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NSC 185058

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Catalog No. T5211Cas No. 39122-38-8
Alias NSC185058

NSC 185058, an inhibitor of ATG4B (a major cysteine protease), can also attenuate autophagic activity.

NSC 185058

NSC 185058

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🥰Excellent
Purity: 99.27%
Catalog No. T5211Alias NSC185058Cas No. 39122-38-8
NSC 185058, an inhibitor of ATG4B (a major cysteine protease), can also attenuate autophagic activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$60In StockIn Stock
5 mg$129In StockIn Stock
10 mg$198In StockIn Stock
25 mg$413In StockIn Stock
50 mg$619In StockIn Stock
100 mg$868In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.27%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
NSC 185058, an inhibitor of ATG4B (a major cysteine protease), can also attenuate autophagic activity.
In vitro
NSC185058 effectively suppressed starvation-induced autophagy in both cell types. GFP-LC3B labeled AVs were absent in starved MDA-MB468 cells when treated with NSC185058. The inhibitory effects of both NSC185058 on starvation-induced protein turnover were comparable to 3MA.
In vivo
Mice were injected at 2 24 h intervals with vehicle or NSC185058, autophagy induced by 20 h fasting. Fasting resulted in an increase of GFP-LC3B AVs compared with ad libitum fed mice. NSC185058 significantly decreased the appearance of GFP-LC3B AVs compared with fasted mice.
Cell Research
Saos-2 transiently expressing FYVE-RFP was incubated in DMEM medium supplemented with amino acids and serum (Fed) or Krebs-Heinseleit medium lacking amino acids and serum (Starved). The starved cells were incubated in the presence and absence of the NSC185058 or NSC377071 for 4 h at which time the cells were examined by fluorescence microscopy. The numbers of red "dots" per cell was quantified using ImageJ software. Taking into account basal responses, those cells with 3 or more puncta were defined as PtdIns3K active.
Animal Research
Immunodeficient nu/nu nude female mice were injected subcutaneously with 6 × 10^6 Saos-2 (GFP-LC3B), shCon-Saos-2(GFP-LC3B) or shATG4B-Saos-2(GFP-LC3B) cells. Palpable Saos-2 (GFP-LC3B) tumors developed in 7 to 10 d, at which time, the mice were divided into 2 groups and injected IP on Monday, Wednesday, and Friday with either peanut oil vehicle or NSC185058 (100 mg/kg body weight) dissolved in peanut oil. Over time, the tumor dimensions were measured using calipers and volumes calculated using the formula: (W2 × L)/2.
SynonymsNSC185058
Chemical Properties
Molecular Weight215.27
FormulaC11H9N3S
Cas No.39122-38-8
SmilesS=C(Nc1ccccn1)c1ccccn1
Relative Density.1.323 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 30 mg/mL (139.36 mM), Sonication is recommended.
Ethanol: 2.5 mg/mL (11.61 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (9.29 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM4.6453 mL23.2266 mL46.4533 mL232.2665 mL
5 mM0.9291 mL4.6453 mL9.2907 mL46.4533 mL
10 mM0.4645 mL2.3227 mL4.6453 mL23.2266 mL
DMSO
1mg5mg10mg50mg
20 mM0.2323 mL1.1613 mL2.3227 mL11.6133 mL
50 mM0.0929 mL0.4645 mL0.9291 mL4.6453 mL
100 mM0.0465 mL0.2323 mL0.4645 mL2.3227 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

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

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