STO-609 (acetate)

Description

STO-609 (1173022-21-3) is a selective inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki = 80 and 15 ng/ml for inhibition of CaM-KKα and CaM-KKβ respectively).1 Binds to the? ATP-binding site.2 Displays > 80-fold selectivity over CaMK1, CaMK2, CaMK4, MLCK, PKC, PKA and p42 MAPK. Important tool for probing distinct CaMK pathways in LTP.3 Reduces starvation-induced autophagosomal membrane formation.4 Reverses age-associated decline in bone mass.5 Stimulates osteoblast formation, inhibits osteoclast differentiation.6

The Uses of STO-609 (acetate)

STO-609 is a cell-permeable inhibitor of calcium/calmodulin-dependent kinase kinases (CaMKK) isoforms CaMKKα and CaMKKβ. It is used to evaluate the action of CaMKK isoforms both in vitro and in cells.

What are the applications of Application

STO-609 acetate salt is a selective CaMKK inhibitor

General Description

STO-609 reduces tumorigenicity of liver cancer cells in vivo. TO-609 reduces the activation of AMP (adenosine monophosphate)-activated protein kinase (AMPK) by ionomycin in a dose dependant manner.

Biochem/physiol Actions

Selective Ca2+/Calmodulin-dependent protein kinase kinase (CaM-KK) antagonist. Inhibits CamKKa and CaMKKb with Ki = 80 and 15 ng/mL, respectively. Does not inhibit downstream CaM kinases (CaMKI and CaMKIV).

storage

Room temperature (desiccate)

References

1) Tokumitsu?et al. (2002), STO-609, a Specific Inhibitor of the Ca2+/Calmodulin-dependent Protein Kinase Kinase;?J. Biol. Chem. 277 15813 2) Tokumitsu?et al. (2003) A single amino acid difference between alpha and beta Ca2+/calmodulin-dependent protein kinase kinase dictates sensitivity to the specific inhibitor, STO-609;?J. Biol. Chem. 278 10908 3) Redondo et al. (2010) Synaptic tagging and capture: differential role of distinct calcium/calmodulin kinases in protein synthesis-dependent long-term potentiation;?J. Neurosci. 30 4981 4) Pfisterer et al. (2011) Ca+2/calmodulin –dependent kinase (CaMK) signaling via CaMKI and AMP-activated protein kinase contributes to the regulation of WIPI-1 ar the onset of autophagy; Mol. Pharmacol. 80 1066 5) Pritchard et al. (2015) Inhibition of CaMKK2 reverses age-associated decline in bone mass; Bone, 75 120 6)Cary?et al. (2013) Inhibition of Ca+2/Calmodulin-dependent protein kinase kinase 2 stimulates osteoblast formation and inhibits osteoclast differentiation;?J. Bone Miner. Res. 28 1599 7) Matsukawa et al. (2017) Upregulation of skeletal muscle PGC-1α through the elevation of cyclic AMP levels by Cyanidin-3-glucoside enhances exercise performance; Sci. Rep., 7 44799