YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 of 6.56/1.77/20.5 nM for SIK1/2/3, respectively.
YKL-06-061 inhibits only one kinase FRK (IC50=1.1 nM), more strongly than SIKs, in a panel of 468 human kinases.
YKL-06-061 dose-dependently increases MITF mRNA expression in human melanoma cells.
YKL-06-061 induces significant pigmentation in Mc1r-deficient mice and normal human skin.
