PX-12

SKU: orb1305801

Description

PX-12 is a thioredoxin-1 (Trx-1) inhibitor that induces apoptosis and suppresses HIF-1α and VEGF, demonstrating antitumor activity in preclinical models. It is a research tool for studying cancer mechanisms and has been evaluated in clinical trials for advanced metastatic cancers.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 141400-58-0
• MW: 188.31
• Purity: 99.60%
• Formula: C₇H₁₂N₂S₂
• SMILES: CCC(C)SSc1ncc[nH]1
• Target: Apoptosis,Others,Thioredoxin
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:38 mg/mL (201.79 mM);DMSO:48 mg/mL (254.9 mM)

Bioactivity

• Target IC50:
  MCF-7 cells:1.9 μM|HT29 cells:2.9 μM
• In Vivo:
  In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density.
• In Vitro:
  In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9 μM, respectively. PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity.
• Cell Research:
  Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.(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

inhibit, IV 2, IV2, IV-2, PX12, PX-12, PX 12, Inhibitor, TRX (HT-29 cells), TRX (MCF-7)

Compound Identifiers

PubChem CID

219104