Probenecid

- Overview
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    Background
    
    Probenecid is an inhibitor of organic anion transport and MRP [1] [2]. Also, probenecid inhibited pannexin-1 channel with IC50 value of 150μM [3].
    Multidrug resistance-associated proteins (MRPs) are ATP-binding cassette (ABC) transporters that transport various molecules across cellular membranes and are involved in multi-drug resistance.
    Probenecid is an inhibitor of organic anion transport, MRP and pannexin-1 channel. In MRP-overexpressing HL60/AR and H69/AR tumor cell lines, probenecid reversed resistance to daunorubicin (DNR) and vincristine (VCR) in a concentration-dependent way [1]. In wild-type AML-2 cells, probenecid increased the MRP levels in a dose- and time-dependent way. In MRP-overexpressing AML cells, probenecid exhibited a significant chemosensitizing effect. These results suggested that probenecid functioned as an effective chemosensitizer of multidrug resistance (MDR) tumor cells but also an MRP activator [2].
    In ischemia/reperfusion (I/R) injury rats, probenecid protected against CA1 neuronal death. Probenecid strengthened the upregulation of Hsp70 and inhibited the expression of calpain-1 and the released of cathepsin B. Also, probenecid inhibited the proliferation of astrocytes and microglia [4].
    
    [1]. Gollapudi S, Kim CH, Tran BN, et al. Probenecid reverses multidrug resistance in multidrug resistance-associated protein-overexpressing HL60/AR and H69/AR cells but not in P-glycoprotein-overexpressing HL60/Tax and P388/ADR cells. Cancer Chemother Pharmacol, 1997, 40(2): 150-158.
    [2]. Kim HS, Min YD, Choi CH. Double-edged sword of chemosensitizer: increase of multidrug resistance protein (MRP) in leukemic cells by an MRP inhibitor probenecid. Biochem Biophys Res Commun, 2001, 283(1): 64-71.
    [3]. Silverman W, Locovei S, Dahl G. Probenecid, a gout remedy, inhibits pannexin 1 channels. Am J Physiol Cell Physiol, 2008, 295(3): C761-767.
    [4]. Wei R, Wang J, Xu Y, et al. Probenecid protects against cerebral ischemia/reperfusion injury by inhibiting lysosomal and inflammatory damage in rats. Neuroscience, 2015, 301: 168-177.
- Properties
  - Alternative Name
    
    4-(dipropylsulfamoyl)benzoic acid
    
    CAS Number
    
    57-66-9
    
    Molecular Formula
    
    C13H19NO4S
    
    Molecular Weight
    
    285.36
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥13.66 mg/mL in EtOH; ≥8.7 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Beltrán-Castillo S, Olivares et al. "D-serine released by astrocytes in brainstem regulates breathing response to CO(2) levels." Nat Commun. 2017 Oct 10;8(1):838. PMID:29018191

Probenecid

Background

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