| 产品描述： | GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members |
| 靶点： |
KDM5:10 nM (Ki);KDM5:26 nM (IC50);istoneDemethylase; HistoneMethyltransferase |
| 体外研究： |
GSK467 (0-100 μM; 6 days) shows antiproliferative effect against human multiple myeloma tumor cells. GSK467 is located in the 2-OG-binding pocket. GSK467 inhibits spheroid formation, colony formation, invasion and migration of HCC cells. Cell Proliferation Assay Cell Line: Human multiple myeloma tumor cell line MM.1S Concentration: 0-100 μM Incubation Time: 6 days Result: Showed antiproliferative effect with an IC50 of >50 μM. |
| 体内研究： |
GSK-467 can inhibit the proliferation and growth of HCC tumor cells by promoting the expression of miR-448 and inhibiting the YTHDF3/ITGA6 pathway in female BALB/c nude mice |
| 参考文献： |
1. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45. 2. Fu YD, et al. Targeting histone demethylase KDM5B for cancer treatment. Eur J Med Chem. 2020 Dec 15;208:112760. 3. Guo JC, et al. KDM5B promotes self-renewal of hepatocellular carcinoma cells through the microRNA-448-mediated YTHDF3/ITGA6 axis. J Cell Mol Med. 2021 Apr 7;25(13):5949–62. |
| 溶解性： |
Soluble in DMSO |
| 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 |
3.132 ml |
15.658 ml |
31.317 ml |
| 5 mM |
0.626 ml |
3.132 ml |
6.263 ml |
| 10 mM |
0.313 ml |
1.566 ml |
3.132 ml |
| 50 mM |
0.063 ml |
0.313 ml |
0.626 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京