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YKL-05-099

產(chǎn)品活性：YKL-05-099 是一種鹽誘導(dǎo)型激酶 (SIK) 抑制劑。YKL-05-099 作用于SIK1 和 SIK3，IC₅₀ 分別約為 10 和 30 nM。YKL-05-099 抑制 SIK2 的活性稍低，IC₅₀ 值為 40 nM。

研究領(lǐng)域：Immunology/Inflammation

作用靶點(diǎn)：Salt-inducible Kinase (SIK)

In Vitro: 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.

In Vivo: 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 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.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Pyroptosis Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  ARN-3236  |  MR22  |  Phanginin A  |  HG-9-91-01  |  RSS0680  |  YKL-06-062  |  MRIA9  |  DB1113  |  Pterosin B  |  WH-4-025  |  DB0614  |  MRT199665  |  YKL-06-061  |  GLPG3970

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