STO-609

N.º de catálogoS8274 Lote:S827402

Imprimir

Datos técnicos

Fórmula

C₁₉H₁₀N₂O₃

Peso molecular

314.29

Número CAS

52029-86-4

Solubilidad (25°C)*

In vitro

DMSO

3 mg/mL (9.54 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Agregue los solventes al producto individualmente y en orden.)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, póngase en contacto con nuestro equipo de ventas para pruebas personalizadas.	0.150mg/ml (0.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, póngase en contacto con nuestro equipo de ventas para pruebas personalizadas.	0.075mg/ml (0.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 1.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción

STO-609 es un inhibidor específico de la Ca2+/Calmodulin-dependent protein kinase kinase (CaM-KK) que inhibe las actividades de las isoformas recombinantes CaM-KKα y CaM-KKβ, con valores de Ki de 80 y 15 ng/ml, respectivamente, y también inhibe sus actividades de autofosforilación. Este compuesto inhibe la actividad de la AMPKK e inhibe la autophagy.

Objetivos

AMPK	CaM-KKβ (Cell-free assay)	CaM-KKα (Cell-free assay)
	47 nM(Ki)	0.25 μM(Ki)

In vitro

STO-609 inhibe las actividades de las isoformas recombinantes CaM-KKα y CaM-KKβ, con valores de Ki de 80 y 15 ng/ml, respectivamente, y también inhibe sus actividades de autofosforilación. Este compuesto es altamente selectivo para CaM-KK sin ningún efecto significativo sobre las CaM quinasas aguas abajo (CaM-KI y -IV). En células HeLa transfectadas, este químico suprime la activación de CaM-KIV inducida por Ca²⁺ de manera dosis-dependiente. Puede permear las células y es un inhibidor competitivo de ATP.

In vivo

La administración in vivo de STO-609 resulta en un aumento de osteoblastos y una disminución de osteoclastos, confiriendo una protección significativa contra la osteoporosis inducida por ovariectomía (OVX) en ratones adultos. La administración ICV de este compuesto in vivo no afectó las respuestas contrarreguladoras a la neuroglucopenia y la activación de AMPK inducida por glucopenia.

Protocolo (de referencia)

Ensayo celular:^{^[1]}	Líneas celulares HeLa cells Concentraciones 0.01-10 μg/ml Tiempo de incubación 6 h Método HeLa cells were maintained in Dulbecco's modified Eagle's medium containing 10% fetal bovine serum. Cells were subcultured in 6-cm dishes 12 h before transfection. The cells were then transferred to serum-free medium and treated with a mixture of either 3 g of pME18s plasmid DNA or 3 g of HA(hemagglutinin-tagged)-CaM-KIV and 20 μg of LipofectAMINE reagent in 2.5 ml of medium. After 20 h of incubation, the cells were further cultured in serum-free medium for 6 h in either the absence or presence of various concentrations of STO-609 (0.01-10 μg/ml in Me₂SO at a final concentration of 0.5%) and then treated with or without 1 μM ionomycin for 5 min. Stimulation was terminated by the addition of 1 ml of lysis buffer, 2 mM EDTA, 2 mM EGTA, 1% Nonidet P-40, 10% glycerol, 0.2 mM phenylmethylsulfonyl fluoride, 10 mg/liter leupeptin, 10 mg/liter trypsin inhibitor, and 1 μM microcystin LR), and the cells were lysed for 30min on ice. The cell extract was collected and centrifuged at 15,000×g for 15 min, the supernatant was precleared with 40 μl of Protein G-Sepharose for 2h at 4 °C, and the supernatant was mixed with 4 g of anti-HA antibody for 3h. 40 μl of Protein G-Sepharose was then applied to the extract and incubated overnight. The immunoprecipitated resin was washed three times with 1 ml of the lysis buffer and then washed with 1 ml of kinase buffer. Protein G-Sepharose with immunoprecipitated HA-CaM-KIV was subjected to the protein kinase assay in the presence of 1 mM EGTA using syntide-2 as a substrate.
Estudio en animales:^{^[2]}	Modelos animales WT, Camkk2−/− and Camk4−/− mice (all in C57BL/6 background) Dosificaciones 10 μmol/kg Administración i.p.

Ensayo celular:^{^[1]}

Líneas celulares
HeLa cells
Concentraciones
0.01-10 μg/ml
Tiempo de incubación
6 h
Método
HeLa cells were maintained in Dulbecco's modified Eagle's medium containing 10% fetal bovine serum. Cells were subcultured in 6-cm dishes 12 h before transfection. The cells were then transferred to serum-free medium and treated with a mixture of either 3 g of pME18s plasmid DNA or 3 g of HA(hemagglutinin-tagged)-CaM-KIV and 20 μg of LipofectAMINE reagent in 2.5 ml of medium. After 20 h of incubation, the cells were further cultured in serum-free medium for 6 h in either the absence or presence of various concentrations of STO-609 (0.01-10 μg/ml in Me₂SO at a final concentration of 0.5%) and then treated with or without 1 μM ionomycin for 5 min. Stimulation was terminated by the addition of 1 ml of lysis buffer, 2 mM EDTA, 2 mM EGTA, 1% Nonidet P-40, 10% glycerol, 0.2 mM phenylmethylsulfonyl fluoride, 10 mg/liter leupeptin, 10 mg/liter trypsin inhibitor, and 1 μM microcystin LR), and the cells were lysed for 30min on ice. The cell extract was collected and centrifuged at 15,000×g for 15 min, the supernatant was precleared with 40 μl of Protein G-Sepharose for 2h at 4 °C, and the supernatant was mixed with 4 g of anti-HA antibody for 3h. 40 μl of Protein G-Sepharose was then applied to the extract and incubated overnight. The immunoprecipitated resin was washed three times with 1 ml of the lysis buffer and then washed with 1 ml of kinase buffer. Protein G-Sepharose with immunoprecipitated HA-CaM-KIV was subjected to the protein kinase assay in the presence of 1 mM EGTA using syntide-2 as a substrate.

Estudio en animales:^{^[2]}

Modelos animales
WT, Camkk2−/− and Camk4−/− mice (all in C57BL/6 background)
Dosificaciones
10 μmol/kg
Administración
i.p.

Referencias

https://pubmed.ncbi.nlm.nih.gov/11867640/
https://pubmed.ncbi.nlm.nih.gov/23408651/
https://pubmed.ncbi.nlm.nih.gov/17687000/

https://pubmed.ncbi.nlm.nih.gov/15980064/

Expandir

Sellecks STO-609 Ha sido citado por 23 Publicaciones

Artemisinin protected human bronchial epithelial cells from amiodarone-induced oxidative damage via 5'-AMP-activated protein kinase (AMPK) activation [ Redox Rep, 2025, 30(1):2447721]	PubMed: 39803706
Piezo1 regulates autophagy in HT22 hippocampal neurons through the Ca2+/Calpain and Calcineurin/TFEB signaling pathways [ PLoS One, 2025, 20(8):e0330282]	PubMed: 40857264
A highland-adaptation variant near MCUR1 reduces its transcription and attenuates erythrogenesis in Tibetans [ Cell Genom, 2025, 5(3):100782]	PubMed: 40043709
Mechanical regulation of lipid and sugar absorption by Piezo1 in enterocytes [ Acta Pharm Sin B, 2024, 14(8):3576-3590]	PubMed: 39220873
Targeting Dlat-Trpv3 pathway by hyperforin elicits non-canonical promotion of adipose thermogenesis as an effective anti-obesity strategy [ J Adv Res, 2024, S2090-1232(24)00555-1]	PubMed: 39631519
Mechano-regulation of GLP-1 production by Piezo1 in intestinal L cells [ Elife, 2024, 13RP97854]	PubMed: 39509292
Artemisinin conferred cytoprotection to human retinal pigment epithelial cells exposed to amiodarone-induced oxidative insult by activating the CaMKK2/AMPK/Nrf2 pathway [ J Transl Med, 2024, 22(1):844]	PubMed: 39285426
Aβ25-35-induced autophagy and apoptosis are prevented by the CRMP2-derived peptide ST2-104 (R9-CBD3) via a CaMKKβ/AMPK/mTOR signaling hub [ PLoS One, 2024, 19(9):e0309794]	PubMed: 39325788
Mechanical activation of VE-cadherin stimulates AMPK to increase endothelial cell metabolism and vasodilation [ bioRxiv, 2024, 2024.05.09.593171]	PubMed: 38798670
Highly expressed SERCA2 triggers tumor cell autophagy and is a druggable vulnerability in triple-negative breast cancer [ Acta Pharm Sin B, 2022, 12(12):4407-4423]	PubMed: 36561988

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