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Xcessbio/UNC2170, Methyl-lysine Binding Protein 53BP1 Inhibitor-Xcessbio Biosciences Inc/2 mg solid/M60260-2s

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¥1980.00
货号:M60260-2s
浏览量:113
品牌:Xcess
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Molecular Weight:429.30
Formula:C14H21BrN2O.C4H4O4
Purity:≥98%
CAS#:n/a
Solubility:DMSO up to 100 mM
Chemical Name:3-bromo-N-(3-(tert-butylamino)propyl)benzamide maleate
Storage:Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year.

Biological Activity:UNC2170 is a selective and cell permeable methyl-lysine binding protein 53BP1 antagonist with micromolar activity. It displays >17-fold selectivity for 53BP1 as compared to other methyl-lysine (Kme) binding proteins tested. Structural studies revealed that the tert-butyl amine of UNC2170 anchors the compound in the methyl-lysine (Kme) binding pocket of 53BP1, making it competitive with endogenous Kme substrates. X-ray crystallography also demonstrated that UNC2170 binds at the interface of two tudor domains of a 53BP1 dimer. It functions as a 53BP1 antagonist in cellular lysates and shows cellular activity by suppressing class switch recombination, a process which requires a functional 53BP1 tudor domain.How to Use: In vitro:UNC2170 was used at 10-30 µM final concentration in various in vitro assays.In vivo: n/aReference:

  • 1.Perfetti MT, et al. Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. (2015) ACS Chem Biol. 10(4):1072-81.
UNC2170_spec.pdf
UNC2170_MSDS.pdf
Products are for research use only. Not for human use.

Xcess新型高效神经保护分子P7C32014年10月13日03:55  | 新闻印刷版刚刚在上个月的Cell中发表,最近关于神经保护小分子P7C3的 MOA研究具有广泛的体外和体内活性,为研究共享其他常见组织的神经系统疾病,损伤,发育和退行性疾病提供了新的令人兴奋的机会机制。  P7C3 是直接从体内神经发生筛选中鉴定出的无毒,稳定且可口服生物利用的合成小分子。它可以保护齿状回中的新生神经元,并刺激新神经元的生长。它还可以增强老年大鼠的学习和记忆能力。在爆炸介导的创伤性脑损伤(TBI)的啮齿动物模型中,P7C3还可以在损伤后,在神经元细胞死亡发生之前保持轴突的完整性。MOA研究表明P7C3可以结合烟酰胺磷酸核糖基转移酶(NAMPT),这是一种将烟酰胺转化为烟酰胺腺嘌呤二核苷酸(NAD)的限速酶。将活性P7C3化学物质施用至用阿霉素处理的细胞(诱导NAD耗竭),可导致细胞内NAD水平反弹,并免受阿霉素介导的毒性的影响。  如何订购:  Xcess Biosciences是一家领先的试剂和服务公司,提供10 mM DMSO溶液和以克计的固体形式的化合物。请访问我们的网站以获取订单信息和其他创新产品。特别是Xcess Biosciences继续向我们的表观遗传调节剂工具箱  (现在我们提供72种独特的化合物)和  泛素调节剂工具箱  (现在我们提供15种独特的化合物)中添加了更多新颖的小分子化学探针  。