GLPBio

STO-609

Catalog No.: GC37694Purity:>98.00%
STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.

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STO-609
Cas No.: 52029-86-4
10mM (in 1mL DMSO)In Stock
$39.00
1
1mgIn Stock
$28.00
1
5mgIn Stock
$56.00
1
10mgIn Stock
$90.00
1
25mgIn Stock
$188.00
1
50mgIn Stock
$301.00
1
100mgIn Stock
$476.00
1

Citations

1 publicationsPublications from researchers using this product

Description

STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively[1]. CaM-KK is a key signal transduction protein that plays an important role in intracellular calcium signal transduction by activating members of the CaM kinase family (such as CaM-KI, CaM-KIV, etc.)[2]. STO-609 is typically used to study CAM-KK-related signaling pathways and their roles in various cellular physiological processes such as cell proliferation, differentiation, metabolism, and neural signal transduction[3][4].

In vitro, treatment of non-functional pituitary adenoma (NFPA) cells with STO-609 (0.4-51.2μM; 24h)significantly inhibits cells proliferation and migration and induces apoptosis in a dose-dependent manner by suppressing the Ca²⁺/CaM signaling pathway[5]. Treatment of insect neurosecretory cells with STO-609 (15μM; 10min) significantly reduced nicotine-induced currents and intracellular calcium levels increase by inhibiting the CaMKK/AMPK pathway[6].

In vivo, STO-609 (30μg/kg; i.p.; twice a week; 3 weeks) significantly reduced the lung weight of mice inhibited experimental lung metastasis in mice with oral squamous cell carcinoma (OSCC) cells overexpressing EP4[7].

References:
[1] Tokumitsu H, Inuzuka H, Ishikawa Y, Ikeda M, Saji I, Kobayashi R. STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J Biol Chem. 2002;277(18):15813-15818.
[2] Tokumitsu H, Sakagami H. Molecular Mechanisms Underlying Ca2+/Calmodulin-Dependent Protein Kinase Kinase Signal Transduction. Int J Mol Sci. 2022;23(19):11025.
[3] York B, Li F, Lin F, et al. Pharmacological inhibition of CaMKK2 with the selective antagonist STO-609 regresses NAFLD. Sci Rep. 2017;7(1):11793.
[4] Fujiwara Y, Hiraoka Y, Fujimoto T, Kanayama N, Magari M, Tokumitsu H. Analysis of Distinct Roles of CaMKK Isoforms Using STO-609-Resistant Mutants in Living Cells. Biochemistry. 2015;54(25):3969-3977.
[5] Wu B, Jiang S, Wang X, et al. Identification of driver genes and key pathways of non-functional pituitary adenomas predicts the therapeutic effect of STO-609. PLoS One. 2020;15(10):e0240230.
[6] Taha M, Houchat JN, Taillebois E, Thany SH. The calcium-calmodulin-dependent protein kinase kinase inhibitor, STO-609, inhibits nicotine-induced currents and intracellular calcium increase in insect neurosecretory cells. J Neurochem. 2024;168(7):1281-1296.
[7] Ishikawa S, Umemura M, Nakakaji R, et al. EP4-induced mitochondrial localization and cell migration mediated by CALML6 in human oral squamous cell carcinoma. Commun Biol. 2024;7(1):567.

Protocol

Cell experiment [1]:

Cell lines

HP75 cells

Preparation Method

HP75 cells were cultured in DMEM containing 15% horse serum, and 2.5% fetal calf serum at 37˚C in an easeful air atmosphere containing 5% carbon dioxide. The cells were seeded into 96-well plates for overnight, and the density is 1.0×105 cells/well. After washing culture medium, different doses of STO-609 were used to the cells and cultured for 24h, control group and solvent control group were classed by using normal saline (NS) and DMSO respectively, and 6 wells were prepared for doses of STO-609 (concentration gradients were 0.4μmol/L, 0.8μmol/L, 1.6μmol/L, 3.2μmol/L, 6.4μmol/L, 12.8μmol/L, 25.6μmol/L and 51.2μmol/L). Cells were cultured for 1h after added CCK-8 into wells with a quantity of 10μl/well. The wave length of 450nm was applied to measure OD value of each well on the microplate reader.

Reaction Conditions

0.4-51.2μM; 24h

Applications

STO-609 significantly inhibits cells proliferation and migration and induces apoptosis in a dose-dependent manner.

Animal experiment [2]:

Animal models

BALB/c Slc-nu/nu mice

Preparation Method

HSC-3 cells transfected with the lentiviral scramble control or EP4 over expression were harvested and injected (2×106cells/0.2mL) into the tail veins of BALB/c Slc-nu/nu mice (female, 4–5 weeks old, 4 mice/group) (SLC). Each group of mice was administered either vehicle (0.1% dimethylsulfoxide in phosphate-buffered saline) or STO-609 by intraperitoneal injection (30μg/kg/body weight) twice per week for 3 weeks. Three weeks after the injection of the cells, the lungs were fixed with formalin, and the weights were measured.

Dosage form

30μg/kg; i.p.; twice per week; 3 weeks

Applications

STO-609 significantly reduced the lung weight of mice.

References:
[1] Wu B, Jiang S, Wang X, et al. Identification of driver genes and key pathways of non-functional pituitary adenomas predicts the therapeutic effect of STO-609. PLoS One. 2020;15(10):e0240230.
[2] Ishikawa S, Umemura M, Nakakaji R, et al. EP4-induced mitochondrial localization and cell migration mediated by CALML6 in human oral squamous cell carcinoma. Commun Biol. 2024;7(1):567

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
52029-86-4
SMILES
O=C(C1=C2C3=C(C4=NC5=CC=CC=C5N4C(C3=CC=C2)=O)C=C1)O
Molecular Formula
C19H10N2O3
Molecular Weight
314.29
Solubility
DMSO: 5.6 mg/mL (17.82 mM and warming); Water: < 0.1 mg/mL (insoluble)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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