受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
|
化学式 | C19H10N2O3 |
|||
分子量 | 314.29 | CAS No. | 52029-86-4 | |
Solubility (25°C)* | 体外 | DMSO | 2 mg/mL (6.36 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy. |
---|---|
in vitro | STO-609 inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV). In transfected HeLa cells, STO-609 suppresses the Ca2+-induced activation of CaM-KIV in a dose-dependent manner. STO-609 can permeate cells and is a competitive inhibitor of ATP[1]. |
in vivo | In vivo administration of STO-609 results in increased osteoblasts and diminished osteoclasts, conferring significant protection from ovariectomy (OVX)-induced osteoporosis in adult mice[2]. ICV administration of STO-609 in vivo did not affect the counterregulatory responses to neuroglucopenia and AMPK activation induced by glucopenia[3]. |
細胞アッセイ | 細胞株 | HeLa cells |
---|---|---|
濃度 | 0.01-10 μg/ml | |
反応時間 | 6 h | |
実験の流れ | 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. |
|
動物実験 | 動物モデル | WT, Camkk2−/− and Camk4−/− mice (all in C57BL/6 background) |
投薬量 | 10 μmol/kg | |
投与方法 | i.p. |
Amino acid starvation-induced LDLR trafficking accelerates lipoprotein endocytosis and LDL clearance [ EMBO Rep, 2022, e53373] | PubMed: 34994492 |
Nuclear UHRF1 is a gate-keeper of cellular AMPK activity and function [ Cell Res, 2021, 10.1038/s41422-021-00565-y] | PubMed: 34561619 |
Vitamin D-VDR (vitamin D receptor) regulates defective autophagy in renal tubular epithelial cell in streptozotocin-induced diabetic mice via the AMPK pathway [ Autophagy, 2021, 1-14] | PubMed: 34432556 |
Elaiophylin reduces body weight and lowers glucose levels in obese mice by activating AMPK [ Cell Death Dis, 2021, 12(11):972] | PubMed: 34671010 |
Inhibition of autophagy by CRMP2-derived peptide ST2-104 (R9-CBD3) via a CaMKKβ/AMPK/mTOR pathway contributes to ischemic postconditioning-induced neuroprotection against cerebral ischemia-reperfusion injury [ Mol Brain, 2021, 14(1):123] | PubMed: 34362425 |
Inhibition of Protein Synthesis Induced by CHK1 Inhibitors Discriminates Sensitive from Resistant Cancer Cells [ ACS Pharmacol Transl Sci, 2021, 4(4):1449-1461] | PubMed: 34423276 |
Orexin A alleviates neuroinflammation via OXR2/CaMKKβ/AMPK signaling pathway after ICH in mice [ J Neuroinflammation, 2020, 17(1):187] | PubMed: 32539736 |
Artesunate reverses LPS tolerance by promoting ULK1-mediated autophagy through interference with the CaMKII-IP3R-CaMKKβ pathway [ Int Immunopharmacol, 2020, 87:106863] | PubMed: 32759048 |
Coniferaldehyde ameliorates the lipid and glucose metabolism in palmitic acid-induced HepG2 cells via the LKB1/AMPK signaling pathway [ J Food Sci, 2020, 85(11):4050-4060] | PubMed: 33037652 |
Coniferaldehyde ameliorates the lipid and glucose metabolism in palmitic acid-induced HepG2 cells via the LKB1/AMPK signaling pathway [ J Food Sci, 2020, 85(11):4050-4060] | PubMed: 33037652 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。