Spautin-1

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.

Spautin-1 Chemical Structure

Spautin-1 Chemical Structure

CAS No. 1262888-28-7

Purity & Quality Control

Spautin-1 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Click to View More Cell Line Experimental Data

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. Spautin-1 enhances apoptosis.
Targets
USP10 [1]
(Cell-free assay)
USP13 [1]
(Cell-free assay)
0.5779 μM 0.6916 μM
In vitro
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, 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]

Experimental Result Images Methods Biomarkers Images PMID
Western blot CDK4 / CDK2 / Cyclin D1 / p15 / p21 p-JNK / JNK / p-ERK / ERK / p-p38 / p38 p-MKK4 / MKK4 / p-MEK / MEK / p-EGFR / EGFR USP10 / SKP2 / P27 / p-Bcr-Abl / Bcr-Abl / p-Crkl / Crkl / p-STAT5 / STAT5 30975171
Immunofluorescence p-JNK / p-ERK Glut1 30975171
Growth inhibition assay Cell viability 30975171

Chemical Information & Solubility

Molecular Weight 271.26 Formula

C15H11F2N3

CAS No. 1262888-28-7 SDF Download Spautin-1 SDF
Smiles C1=CC(=CC=C1CNC2=NC=NC3=C2C=C(C=C3)F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (199.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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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

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