TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the Ki values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC50 values are 0.63 μM and 0.96 μM, respectively.
TIM-063 (0-29 μM, 6 h) dose-dependently inhibits endogenous CaMKK activity in HeLa cells and also inhibits CaMKK isoform-catalyzed phosphorylation of CaMKIV in transfected COS-7 cells[1].
References:
[1]. Satomi Ohtsuka, et al. Development and Characterization of Novel Molecular Probes for Ca2+/Calmodulin-Dependent Protein Kinase Kinase, Derived from STO-609. Biochemistry. 2020 May 5;59(17):1701-1710.