S-(4-Nitrobenzyl)-6-thioinosine (NBTI, NBMPR) is a small molecule inhibitor of equilibrative nucleoside transporter (ENT) proteins. These transport proteins are described in relation to their sensitivity to NBMPR, designated as either es (NBMPR-sensitive) or ei (NBMPR-insensitive). They provide good research tools anticancer, antiviral, cardioprotective, and neuroprotective agents. Inhibition of ENT1 by NBMPR blocks the uptake and transport of adenosine, which affects the regulation of extracellular adenosine levels and the cardiac system signaling associated with adenosine.
1. Krug, E.C., et al. 1989. J. Biol. Chem. 264: 10601-10607. PMID: 2732241 2. Griffiths, M., et al. 1997. Biochem. J. 328: 739-743. PMID: 9396714 3. Yao, S.Y., et al. 1997. J. Biol. Chem. 272: 28423-18430. PMID: 9353301 4. Zhu, Z., et al. 2003. J. Med. Chem. 46: 831-837. PMID: 12593662 5. Baldwin, S.A., et al. 2005. J. Biol. Chem. 280: 15880-15887. PMID: 15701636 6. Barnes, K., et al. 2006. Circ. Res. 99: 510-519. PMID: 16873718
Store stock solutions at -20°C or below and used within 1 month.
Soluble in water (Partly miscible), DMSO, methanol, and DMF. Insoluble in hexane.
Store at -20° C
187-190° C (lit.)
Potent adenosine uptake and nucleoside transport : IC50 = 4.6 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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ShimadaShimada, T. et al. (PubMed 26037416) investigated the gemcitabine (GEM) uptake in rat and human isolated heptaocytes. GEM uptake involved high- and low-affinity saturable components, however this uptake was inhibited by NBMPR, an inhibitor of ENTs with potential anticancer, cardio-, and neuro- protective properties. -SCBT Publication Review
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