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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *