UNC-2170 是 53BP1 (IC50=29 µM; Kd=22 µM) 的功能活性片段状配体。与其他九种甲基赖氨酸 (Kme) 读取器蛋白质相比，UNC-2170 对 53BP1 显示出至少17倍的选择性。53BP1 是一种 Kme 结合蛋白，在 DNA 损伤修复 (DDR) 途径中起核心作用，并被招募到双链断裂 (DSB) 位点。
货号:ajcx36372
CAS:1648707-58-7
分子式:C14H21BrN2O
分子量：313.23
溶解度:Methanol : 125 mg/mL (399.07 mM; Need ultrasonic)|DMSO : 100 mg/mL (319.25 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB)[1].

UNC-2170 (500 µM) results in a significant increase in soluble 53BP1 as compared to untreated lysates or lysates treated with UNC2892, the negative control compound. UNC-2170 (30-100 µM; naive splenocytes cultured with LPS and IL-4 for 3.5 days) clearly phenocopies the reduction in CSR seen in 53BP1 mutant B cells[1].

[1]. Perfetti MT, et al. Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. ACS Chem Biol. 2015;10(4):1072-1081.