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• 產(chǎn)品描述： YKL-05-099 是一種 salt-inducible kinase (SIK) 的抑制劑，對(duì)SIK1、SIK2和SIK3的IC50值分別為~10 nM、~40 nM 和 ~30 nM

• 靶點(diǎn)： SIK1(Cell-free assay):10 nM; SIK3(Cell-free assay):30 nM; SIK2(Cell-free assay):40 nM;SIK

• 體外研究：
  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

• 體內(nèi)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

• 細(xì)胞實(shí)驗(yàn)： Cell lines: bone marrow-derived dendritic cells (BMDCs) Concentrations: 1 μM Incubation Time: 24 hr Method: --

• 動(dòng)物實(shí)驗(yàn)： Animal Models: male 8–10 week-old C57BL/6 mice Dosages: 5 mg/kg-50 mg/kg Administration: IP

• 參考文獻(xiàn)：
  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

• 保存條件： -20°C

• 配置溶液濃度參考：
  

  	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：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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