YKL-05-099

For research use only.

Catalog No.S9646

1 publication

YKL-05-099 Chemical Structure

CAS No. 1936529-65-5

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.

Selleck's YKL-05-099 has been cited by 1 publication

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

Cell Research:

[1]

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

    --


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (166.63 mM)
Water Insoluble
Ethanol ''''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 600.11
Formula

C32H34ClN7O3

CAS No. 1936529-65-5
Storage powder
in solvent
Synonyms N/A
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

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID