S0859 is a selective, high-affinity generic NBC inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
Treatment with NBC inhibitor S0859 significantly increased caspase-3 activity and elevated the number of apoptotic EC. S0859 is potentially important for probing the transporter's functional role in heart and other tissues[1].
References:
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[2]. Lauritzen G, Stock CM, Lemaire J, et al. The Na+/H+ exchanger NHE1, but not the Na+, HCO3(-) cotransporter NBCn1, regulates motility of MCF7 breast cancer cells expressing constitutively active ErbB2. Cancer Lett. 2012 Apr 28;317(2):172-83.
[3]. Kumar S, Flacke JP, Kostin S, et al. SLC4A7 sodium bicarbonate co-transporter controls mitochondrial apoptosis in ischaemic coronary endothelial cells. Cardiovasc Res. 2011 Feb 1;89(2):392-400.
[4]. Ch'en FF, Villafuerte FC, Swietach P, et al. S0859, an N-cyanosulphonamide inhibitor of sodium-bicarbonate cotransport in the heart. Br J Pharmacol. 2008 Mar;153(5):972-82.