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
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YKL-05-099
CAS number：1936529-65-5 molecular formula：C32H34ClN7O3
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| Chinese alias | - | ||
| English alias | 3-(2-chloro-6-methylphenyl)-7-[2-methoxy-4-(1-methylpiperidin-4-yl)anilino]-1-(5-methoxypyridin-2-yl)-4H-pyrimido[4,5-d]pyrimidin-2-one | ||
| CAS number | 1936529-65-5 | molecular formula | C32H34ClN7O3 |
| molecular weight | 600.11 g/mol | Exact mass | ≥98% |
| PSA | 96.000 Ų | logp | 6.293 |
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