| 产品描述: | 有力和选择性的PARP-1抑制剂;a potent and selective PARP-1 inhibitior;BYK204165,也称为PARP抑制剂XIV,是一种细胞可渗透的异喹啉二酮化合物,可有效和选择性地抑制聚(ADP-核糖)聚合酶1(PARP1)。PARP1是一种核酶,参与调节各种细胞过程,例如分化,增殖和肿瘤转化。它也参与分子事件的调控,这些分子事件涉及从DNA损伤中恢复细胞。BYK204165的效价与目前大多数标准PARP-1抑制剂相似或更高(仅略低于PJ34),并且对PARP-1的选择性是PARP-2的100倍。;BYK204165, also known as PARP Inhibitor XIV, is a cell-permeable isoquinolinedione compound that potently and selectively inhibits poly (ADP-ribose) polymerase 1 (PARP1). PARP1 is a nuclear enzyme involved in the regulation of various cell processes such as differentiation, proliferation, and tumor transformation. It is also involved in the regulation of the molecular events involved in the recovery of cell from DNA damage. BYK204165's potency is similar or higher than most current standard PARP-1 inhibitors (just slightly lower than PJ34), and it is 100-fold selective for PARP-1 over PARP-2. |
| 体内研究: |
BYK204165 未在体内进行研究,因为它在大鼠微粒体体外测量的半衰期 (t1/2) 较短,仅为 23 分钟。 |
| 参考文献: |
1. Eltze T, et al. Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. Mol Pharmacol. 2008 Dec;74(6):1587-98. |
| 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 |
3.964 ml |
19.82 ml |
39.64 ml |
| 5 mM |
0.793 ml |
3.964 ml |
7.928 ml |
| 10 mM |
0.396 ml |
1.982 ml |
3.964 ml |
| 50 mM |
0.079 ml |
0.396 ml |
0.793 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。 |