YKL-05-099 - 10mM in DMSO, high purity , CAS No.1936529-65-5

Item Number

Y422363

• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: 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.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

Information

YKL-05-099 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 (Cell-free assay); SIK3 (Cell-free assay); SIK2 (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.

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 and further support the development of SIK inhibitors for treatment of inflammatory disorders.

Cell Research(from reference)

Cell lines：bone marrow-derived dendritic cells (BMDCs) 

Concentrations：1 μM 

Incubation Time：24 hr