YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively
YKL-05-099 displays increased SIK selectivity and enhanced pharmacokinetic properties compared with HG-9-91-01.
YKL-05-099 reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259, increases expression of the CREB target genes Il10 and Nurr77, suppresses production of TNFα, IL-6 and IL-12p40 in BMDMs.
YKL-05-099 is a useful probe to investigate SIK function in vivo.
