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Biological Activity for 2-APB
2-APB is an 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 for 2-APB
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for 2-APB
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||22.51||100 with gentle warming|
Preparing Stock Solutions for 2-APB
The following data is based on the product molecular weight 225.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.44 mL||22.21 mL||44.42 mL|
|5 mM||0.89 mL||4.44 mL||8.88 mL|
|10 mM||0.44 mL||2.22 mL||4.44 mL|
|50 mM||0.09 mL||0.44 mL||0.89 mL|
References for 2-APB
References are publications that support the biological activity of the product.
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
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
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
Varnai et al (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry. TiPs 30 118 PMID: 19187978
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
If you know of a relevant reference for 2-APB, please let us know.
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Keywords: 2-APB, 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, Signal, Non-selective, 1224, Tocris Bioscience
44 Citations for 2-APB
Citations are publications that use Tocris products. Selected citations for 2-APB include:
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
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
O'Malley et al (2020) TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations J Neurosci 40 4813 PMID: 32414784
Qin et al (2016) Connexin 32-mediated cell-cell communication is essential for hepatic differentiation from humanembryonic stem cells Scientific Reports 6 37388 PMID: 27874032
Chen et al (2010) The amiloride-sensitive epithelial Na+ channel PPK28 is essential for drosophila gustatory water reception. J Neurosci 30 6247 PMID: 20445050
Facchinetti et al (2006) Nimodipine selectively stimulates beta-amyloid 1-42 secretion by a mechanism independent of calcium influx blockage. Neurobiol Aging 27 218 PMID: 16399208
Yamboliev (2005) PI3K and PKC contribute to membrane depolarization mediated by alpha2-adrenoceptors in the canine isolated mesenteric vein. BMC Physiol 5 9 PMID: 15958164
Gu et al (2005) 2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels. Am J Physiol Lung Cell Mol Physiol 288 L932 PMID: 15653710
Colavita et al (2016) Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus. Sci Rep 6 28454 PMID: 27345695
Patel et al (2009) Mobilization of calcium from intracellular stores facilitates somatodendritic DA release. J Neurosci 29 6568 PMID: 19458227
Bagayogo and Dreyfus (2009) Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway. ASN Neuro 1 PMID: 19570026
Zhao et al (2019) Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area. Sci Adv 5 eaaw7243 PMID: 31355337
Kim et al (2019) Role of miRNA-181a-2-3p in cadmium-induced inflammatory responses of human bronchial epithelial cells. J Thorac Dis 11 3055 PMID: 31463135
Varadarajan et al (2013) Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis. PLoS One 8 e56603 PMID: 23457590
Lee et al (2011) Regulation of Substantia Nigra Pars Reticulata GABAergic Neuron Activity by H?O? via Flufenamic Acid-Sensitive Channels and K(ATP) Channels. Front Syst Neurosci 5 14 PMID: 21503158
Florea et al (2017) Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma. Oncotarget 8 22876 PMID: 28206967
Khrimian et al (2017) Gpr158 mediates osteocalcin's regulation of cognition. J Exp Med 214 2859 PMID: 28851741
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
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
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
Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins 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
Aihara et al (2013) In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium. PLoS One 288 33585 PMID: 24121509
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
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
Villalba et al (2007) Contribution of both Ca2+ entry and Ca2+ sensitization to the alpha1-adrenergic vasoconstriction of rat penile small arteries. Am J Physiol Heart Circ Physiol 292 H1157 PMID: 17085536
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
Gonçalves et al (2014) Activation of a TRP-like channel and intracellular Ca2+ dynamics during phospholipase-C-mediated cell death. J Cell Sci 127 3817 PMID: 25037570
Hendron et al (2014) Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs. Cell Calcium 56 482 PMID: 25459299
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
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
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
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
Lim et al (2018) Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures. Int J Mol Sci 19 PMID: 30274399
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
Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Dev Neurobiol 6 e1629 PMID: 25654762
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
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
Begum et al (2012) DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia. J Neurochem 120 622 PMID: 22129278
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333
Do you know of a great paper that uses 2-APB from Tocris? Please let us know.
Reviews for 2-APB
Average Rating: 4.8 (Based on 4 Reviews.)
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It significantly inhibits TRPM7 current. Very good.
HEK293 cells were incubated with intracellular Ca2+ sensitive dye, Fura-2AM in normal tyrode solution for 40 min, washed and kept aside for 20 min. Fura2-loaded cells were excited alternately at 340 and 380 nm and fluorescence at 510 nm was expressed as 340/380 ratio. Intracellular Ca2+ stores were depleted with 30 μM BHQ which promotes store-operated Ca2+ entry into the cells upon addition of 1 mM extracellular Ca2+. Preincubation of cells with 50 μM 2-APB for 10 min reduces this Ca2+ entry.
We used 2-APB to determine whether IP3R involved in the related calcium signaling