STF-62247

SKU: orb1300558

Description

STF-62247 is a potent TGN inhibitor, demonstrating differential activity with IC50 values of 0.625 μM in RCC4 cells and 16 μM in RCC4/VHL cells. This small molecule is a valuable research tool for investigating autophagy, cellular stress responses, and VHL-dependent pathways in cancer models, both in vitro and in vivo.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 315702-99-9
• MW: 267.35
• Purity: 99.67% (May vary between batches)
• Formula: C₁₅H₁₃N₃S
• SMILES: Cc1cccc(Nc2nc(cs2)-c2ccncc2)c1
• Target: Autophagy,Estrogen/progestogen Receptor
• Solubility: Ethanol:3 mg/mL (11.22 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.48 mM);DMSO:55 mg/mL (205.72 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  TGN (RCC4):0.625 μM|TGN (RCC4/VHL):16 μM
• In Vivo:
  In vivo mouse model, STF-62247 at a dose of 8 mg/kg by intraperitoneal injection significantly reduces tumor growth of VHL-deficient SN12C tumor cells.
• In Vitro:
  In vitro, STF-62247 shows cytotoxicity and tumor growth inhibitory activity against wild-type VHL and VHL-deficient renal cell carcinoma (RCC) in a HIF-independent manner with IC50 of 16 μM and 0.625 μM, respectively. Moreover, STF-62247 also leads to cell death by increasing acidification and inducing autophagy in VHL-deficient cells. STF-62247 specifically induces macroautophagy and enhances the fusion of autophagosome and lysosomes to form autolysosomes by interfering with Golgi-endoplasmic reticulum transport in cells that have lost VHL . A recent study shows that induction of autophagy by STF-62247 increases sensitivity of RCC under hypoxic conditions to radiation in a VHL-dependent manner.
• Cell Research:
  For cell viability, 100,000 cells are plated in a 12-well plate. The following day, 1.25 μM STF-62247 is added in the presence or absence of 1 mM 3-MA for 24 hours at 37 °C. Cells are trypsinized and counted by trypan blue exclusion. For XTT assays, 5000 RCC4 with and without VHL cells or 2,500 SN12C with and without VHL shRNA cells are plated in 96-well plates. The following day, vehicle (DMSO), STF-62247 is added to media by serial dilution. Four days later, the media is aspirated and XTT solution containing 0.3 mg/ml of XTT in Phenol Red-free media, 20% FCS and 2.65 mg/ml N-methyl dibenzopyrazine methyl sulfate (PMS) is added to the cells and incubated at 37 °C for 1-2 hours. Metabolism of XTT is quantified by measuring the absorbance at 450 nm on a plate reader. (Only for Reference)

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

cell, cytotoxic, carcinoma, Autophagy, Inhibitor, Estrogen Receptor, EstrogenReceptor, ER, inhibit, intracytoplasmic, RCC, progestogenReceptor, progestogen Receptor, renal, STF 62247, STF62247, STF-62247, vacuoles, VHL

Compound Identifiers

PubChem CID

704473