1173022-21-3

Basic information

• Product Name: STO-609 (acetate)
• Synonyms: CS-2405;PubChem ID: 16760660;STO-609;STO 609;STO609;7-oxo-7H-benzo[de]benzo[4,5]imidazo[2,1-a]isoquinoline-3-carboxylic acid;7H-Benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid, 7-oxo-, acetate (1:1);7-Oxo-7H-benzo[de]benzo[4,5]imidazo[2,1-a]isoquinoline-3-carboxylic Acid Acetate (1:1)
• CAS NO: 1173022-21-3
• Molecular Formula: C21H14N2O5
• Molecular Weight: 374.34626
• EINECS: 604-604-1
• Mol File: 1173022-21-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Storage Temp.: 2-8°C
• Solubility: Soluble in DMSO (up to 10 mg/ml).
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
• CAS DataBase Reference: STO-609 (acetate)(CAS DataBase Reference)
• NIST Chemistry Reference: STO-609 (acetate)(1173022-21-3)
• EPA Substance Registry System: STO-609 (acetate)(1173022-21-3)

Safety Data

• Hazardous Substances Data: 1173022-21-3(Hazardous Substances Data)

Usage

Description

STO-609 (acetate) is a selective inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (CaMKK) isoforms CaMKKα and CaMKKβ, with Ki values of 80 and 15 ng/ml respectively. It binds to the ATP-binding site and displays greater than 80-fold selectivity over other kinases such as CaMK1, CaMK2, CaMK4, MLCK, PKC, PKA, and p42 MAPK. This makes it an important tool for probing distinct CaMK pathways in LTP. Additionally, STO-609 reduces tumorigenicity of liver cancer cells in vivo, reduces the activation of AMP-activated protein kinase (AMPK) by ionomycin in a dose-dependent manner, reduces starvation-induced autophagosomal membrane formation, reverses age-associated decline in bone mass, stimulates osteoblast formation, and inhibits osteoclast differentiation.

Uses

Used in Pharmaceutical Research:
STO-609 (acetate) is used as a cell-permeable inhibitor of calcium/calmodulin-dependent kinase kinases (CaMKK) isoforms CaMKKα and CaMKKβ for evaluating the action of these isoforms both in vitro and in cells.
Used in Cancer Research:
STO-609 (acetate) is used as a compound to reduce tumorigenicity of liver cancer cells in vivo, providing insights into the role of CaMKK isoforms in cancer progression.
Used in Autophagy Research:
STO-609 (acetate) is used as a reagent to reduce starvation-induced autophagosomal membrane formation, aiding in the study of autophagy mechanisms and their regulation.
Used in Bone Health Research:
STO-609 (acetate) is used as a compound to reverse age-associated decline in bone mass, stimulate osteoblast formation, and inhibit osteoclast differentiation, contributing to the understanding of bone health and age-related bone loss.

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).

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