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NSC 185058

Catalog No. T5211   CAS 39122-38-8
Synonyms: NSC185058

NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. It also can attenuate the autophagic activity.

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NSC 185058 Chemical Structure
NSC 185058, CAS 39122-38-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 88.00
5 mg In stock $ 189.00
10 mg In stock $ 297.00
25 mg In stock $ 516.00
50 mg In stock $ 736.00
100 mg In stock $ 987.00
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Purity: 99.83%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. It also can attenuate the 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.
Synonyms NSC185058
Molecular Weight 215.27
Formula C11H9N3S
CAS No. 39122-38-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (139.36 mM)

Ethanol: 2.5 mg/mL

TargetMolReferences and Literature

1. Akin D, et al. A novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors. Autophagy. 2014;10(11):2021-35.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library NO PAINS Compound Library Protease Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Autophagy Compound Library

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Keywords

NSC 185058 39122-38-8 Autophagy Proteases/Proteasome Cysteine Protease Inhibitor NSC185058 Atg4 Autophagy-related 4 NSC-185058 inhibit inhibitor

 

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