| 产品描述： | YKL-05-099 是一种 salt-inducible kinase (SIK) 的抑制剂，对SIK1、SIK2和SIK3的IC50值分别为~10 nM、~40 nM 和 ~30 nM |
| 靶点： |
SIK1(Cell-free assay):10 nM; SIK3(Cell-free assay):30 nM; SIK2(Cell-free assay):40 nM;SIK |
| 体外研究： |
YKL-05-099 displays cell-based activities consistent with SIK inhibition. Pre-treatment with the indicated concentrations of YKL-05-099 for 24 hr potentiates IL-10 production by Zymosan A-stimulated BMDCs |
| 体内研究： |
Well-tolerated doses of YKL-05-099 achieve free serum concentrations above its IC50 for SIK2 inhibition for > 16 hours and reduce phosphorylation of a known SIK substrate in vivo. While in vivo active doses of YKL-05-099 recapitulate the effects of SIK inhibition on inflammatory cytokine responses, they do not induce metabolic abnormalities observed in Sik2 knockout mice. These results identify YKL-05-099 as a useful probe to investigate SIK function in vivo, and further support the development of SIK inhibitors for treatment of inflammatory disorders |
| 细胞实验： |
Cell lines: bone marrow-derived dendritic cells (BMDCs) Concentrations: 1 μM Incubation Time: 24 hr Method: -- |
| 动物实验： |
Animal Models: male 8–10 week-old C57BL/6 mice Dosages: 5 mg/kg-50 mg/kg Administration: IP |
| 参考文献： |
1. Thomas B Sundberg, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 Aug 19;11(8):2105-11. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.666 ml |
8.332 ml |
16.664 ml |
| 5 mM |
0.333 ml |
1.666 ml |
3.333 ml |
| 10 mM |
0.167 ml |
0.833 ml |
1.666 ml |
| 50 mM |
0.033 ml |
0.167 ml |
0.333 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