YKL-05-099

Catalog No.S9646

For research use only.

YKL-05-099 is an inhibitor of salt-inducible kinase (SIK) with IC50 of ~10 nM, ~40 nM and ~30 nM for SIK1, SIK2 and SIK3, respectively.

YKL-05-099 Chemical Structure

CAS No. 1936529-65-5

Selleck's YKL-05-099 has been cited by 2 Publications

Purity & Quality Control

Choose Selective SIK Inhibitors

Biological Activity

Description YKL-05-099 is an inhibitor of salt-inducible kinase (SIK) with IC50 of ~10 nM, ~40 nM and ~30 nM for SIK1, SIK2 and SIK3, respectively.
Targets
SIK1 [1]
(Cell-free assay)
SIK3 [1]
(Cell-free assay)
SIK2 [1]
(Cell-free assay)
10 nM 30 nM 40 nM
In vitro

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.[1]

In vivo

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.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: bone marrow-derived dendritic cells (BMDCs)
  • Concentrations: 1 μM
  • Incubation Time: 24 hr
  • Method:

    --

Animal Research:

[1]

  • Animal Models: male 8–10 week-old C57BL/6 mice
  • Dosages: 5 mg/kg-50 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 600.11
Formula

C32H34ClN7O3

CAS No. 1936529-65-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=CC=C1)Cl)N2CC3=CN=C(N=C3N(C2=O)C4=NC=C(C=C4)OC)NC5=C(C=C(C=C5)C6CCN(CC6)C)OC

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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