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YKL-05-099 Chemical Structure

YKL-05-099

Data Sheet For research use only. Not for human use.
Cat. No. :BCP20631CAS No. :1936529-65-5Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 1936529-65-5 Cat. No. BCP20631
Name YKL-05-099
Synonyms YKL 05 099; YKL05099;
SMILES
Chemical Name
Formula C32H34ClN7O3 M. Wt 600.11
Purity 98% Storage Store at 4-8°C
Description YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM) and IL-10-enhancing activities (EC50=460 nM). YKL-05-099 binds to SIK1 and SIK3 with IC50s of 10 and 30 nM, respectively, in a competitive binding assay. Preincubating bone marrow-derived macrophages with YKL-05-099 reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259. YKL-05-099 suppresses production of the inflammatory cytokines TNFα, IL-6 and IL-12p40, and only modestly enhances IL-1β release in BMDCs stimulated with the yeast cell wall extract Zymosan A[1].YKL-05-099 is non-toxic at concentrations less than 10 μM and stable in mouse liver microsomes for more than 2 hours. YKL-05-099 is highly soluble (PBS solubility=428 μM) and present in an unbound state at appreciable levels in mouse plasma. YKL-05-099 dose dependently decreases phosphorylation of HDAC5 at the SIK-regulated site Ser259; reduced phosphorylation is observed at the lowest dose (5 mg/Kg) and is below the limit
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