STO-609

카탈로그 번호S8274 배치:S827402

인쇄

기술 자료

화학식

C₁₉H₁₀N₂O₃

분자량

314.29

CAS 번호

52029-86-4

용해도 (25°C)*

시험관 내(In vitro)

DMSO

3 mg/mL (9.54 mM)

Water

Insoluble

Ethanol

Insoluble

생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)

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 Selleck 연구소에서 검증했습니다. 이 제형에 대한 조정이 필요한 경우 맞춤형 테스트를 위해 당사 영업팀에 문의하십시오.	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 Selleck 연구소에서 검증했습니다. 이 제형에 대한 조정이 필요한 경우 맞춤형 테스트를 위해 당사 영업팀에 문의하십시오.	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/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명

STO-609는 재조합 CaM-KKα 및 CaM-KKβ isoform의 활성을 Ki 값 80 및 15 ng/ml로 각각 억제하고, 자가인산화 활성도 억제하는 Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK)의 특이적 억제제입니다. 이 화합물은 AMPKK 활성을 억제하고 autophagy를 억제합니다.

표적

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

시험관 내(In vitro)

STO-609는 재조합 CaM-KKα 및 CaM-KKβ 동형의 활성을 각각 80 및 15ng/ml의 Ki 값으로 억제하며, 자가인산화 활성도 억제합니다. 이 화합물은 CaM-KK에 대해 높은 선택성을 가지며 하위 CaM 키나아제(CaM-KI 및 -IV)에는 유의미한 영향을 미치지 않습니다. 형질감염된 HeLa 세포에서 이 화학물질은 Ca²⁺ 유도 CaM-KIV 활성화를 용량 의존적으로 억제합니다. 이는 세포를 투과할 수 있으며 ATP의 경쟁적 억제제입니다.

생체 내(In Vivo)

STO-609의 생체 내 투여는 골아세포를 증가시키고 파골세포를 감소시켜 성체 쥐의 난소절제술(OVX) 유발 골다공증으로부터 상당한 보호 효과를 부여합니다. 이 화합물의 생체 내 ICV 투여는 신경글루코페니아 및 글루코페니아 유발 AMPK 활성화에 대한 역조절 반응에 영향을 미치지 않았습니다.

프로토콜 (참조)

세포 분석:^{^[1]}	세포주 HeLa cells 농도 0.01-10 μg/ml 배양 시간 6 h 방법 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.
동물 연구:^{^[2]}	동물 모델 WT, Camkk2−/− and Camk4−/− mice (all in C57BL/6 background) 용량 10 μmol/kg 투여 i.p.

세포 분석:^{^[1]}

세포주
HeLa cells
농도
0.01-10 μg/ml
배양 시간
6 h
방법
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.

동물 연구:^{^[2]}

동물 모델
WT, Camkk2−/− and Camk4−/− mice (all in C57BL/6 background)
용량
10 μmol/kg
투여
i.p.

참조

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/

펼치기

Sellecks STO-609 인용됨 23 출판물

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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