TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.
TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.
TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.
TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.
TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells.
TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.
