| 产品描述： | PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively |
| 靶点： |
IC50: 3 μM (JARID1B), 6 μM (JARID1A), 4.9 μM (JARID1C);HistoneDemethylase; HistoneMethyltransferase |
| 体外研究： |
PBIT inhibits proliferation of cells expressing higher levels of JARID1B. PBIT (1-10 μM for UACC-812 cells, 2.5-10μM for MCF7 and MCF10A cells; 72 hours) inhibits cell proliferation in a JARID1B level-dependent manner. Cell Proliferation Assay Cell Line: Human breast cancer cell lines (UACC-812 and MCF7) and human mammary epithelial cells (MCF10A) Concentration: 1, 3, and 10 μM for UACC-812 cells; 2.5, 5, and 10 μM for MCF7 and MCF10A cells Incubation Time: 72 hours Result: Inhibited cell proliferation in a JARID1B level-dependent manner. 10 μM killed most of the UACC-812 cells, but showed minimal toxicity to MCF7 cells and MCF10A cells. |
| 参考文献： |
1. Sayegh J, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. J Biol Chem. 2013 Mar 29;288(13):9408-17. |
| 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 |
4.144 ml |
20.72 ml |
41.44 ml |
| 5 mM |
0.829 ml |
4.144 ml |
8.288 ml |
| 10 mM |
0.414 ml |
2.072 ml |
4.144 ml |
| 50 mM |
0.083 ml |
0.414 ml |
0.829 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。 |
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