PF-543

SKU: orb1222707

Description

PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.

Key Properties

• CAS Number: 1415562-82-1
• MW: 465.6
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₁NO₄S
• SMILES: C(O)[C@@H]1N(CCC1)Cc1ccc(cc1)COc1cc(cc(c1)C)CS(=O)(=O)c1ccccc1
• Target: SphK1| SphK1
• Solubility: In Vitro: DMSO : 100 mg/mL (214.78 mM)

Bioactivity

• In Vivo:
  Animal model: Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension. Dosage: 1 mg/kg. Administration: Intraperitoneal injection; every second day; for 21 days. Result: Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.
• In Vitro:
  Western blot analysis. Cell line: Human pulmonary arterial smooth muscle (PASM) cells. Concentration: 10 nM, 100 nM, 1000 nM. Incubation time: 24 hours. Result: Abolished SK1 expression at nM concentrations. Apoptosis Analysis. Cell line: Human pulmonary arterial smooth muscle (PASM) cells. Concentration: 0.1 μM, 1 μM, 10 μM Incubation time: 24 hours. Result: Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.

Storage & Handling

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

Alternative Names

Sphingosine Kinase 1 Inhibitor II

Quick Database Links

Gene Symbol

SphK1| SphK1