Spautin-1 | Autophagy inhibitor | CAS 1262888-28-7

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Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	CXCR Nrf2 Mitophagy LRRK2 ULK FKBP Heme Oxygenase cGAS LC3 Cell wall
Other Autophagy Inhibitors	Resveratrol (trans-Resveratrol) PIK-III DC661 Lys05 Autophinib SMER28 EAD1 Flubendazole EN6 ROC-325

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	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

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (199.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
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.
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 1 40% PEG 300 2 5%Tween80 3 50%H2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	271.26	Formula	C₁₅H₁₁F₂N₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1262888-28-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC=C1CNC2=NC=NC3=C2C=C(C=C3)F)F

Mechanism of Action

Targets/IC₅₀/Ki	USP10 (Cell-free assay) 0.5779 μM USP13 (Cell-free assay) 0.6916 μM
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. 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. 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. This chemical also specifically reduces infectious dengue virus titers in BHK-21 cells.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21962518/ [2] https://pubmed.ncbi.nlm.nih.gov/23421427/ [3] https://pubmed.ncbi.nlm.nih.gov/24585095/ [4] https://pubmed.ncbi.nlm.nih.gov/23175363/

Applications

Methods	Biomarkers	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