1936529-65-5

YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM)[1].

Potent and selective salt-inducible kinases (SIK1SIK2SIK3) inhibitor in vitro and in vivo.



YKL-05-099 is a potent and selective salt-inducible kinases inhibitor (SIK1/2/3 IC50 = 10/40/30 nM) with superior pharmacokinetic properties than HG-9-91-01. YKL-05-099 pre-treatment of murine BDMCs up-regulates Zymosan A-stimulated IL-10 (EC50 = 460 nM with 24h )while suppresses inflammatory cytokines production (TNFαIL-6 and IL-12p40). LikewiseYKL-05-099 intraperitoneal administration in mice (20 mg/kg i.p.) 15 min prior to LPS (0.5 mg/kg i.p.) enhances serum IL-10while reduces HDAC5 pSer259 levels in total splenic leukocytes and serum TNFα level in vivo.

SIK1; SIK3

Store at -20°C

[1] Sundberg TB, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 Aug 19;11(8):2105-11. DOI:10.1021/acschembio.6b00217