STO-609 is a selective and cell-permeable inhibitor of Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), exhibiting Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. It inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates (IC50 ~0.02 g/ml) and is highly selective for CaM-KK, with no significant effect on downstream CaM-KI and -IV. It also inhibits both constitutively active and wild-type CaM-KKα, and suppresses Ca2+-induced activation of CaM-KIV. The inhibition mechanism is ATP-competitive.
- Selective and cell-permeable CaM-KK inhibitor.
- Inhibits AMPKK activity.
- High selectivity for CaM-KK.
- Suppresses Ca2+-induced activation of CaM-KIV.
- ATP-competitive inhibition mechanism.