| 产品描述： | KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM. |
| 靶点： |
IC50: 15.1 nM (KDM5); EC50: 0.34 μM (PC9 H3K4Me3);HistoneDemethylase |
| 体外研究： |
KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A |
| 体内研究： |
When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo |
| 参考文献： |
1. Liang J, et al. Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.083 ml |
15.414 ml |
30.828 ml |
| 5 mM |
0.617 ml |
3.083 ml |
6.166 ml |
| 10 mM |
0.308 ml |
1.541 ml |
3.083 ml |
| 50 mM |
0.062 ml |
0.308 ml |
0.617 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