μM, 30 μM and 100 μM, respectively.
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