Spautin-1

SKU: orb1307049

Description

Spautin-1 is a small molecule autophagy inhibitor that functions by targeting and inhibiting the deubiquitinases USP10 and USP13. It suppresses the unfolded protein response (UPR) and demonstrates selective toxicity toward cancer cells under glucose-deprived conditions, making it a useful research tool for studying autophagy, cancer metabolism, and cellular stress responses in vitro.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1262888-28-7
• MW: 271.27
• Purity: >98%
• Formula: C₁₅H₁₁F₂N₃
• SMILES: Fc1ccc(CNc2ncnc3ccc(F)cc23)cc1
• Target: Protease
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 15 mg/ml with warming).

Bioactivity

• Target IC50:
  K562 cells:1.03 μM
• In Vivo:
  Spautin-1 effectively mitigates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Pretreatment with Spautin-1 significantly reduces elevated serum amylase and lipase levels, markers of trypsin activity, and inhibits the increase of serum TNFα caused by cerulein. Additionally, Spautin-1 treatment alleviates inflammation-induced damage such as edema, degeneration, coagulative necrosis, and the infiltration of inflammatory cells.
• In Vitro:
  In Bcap-37 cells, Spautin-1 dramatically enhanced cell death in glucose-free media and induces apoptotic morphology. In Bax-Bak DKO cells, spautin-1 inhibits etoposide induced autophagic cell death. 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, 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. 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. Spautin-1 also specifically reduces infectious dengue virus titers in BHK-21 cells.
• Cell Research:
  Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1x105/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a microplate reader.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Spautin 1, Spautin1, Spautin-1, USP10, USP13, Apoptosis, Autophagy, inhibit, Inhibitor

Compound Identifiers

PubChem CID

51037431