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YKL-05-099

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YKL-05-099
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Cat #: V2134 CAS #: 1936529-65-5 Purity ≥ 98%

Description: YKL-05-099 (YKL05099) is a novel, potent and selective inhibitor of salt-inducible kinase (SIK) with the potential to be used for treatment of inflammatory disorders. YKL-05-099 acts by binding to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM). SIKs are promising therapeutic targets for modulating cytokine responses during innate immune activation.

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CAS No.1936529-65-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
ProtocolIn VitroYKL-05099 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].
In VivoYKL-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 of detection by immunoblotting beginning at the 20 mg/Kg dose. YKL-05-099 dose-dependently reduces abundance of TNFα in serum beginning at 5 mg/Kg, and increases IL-10 levels at the 20 mg/Kg dose by more than 2-fold[1].
These protocols are for reference only. InvivoChem does not independently validate these methods.
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