货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T28979-1ml	10mM in DMSO	￥840.00 T28979-1ml ￥840.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T28979-1ml

10mM in DMSO

￥840.00

货期：3-5天

产品描述：

Bractoppin is a potent and selective drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response

靶点：

DNA/RNA Synthesis;RAD51

体外研究：

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.

参考文献：

1. Jayaprakash Periasamy, 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.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.413 ml	12.064 ml	24.127 ml
5 mM	0.483 ml	2.413 ml	4.825 ml
10 mM	0.241 ml	1.206 ml	2.413 ml
50 mM	0.048 ml	0.241 ml	0.483 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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