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Xcessbio/UNC669, L3MBTL1 Domain Inhibitor -Xcessbio Biosciences Inc/10 mM DMSO (1.479 mL)/M60083-5

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¥1780.00
货号:M60083-5
浏览量:127
品牌:Xcess
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Details
Product Information
Molecular Weight:338.24
Formula:C15H20BrN3O
Purity:≥ 98%
CAS#:314241-44-5
Solubility:DMSO up to 50 mM
Chemical Name:(2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)
Storage:Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year.

Biological Activity:

UNC669 is a potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL1, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC669 binds L3MBTL1 with a Kd of 5±1 μM (IC50= 6 ±0.5 μM), exhibiting 5-fold greater affinity than the cognate peptide H4K20Me1, 6-fold selective over its close homologue L3MBTL3 and 10-fold selective over L3MBTL4. The first cocrystal structure of UNC669 bound to L3MBTL1 was determined and provides new insights into binding requirements for further ligand design. UNC669 can serve as a useful chemical tool to interrogate the functions of MBT proteins and probe methyl-lysine reader proteins as a target class.

How to Use:

  • In vitro: UNC1215 was used at 10-25 µM final concentration in vitro and in cellular assays.
  • In vivo:n/a

Reference:

  1. 1. Herold JM, et al. Small-molecule ligands of methyl-lysine binding proteins. (2011) J Med Chem. 54(7):2504-11.

  • UNC669_spec.pdf
  • UNC669_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  。