Spautin-1

製品コードS7888 バッチS788801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H11F2N3
分子量 271.26 CAS No. 1262888-28-7
Solubility (25°C)* 体外 DMSO 40 mg/mL (147.46 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）
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 40% PEG 300 5%Tween80 50%H2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.000mg/ml (7.37mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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 make it clear; 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. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro

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, this compound 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, it markedly inhibits IM-induced autophagy by downregulating Beclin-1, and enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β. [3] This chemical also specifically reduces infectious dengue virus titers in BHK-21 cells. [4]

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Deubiquitination Assay
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/21962518/
  • https://pubmed.ncbi.nlm.nih.gov/23421427/
  • https://pubmed.ncbi.nlm.nih.gov/24585095/
  • https://pubmed.ncbi.nlm.nih.gov/23175363/

カスタマーフィードバック

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. ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Increased DNA damage in full-grown oocytes is correlated with diminished autophagy activation [ Nat Commun, 2024, 15(1):9463] PubMed: 39487138
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
Macroautophagy/autophagy promotes resistance to KRASG12D-targeted therapy through glutathione synthesis [ Cancer Lett, 2024, 604:217258] PubMed: 39276914
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
Matrine induces autophagic cell death by triggering ROS/AMPK/mTOR axis and apoptosis in multiple myeloma [ Biomed Pharmacother, 2024, 175:116738] PubMed: 38759291
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
Beclin-1-dependent autophagy, but not apoptosis, is critical for stem-cell-mediated endometrial programming and the establishment of pregnancy [ Dev Cell, 2023, 58(10):885-897.e4] PubMed: 37040770
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

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。

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