| 产品描述: | 强效选择性酪蛋白激酶1ε(CK1ε)和CK1δ抑制剂;Potent, selective casein kinase 1ε (CK1ε) and CK1δ inhibitor;PF 670462 is a selective casein kinase, CK1ε and CK1δ inhibitor which also shows potency against 42 other kinases. In addition, PF 670462 can inhibit Period circadian protein homolog 1 (PER1) protein nuclear translocation which results in phase shifts in circadian rhythms.;PF 670462 is a selective casein kinase, CK1ε and CK1δ inhibitor which also shows potency against 42 other kinases. In addition, PF 670462 can inhibit Period circadian protein homolog 1 (PER1) protein nuclear translocation which results in phase shifts in circadian rhythms.A selective CK1ε and CK1δ inhibitor. |
| 体内研究: |
PF-670462 dihydrochloride (50 mg/kg,皮下注射) 产生强烈的相位延迟,并且活性保持持续,在大鼠中没有外源性时间的情况下没有明显的校正。PF-670462 dihydrochloride (25、50 和 100 mg/kg,皮下注射) 诱导剂量依赖性相移。PF-670462 dihydrochloride (50 mg/kg;皮下注射) 在给药后 1 天显著延迟肝脏和胰腺中 Bmal1、Per1、Per2 和 Nr1d1 的节律转录,分别延迟 4.5 ± 1.3 小时和 4.5 ± 1.2 小时。在视交叉上核 (SCN),Nr1d1 和 Dbp mRNA的表达节律也分别延迟了4.2和4 小时。 |
| 参考文献: |
1. Badura L, et al. An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions. J Pharmacol Exp Ther. 2007 Aug;322(2):730-8. Epub 2007 May 14. 2. Cheong JK, et al. IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/? and Wnt/β-catenin independent inhibition of mitotic spindle formation. Oncogene. 2011 Jun 2;30(22):2558-69. 3. Kennaway DJ, et al. Acute inhibition of casein kinase 1δ/ε rapidly delays peripheral clock gene rhythms. Mol Cell Biochem. 2015 Jan;398(1-2):195-206. |
| 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 |
2.437 ml |
12.186 ml |
24.371 ml |
| 5 mM |
0.487 ml |
2.437 ml |
4.874 ml |
| 10 mM |
0.244 ml |
1.219 ml |
2.437 ml |
| 50 mM |
0.049 ml |
0.244 ml |
0.487 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。 |