2-APB
TRP blocker / An IP3 receptor antagonist (IC50=42 μM).1 Inhibits store-operated Ca2+ channels at high concentrations (50 μM) but stimulates at low concs. (<10 μM).2 Modulates TRP channels, blocking TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8, TRPP2 and at higher concentrations, activating TRPV1, TRPV2, TRPV3.3,4 Also inhibits selected GAP junction subtypes.5
Biochemicals & reagents
524-95-8
1) Maruyama et al. (1997) 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release; J. Biochem., 122 498 2) Varnai et al. (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry; Trends Pharmacol. Sci., 30 118 3) Togashi et al. (2008) Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB); Br. J. Pharmacol., 153 1324 4) Xu et al. (2005) Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect; Br. J. Pharmacol., 145 405 5) Bai et al. (2006) Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB); J. Pharmacol. Exp. Ther., 319 1452
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TARGET: Ion channel -- PATHWAY: Calcium signaling; Carbohydrate metabolism -- DISEASE AREA: Diabetes