Suramin

SKU: orb2655902

Description

An antitrypansomal drug that also possesses antitumor activity; inhibits CRL (Cullin-RING E3 ubiquitin ligases) activity by disrupting its ability to recruit Cdc34; induces accumulation of CRL substrates; also inhibits multiple viruses (ZIKVs, EV71).Parasite Infection Approved.

Key Properties

• CAS Number: 145-63-1
• MW: 1297.28
• Purity: >98% (HPLC)
• Formula: C₅₁H₄₀N₆O₂₃S₆
• SMILES: CC1=C(C=C(C=C1)C(=O)NC2=C3C(=CC(=CC3=C(C=C2)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)NC(=O)C4=CC(=CC=C4)NC(=O)NC5=CC=CC(=C5)C(=O)NC6=C(C=CC(=C6)C(=O)NC7=C8C(=CC(=CC8=C(C=C7)S(=O)(=O)O)S(=O)(=O)O)S(=O)(=O)O)C
• Target: P2Y Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Suramin (10 mg/kg; IV; twice weekly for 3 weeks) reverses established pulmonary hypertension (PH), thereby normalizing the pulmonary artery pressure values and vessel structure. Animal model: Adult male Wistar rats (200-225 g). Dosage: 10 mg/kg. Administration: IV; twice weekly for 3 weeks. Result: Reversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure.
• In Vitro:
  Suramin (50-600 μg/mL; for 24-96 hours) inhibits cells proliferation in a dose-dependent and time-dependent manner and decreases viability in cancer cells. Suramin (300 μg/mL; for 48 hours) induces cells apoptosis, and down-regulates mRNA expression in HeLa cells. Suramin (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2. The IC50 values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively. Suramin blocks viral replication in Vero E6 cells. Cell Proliferation Assay Cell line: HO-8910 PM ovarian and Hela cervical cancer cells. Concentration: 50, 100, 200, 300, 400, 500 and 600 μg/mL. Incubation time: For 24, 48, 72 and 96 hours. Result: Inhibited cells proliferation in a dose-dependent and time-dependent manner. Apoptosis Analysis Cell line: HeLa cells. Concentration: 300 μg/mL. Incubation time: For 48 hours. Result: Induced cells apoptosis.. Western blot analysis. Cell line: PA-SMCs cells. Concentration: 1 mg/mL. Incubation time: For 1 hours. Result: Significantly suppressed the phosphorylated ERK1/2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

P2Y Receptor