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Spautin-1

Catalog No. T1937 CAS 1262888-28-7

Synonyms: Spautin 1

Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03 μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.

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Spautin-1, CAS 1262888-28-7

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Purity: 98%

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Description	Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03 μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
Targets&IC50	K562:1.03 μM
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]
In vivo	Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. The treatment of Spautin-1 can ameliorate the inflammation damage induced by cerulein, like edema, degeneration, coagulative necrosis and infiltration of inflammatory cells[5].
Kinase Assay	Kinase inhibitory assays in Vitro: The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802.
Cell Research	Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1x105/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi?nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a microplate reader[1].

Synonyms	Spautin 1
Molecular Weight	271.26
Formula	C15H11F2N3
CAS No.	1262888-28-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 27.1 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Liu J, et al. Cell. 2011, 147(1), 223-234. 2. Salabei JK, et al. Biochem J. 2013, 451(3), 375-388. 3. Shao S, et al. Int J Oncol. 2014, 44(5), 1661-1668. 4. Mateo R, et al. J Virol. 2013, 87(3), 1312-1321. 5. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22. 6. Yuan T, Chen Z, Yan F, et al. Deubiquitinating Enzyme USP10 Promotes Hepatocellular Carcinoma Metastasis through Deubiquitinating and Stabilizing Smad4 Protein[J]. Molecular oncology. 2020, 14(1): 197-210

Citations

1. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 2. Yuan T, Chen Z, Yan F, et al. Deubiquitinating Enzyme USP10 Promotes Hepatocellular Carcinoma Metastasis through Deubiquitinating and Stabilizing Smad4 Protein. Molecular Oncology. 2020, 14(1): 197-210

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Spautin-1 1262888-28-7 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Spautin 1 inhibit Spautin1 Inhibitor inhibitor

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