| 产品描述: | Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells |
| 靶点: |
Kd: 490 nM (G-quadruplexe) |
| 体外研究: |
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest. Pyridostatin hydrochloride is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin hydrochloride causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin hydrochloride induces the formation of DNA DSBs. Remarkably, Pyridostatin hydrochloride (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level Cell Viability Assay Cell Line: Over 60 different cancer cell lines Concentration: 10 μM Incubation Time: 48 hours Result: Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines. |
| 参考文献: |
1. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5. 2. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28. 3. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970. |
| 溶解性: |
Soluble in H2O |
| 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 |
1.284 ml |
6.419 ml |
12.838 ml |
| 5 mM |
0.257 ml |
1.284 ml |
2.568 ml |
| 10 mM |
0.128 ml |
0.642 ml |
1.284 ml |
| 50 mM |
0.026 ml |
0.128 ml |
0.257 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。 |