NSC 185058

SKU: orb1301994

Description

NSC 185058 is a small molecule inhibitor that selectively targets the ATG4B cysteine protease, a key regulator of autophagy. By inhibiting ATG4B, it effectively attenuates autophagic flux and serves as a valuable research tool for studying autophagy in both cellular and animal models of cancer and neurodegenerative diseases.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 39122-38-8
• MW: 215.27
• Purity: 99.27%
• Formula: C₁₁H₉N₃S
• SMILES: S=C(Nc1ccccn1)c1ccccn1
• Target: ATG,Cysteine Protease,Autophagy
• Solubility: Ethanol:2.5 mg/mL (11.61 mM);DMSO:30 mg/mL (139.36 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (9.29 mM)

Bioactivity

• 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.
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CysteineProtease, Cysteine Protease, Autophagy-related 4, Autophagy, ATG4B, Atg4, Cathepsin, NSC 185058, NSC185058, NSC-185058, Inhibitor, inhibit

Compound Identifiers

PubChem CID

750538