Spautin-1

Catalog No.S7888

Spautin-1 Chemical Structure

Molecular Weight(MW): 271.26

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.

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USD 447 In stock
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Cited by 4 Publications

4 Customer Reviews

  • Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.

    Cancer Lett, 2018, 425:1-12. Spautin-1 purchased from Selleck.

    Autophagosomal inhibition was performed in 32D EV, WT CALR, del52, and ins5 expressing cells. The 32D cell lines were treated with the inhibitor spautin-1 for the indicated time. Lysates were prepared, and SDS-PAGE and Western blotting were performed. Antibodies detecting mutated CALR (CALR mut), CALR, LC3I-II, and GAPDH were used for immunostaining. LC3I-II served as control for successful autophagosomal inhibition.

    J Hematol Oncol, 2016, 9(1):45. Spautin-1 purchased from Selleck.

  • (c) PC-9G cells were treated with BIBW2992 (250 nM) or WZ4002 (15 nM) plus SAHA (2 mM) with or without spautin-1 (20 mM) for 24 hr. The cell lysates were harvested and the indicated proteins were analyzed by Western blotting.

    Int J Cancer, 2015, 136(11):2717-29. . Spautin-1 purchased from Selleck.

    Male C57BL/6 mice (n = 8 for each group) were instilled intratracheally with normal saline (NS), PM (100 μg/d), spautin-1 (0.5 mg/d), or PM plus spautin-1 respectively for 2 days, and after 24 h, representative images of lung tissue stained with H&E

    Toxicol Lett, 2017, 280:206-212. Spautin-1 purchased from Selleck.

Purity & Quality Control

Choose Selective Autophagy Inhibitors

Biological Activity

Description 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.
Targets
USP10 [1]
(Cell-free assay)
USP13 [1]
(Cell-free assay)
0.5779 μM 0.6916 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]

Assay
Methods Test Index PMID
Western blot
CDK4 / CDK2 / Cyclin D1 / p15 / p21 ; 

PubMed: 30975171     


Western blot analysis was performed to detect the expression of CDK4, CDK2, Cyclin D1, P15 and P21 in PCa cells exposed to various doses of Spautin-1 (0, 5, 10, 20 μM) for 24 h (left), or Spautin-1 (10 μM) at various lengths of time (Right).

p-JNK / JNK / p-ERK / ERK / p-p38 / p38 ; 

PubMed: 30975171     


Western blot analysis was performed to detect the expression of phosphor-JNK, JNK, phosphorylated ERK (P-ERK), ERK, P-P38 and P38 in PCa cells exposed to various doses of Spautin-1 (0, 5, 10, 20 μM) for 24 h (left), or Spautin-1 (20 μM) at various time points (Right). 

p-MKK4 / MKK4 / p-MEK / MEK / p-EGFR / EGFR ; 

PubMed: 30975171     


Western blot analysis was performed to detect the expression of P-MKK4, MKK4, P-MEK1/2, MEK1/2 P-EGFR(Y1068), P-EGFR(Y1173) and pan-EGFR in 22Rv1 and PC3 cells exposed to Spautin-1 (20 μM) for the indicated duration.

USP10 / SKP2 / P27 / p-Bcr-Abl / Bcr-Abl / p-Crkl / Crkl / p-STAT5 / STAT5 ; 

PubMed: 31044085     


Western blot assay of indicated cell lines post Spautin-1 treatment for 48 h.

30975171 31044085
Immunofluorescence
p-JNK / p-ERK ; 

PubMed: 30975171     


b Immunofluorescence microscopy was performed to detect the expression and subcellular location of phospho-JNK and d phospho-ERK in 22Rv1 and PC3 cells exposed to Spautin-1 for 6 h. Scale bars represent 50 μm.

Glut1; 

PubMed: 30975171     


Immunofluorescence microscopy were performed to detect the expression of Glut1 in PCa cells treated with Spautin-1 for 24 h. 

30975171
Growth inhibition assay
Cell viability; 

PubMed: 30975171     


Cell viability assay was performed in LNCaP, 22Rv1, C4–2, PC3 and DU145 PCa cells post various concentrations of Spautin-1 treatment for indicated hours. 

30975171

Protocol

Solubility (25°C)

In vitro DMSO 54 mg/mL (199.07 mM)
Ethanol 7 mg/mL (25.8 mM)
Water 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.

Chemical Information

Molecular Weight 271.26
Formula

C15H11F2N3

CAS No. 1262888-28-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID