CPI-455 HCl
产品说明书
 |
同义名 : | CPI-455 HCl |
| CAS号 : | 2095432-28-1 | |
| 货号 : | A301323 | |
| 分子式 : | C16H15ClN4O | |
| 纯度 : | 98% | |
| 分子量 : | 314.77 | |
| MDL号 : | N/A | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - |
| 生物活性 | |||
|---|---|---|---|
| 描述 | CPI-455 Hydrochloride is the hydrochloride form of CPI-455. CPI-455 is a specific KDM5 inhibitor with IC50 value of 10nM for inhibition of full-length KDM5A in enzymatic assays. CPI-455-mediated KDM5 inhibition resulted in a dose-dependent increase in global H3K4me3 in HeLa cells. Also it induced a time-dependent increase in H3K4me3 that was detected only after 2 or more days of treatment. The elevation of H3K4 trimethylation mediated by this inhibition of KDM5 by CPI-455 decreased the number of drug-tolerant state in multiple cancer cell line models treated with standard chemotherapy or targeted agents[2]. | ||
| 作用机制 | The nitrile of CPI-455 makes a single interaction with the active-site metal ion of KDM5. The position occupied by CPI-455 completely overlaps the binding site of 2-OG, demonstrating a competitive mode of action.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.88mL 3.18mL 1.59mL |
31.77mL 6.35mL 3.18mL |
| 参考文献 |
|---|