Cat. No. 1224

2-APB C14H16BNO [524-95-8]

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Chemical Name: 2-Aminoethoxydiphenylborane

Biological Activity

A functional and membrane permeable D-myo-inositol 1,4,5-trisphosphate (IP3) receptor antagonist (IC50 = 42 μM). Stimulates store-operated calcium (SOC) release at low concentrations (< 10 μM) and inhibits it at higher concentrations (up to 50 μM). Increases STIM-Orai channel conductance and limits ion selectivity. Modulator of TRP channels; blocks TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8 and TRPP2 and at higher concentrations stimulates TRPV1, TRPV2 and TRPV3. Also blocks specific gap channel subtypes.

Technical Data

Soluble to 10 mM in ethanol with gentle warming and to 100 mM in DMSO with gentle warming
>98 %
Store at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Varnai et al (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry. TiPs 30 118. PMID: 19187978.

Togashi et al (2008) Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB). Br.J.Pharmacol. 153 1324. PMID: 18204483.

Bai et al (2006) Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB). J.Pharmacol.Exp.Ther. 319 1452. PMID: 16985167.

Xu et al (2005) Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltafe-dependent effect. Br.J.Pharmacol. 145 405. PMID: 15806115.

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. PMID: 9348075.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for 2-APB include:

Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Dev Neurobiol 6 e1629. PMID: 25654762.

Dobson et al (2015) Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling. Biomed Res Int 10 e0125974. PMID: 25933382.

Flynn et al (2015) Activation of the neurokinin 3 receptor promotes filopodia growth and sprouting in rat embryonic hypothalamic cells. Carcinogenesis 75 44896. PMID: 25044785.

Fransen et al (2015) Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments. PLoS One 10 e0121634. PMID: 25803863.

Nakakura et al (2015) Pathophysiological significance of the two-pore domain K(+) channel K2P5.1 in splenic CD4(+)CD25(-) T cell subset from a chemically-induced murine inflammatory bowel disease model. Cell Death Dis 6 299. PMID: 26578971.

Tang et al (2015) Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP. J Neurosci 35 3016. PMID: 25698739.

Grimes et al (2014) Cross-synaptic synchrony and transmission of signal and noise across the mouse retina. Elife 3 e03892. PMID: 25180102.

Hutchins and Wray (2014) Capture of microtubule plus-ends at the actin cortex promotes axophilic neuronal migration by enhancing microtubule tension in the leading process. J Biol Chem 8 400. PMID: 25505874.

Tamura et al (2014) Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum. PLoS One 9 e85351. PMID: 24454845.

Aihara et al (2013) In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium. PLoS One 288 33585. PMID: 24121509.

Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells. Hypertension 85 991. PMID: 23333427.

Chang et al (2013) Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition. Front Cell Neurosci 34 1096. PMID: 23349021.

Hutchins et al (2013) Calcium release-dependent actin flow in the leading process mediates axophilic migration. J Pharmacol Exp Ther 33 11361. PMID: 23843509.

Li et al (2013) Antagonism of neuronal prostaglandin E(2) receptor subtype 1 mitigates amyloid β neurotoxicity in vitro. Biochem Pharmacol 8 87. PMID: 22718277.

Varadarajan et al (2013) Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis. PLoS One 8 e56603. PMID: 23457590.

Begum et al (2012) DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia. J Neurochem 120 622. PMID: 22129278.

Huang et al (2012) SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes. Korean J Physiol Pharmacol 7 e49954. PMID: 23185493.

Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123. PMID: 23143333.

Chow et al (2011) Calcium-sensing receptor modulates extracellular Ca(2+) entry via TRPC-encoded receptor-operated channels in human aortic smooth muscle cells. PLoS One 301 C461. PMID: 21562303.

Choi et al (2010) Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell. J Neuroimmune Pharmacol 14 105. PMID: 20473382.

Kim et al (2010) Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation. Front Physiol 19 783. PMID: 20001453.

Clark et al (2009) Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation. J Neurosci 29 11237. PMID: 19741130.

Dong et al (2009) P2Y receptors mediate Ca2+ signaling in duodenocytes and contribute to duodenal mucosal bicarbonate secretion. Am J Physiol Gastrointest Liver Physiol 296 G424. PMID: 19074643.

Sribnick et al (2009) Estrogen attenuates glutamate-induced cell death by inhibiting Ca2+ influx through L-type voltage-gated Ca2+ channels. Brain Res 1276 159. PMID: 19389388.

Snetkov et al (2008) Low concentrations of sphingosylphosphorylcholine enhance pulmonary artery vasoreactivity: the role of protein kinase C δ and Ca2+ entry. Am J Physiol Cell Physiol 51 239. PMID: 18158336.

Kelm et al (2007) Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons. Stem Cells Dev 323 356. PMID: 17652632.

Do you know of a great paper that uses 2-APB from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: 2-APB, supplier, Increases, STIM-Orai, channels, conductivity, reduces, selectivity, IP3, receptor, antagonist, TRP, modulators, Store, Operated, Calcium, Channels, Ca2+, Inositol, 145-triphosphate, Receptors, Triphosphoinositol, Transient, Receptor, Potential, PIP2, Lipids, cAMP, Signaling, Signalling, TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8, TRPP2, TRPV1, TRPV2, TRPV3, Tocris Bioscience, IP3 Receptor Antagonist products

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