受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C15H11F2N3 |
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分子量 | 271.26 | CAS No. | 1262888-28-7 | ||||
Solubility (25°C)* | 体外 | DMSO | 54 mg/mL (199.07 mM) | ||||
Ethanol | 7 mg/mL (25.8 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis. |
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in vitro | In Bcap-37 cells, Spautin-1 dramatically enhanced cell death in glucose-free media and induces apoptotic morphology. In Bax-Bak DKO cells, spautin-1 inhibits etoposide induced autophagic cell death. Spautin-1 promots the degradation of Vps34 complexes by regulating the deubiquitination activity of USP10 and USP13, and reduces the levels of PtdIns3P. [1] In PDGF-treated cells, spautin-1 stabilizes α-smooth muscle cell actin and calponin, prevents actin filament disorganization, diminishes production of extracellular matrix, and abrogates VSMC hyperproliferation and migration. [2] In CML cells, spautin-1 markedly inhibits IM-induced autophagy by downregulating Beclin-1, and enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β. [3] Spautin-1 also specifically reduces infectious dengue virus titers in BHK-21 cells. [4] |
キナーゼアッセイ | In Vitro Deubiquitination Assay | |
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Ubiquitinated Beclin1 is isolated from 293T cells transfected with expression vectors for HA-UB and FLAG-Beclin1. After Incubation with proteasome inhibitor MG132 (25 μM) and a pan DUB inhibitor G5 (25 μM) for 6 hr, ubiquitinated Beclin1 is purified from the cell extracts with anti-FLAG-affinity column in FLAG-lysis buffer (50 mM Tris-HCl [pH 7.8], 137 mM NaCl, 10mM NaF, 1 mM EDTA, 1% Triton X-100, 0.2% Sarcosyl, 1 mM DTT, 10% glycerol and fresh proteinase inhibitors). After extensive washing with the FLAG-lysis buffer, the proteins are eluted with FLAG-peptides. The recombinant Flag-USP10 and USP10CA are expressed in 293T cells and purified using FLAG affinity column and eluted with FLAG-peptide. For in vitro deubiquitination assay, ubiquitinated Beclin1 protein is incubated with recombinant USP10 in the deubiquitination buffer (50 mM Tris-HCl [pH 8.0], 50 mM NaCl, 1 mM EDTA, 10mM DTT, 5% glycerol) for 2 hr at 37°C. |
Data from [Data independently produced by , , Cancer Lett, 2018, 425:1-12]
Data from [Data independently produced by , , J Hematol Oncol, 2016, 9(1):45]
Data from [Data independently produced by , , Int J Cancer, 2015, 136(11):2717-29. ]
HSPA12A acts as a scaffolding protein to inhibit cardiac fibroblast activation and cardiac fibrosis [ J Adv Res, 2024, S2090-1232(24)00025-0] | PubMed: 38219869 |
The critical role of RAGE in severe influenza infection: A target for control of inflammatory response in the disease [ Clin Immunol, 2024, 262:110178] | PubMed: 38460892 |
USP13 drives lung squamous cell carcinoma by switching lung club cell lineage plasticity [ Mol Cancer, 2023, 22(1):204] | PubMed: 38093367 |
TRPV1 inhibition overcomes cisplatin resistance by blocking autophagy-mediated hyperactivation of EGFR signaling pathway [ Nat Commun, 2023, 14(1):2691] | PubMed: 37165076 |
Compensatory cross-talk between autophagy and glycolysis regulates senescence and stemness in heterogeneous glioblastoma tumor subpopulations [ Acta Neuropathol Commun, 2023, 11(1):110] | PubMed: 37420311 |
Upregulation of the EGFR/MEK1/MAPK1/2 signaling axis as a mechanism of resistance to antiestrogen‑induced BimEL dependent apoptosis in ER+ breast cancer cells [ Int J Oncol, 2023, 62(2)20] | PubMed: 36524361 |
RTN4/Nogo-A-S1PR2 negatively regulates angiogenesis and secondary neural repair through enhancing vascular autophagy in the thalamus after cerebral cortical infarction [ Autophagy, 2022, 1-20] | PubMed: 35263212 |
Carbon dots enhance extracellular matrix secretion for dentin-pulp complex regeneration through PI3K/Akt/mTOR pathway-mediated activation of autophagy [ Mater Today Bio, 2022, 16:100344] | PubMed: 35833197 |
USP13 promotes development and metastasis of high-grade serous ovarian carcinoma in a novel mouse model [ Oncogene, 2022, 41(13):1974-1985] | PubMed: 35173307 |
USP13 promotes development and metastasis of high-grade serous ovarian carcinoma in a novel mouse model [ Oncogene, 2022, 41(13):1974-1985] | PubMed: 35173307 |
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。