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2-APB

Catalog #: 1224
44 Citations 1 Review Datasheet / COA / SDS
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1224/50
2-APB | CAS No. 524-95-8 | Inositol Lipid Antagonists
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Description: IP3 receptor antagonist. Also TRP channel modulator

Chemical Name: 2-Aminoethoxydiphenylborane

Purity: ≥98%

Product Details
Citations (44)
Reviews (1)
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

2-APB is 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

M.Wt:
225.1
Formula:
C14H16BNO
Solubility:
Soluble to 100 mM in DMSO with gentle warming
Purity:
≥98%
Storage:
Store at RT
CAS No:
524-95-8

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.

Background References

  1. In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
    Aihara, Eitaro, Hentz, Courtney, Korman, Abraham, Perry, Nicholas, Prasad, Vikram, Shull, Gary E, Montrose, Marshall
    J Biol Chem, 2013;288(47):33585-97.
  2. Lysosomes integrate metabolic-inflammatory cross-talk in primary macrophage inflammasome activation.
    Weber K, Schilling J
    J Biol Chem, 2014;289(13):9158-71.
  3. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  4. BKCa channel regulates calcium oscillations induced by alpha-2-macroglobulin in human myometrial smooth muscle cells
    M Wakle-Prab, RA Lorca, X Ma, SJ Stamnes, C Amazu, JJ Hsiao, CM Karch, KL Hyrc, ME Wright, SK England
    Proc Natl Acad Sci USA, 2016;113(16):E2335-44.
  5. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
    Nature, 2012;492(7427):123-7.
  6. Role of pituitary adenylyl cyclase-activating polypeptide in intracellular calcium dynamics of neurons and satellite cells in rat superior cervical ganglia
    K Isobe, T Yokoyama, K Moriguchi-, M Kumagai, YI Satoh, A Kuji, T Saino
    Biomed. Res., 2017;38(2):99-109.
  7. SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes.
    Huang C, Wu J, Liao R, Zhang W
    PLoS ONE, 2012;7(11):e49954.
  8. K+ efflux agonists induce NLRP3 inflammasome activation independently of Ca2+ signaling.
    Katsnelson M, Rucker L, Russo H, Dubyak G
    J Immunol, 2015;194(8):3937-52.
  9. Molecular mechanisms of calcium-sensing receptor-mediated calcium signaling in the modulation of epithelial ion transport and bicarbonate secretion.
    Xie R, Dong X, Wong C, Vallon V, Tang B, Sun J, Yang S, Dong H
    J Biol Chem, 2014;289(50):34642-53.
  10. Endothelial nitric-oxide synthase activation generates an inducible nitric-oxide synthase-like output of nitric oxide in inflamed endothelium.
    Lowry J, Brovkovych V, Zhang Y, Skidgel R
    J Biol Chem, 2013;288(6):4174-93.
  11. Functional Characterization of the Odorant Receptor 51E2 in Human Melanocytes

    J Biol Chem, 2016;0(0):.
  12. STIM and Orai: the long-awaited constituents of store-operated calcium entry.
    Varnai et al.
    TiPS, 2009;30:118
  13. Block of specific gap junction channel subtypes by 2-aminoethoxydiphenyl borate (2-APB).
    Bai et al.
    J.Pharmacol.Exp.Ther., 2006;319:1452
  14. 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release.
    Maruyama et al.
    J.Biochem., 1997;122:498
  15. Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltafe-dependent effect.
    Xu et al.
    Br.J.Pharmacol., 2005;145:405
  16. Inhibition of the transient receptor potential cation channel TRPM2 by 2-aminoethoxydiphenyl borate (2-APB).
    Togashi et al.
    Br.J.Pharmacol., 2008;153:1324
  17. Glucagon stimulates gluconeogenesis by INSP3R1-mediated hepatic lipolysis
    RJ Perry, D Zhang, MT Guerra, AL Brill, L Goedeke, AR Nasiri, A Rabin-Cour, Y Wang, L Peng, S Dufour, Y Zhang, XM Zhang, GM Butrico, K Toussaint, Y Nozaki, GW Cline, KF Petersen, MH Nathanson, BE Ehrlich, GI Shulman
    Nature, 2020;0(0):.

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Citations for 2-APB

The citations listed below are publications that use Tocris products. Selected citations for 2-APB include:

44 Citations: Showing 1 - 10

  1. TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations
    Authors: O'Malley Et al.
    J Neurosci  2020;40:4813
  2. Cell sensing and decision-making in confinement: The role of TRPM7 in a tug of war between hydraulic pressure and cross-sectional area.
    Authors: Zhao Et al.
    Sci Adv  2019;5:eaaw7243
  3. Role of miRNA-181a-2-3p in cadmium-induced inflammatory responses of human bronchial epithelial cells.
    Authors: Kim Et al.
    J Thorac Dis  2019;11:3055
  4. Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures.
    Authors: Lim Et al.
    Int J Mol Sci  2018;19
  5. Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma.
    Authors: Florea Et al.
    Oncotarget  2017;8:22876
  6. Gpr158 mediates osteocalcin's regulation of cognition.
    Authors: Khrimian Et al.
    J Exp Med  2017;214:2859
  7. Connexin 32-mediated cell-cell communication is essential for hepatic differentiation from humanembryonic stem cells
    Authors: Qin Et al.
    Scientific Reports  2016;6:37388
  8. Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.
    Authors: Colavita Et al.
    Sci Rep  2016;6:28454
  9. Activation of the neurokinin 3 receptor promotes filopodia growth and sprouting in rat embryonic hypothalamic cells.
    Authors: Flynn Et al.
    Carcinogenesis  2015;75:44896
  10. The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine.
    Authors: Baron Et al.
    Dev Neurobiol  2015;6:e1629
  11. 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.
    Authors: Nakakura Et al.
    Cell Death Dis  2015;6:299
  12. Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP.
    Authors: Tang Et al.
    J Neurosci  2015;35:3016
  13. Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling.
    Authors: Dobson Et al.
    Biomed Res Int  2015;10:e0125974
  14. Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments.
    Authors: Fransen Et al.
    PLoS One  2015;10:e0121634
  15. Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum.
    Authors: Tamura Et al.
    PLoS One  2014;9:e85351
  16. Capture of microtubule plus-ends at the actin cortex promotes axophilic neuronal migration by enhancing microtubule tension in the leading process.
    Authors: Hutchins and Wray
    J Biol Chem  2014;8:400
  17. Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs.
    Authors: Hendron Et al.
    Cell Calcium  2014;56:482
  18. Cross-synaptic synchrony and transmission of signal and noise across the mouse retina.
    Authors: Grimes Et al.
    Elife  2014;3:e03892
  19. Activation of a TRP-like channel and intracellular Ca2+ dynamics during phospholipase-C-mediated cell death.
    Authors: Gon&ccedil;alves Et al.
    J Cell Sci  2014;127:3817
  20. Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis.
    Authors: Varadarajan Et al.
    PLoS One  2013;8:e56603
  21. Antagonism of neuronal prostaglandin E(2) receptor subtype 1 mitigates amyloid β neurotoxicity in vitro.
    Authors: Li Et al.
    Biochem Pharmacol  2013;8:87
  22. AMP-activated protein kinase as regulator of P2Y(6) receptor-induced Ins secretion in mouse pancreatic β-cells.
    Authors: Balasubramanian Et al.
    Hypertension  2013;85:991
  23. Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition.
    Authors: Chang Et al.
    Front Cell Neurosci  2013;34:1096
  24. Calcium release-dependent actin flow in the leading process mediates axophilic migration.
    Authors: Hutchins Et al.
    J Pharmacol Exp Ther  2013;33:11361
  25. In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
    Authors: Aihara Et al.
    PLoS One  2013;288:33585
  26. SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes.
    Authors: Huang Et al.
    Korean J Physiol Pharmacol  2012;7:e49954
  27. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Authors: Lee Et al.
    Nature  2012;492:123
  28. DHA inhibits ER Ca2+ release and ER stress in astrocytes following in vitro ischemia.
    Authors: Begum Et al.
    J Neurochem  2012;120:622
  29. Regulation of Substantia Nigra Pars Reticulata GABAergic Neuron Activity by H?O? via Flufenamic Acid-Sensitive Channels and K(ATP) Channels.
    Authors: Lee Et al.
    Front Syst Neurosci  2011;5:14
  30. Calcium-sensing receptor modulates extracellular Ca(2+) entry via TRPC-encoded receptor-operated channels in human aortic smooth muscle cells.
    Authors: Chow Et al.
    PLoS One  2011;301:C461
  31. The amiloride-sensitive epithelial Na+ channel PPK28 is essential for drosophila gustatory water reception.
    Authors: Chen Et al.
    J Neurosci  2010;30:6247
  32. Non-cardiomyocytes influence the electrophysiological maturation of human embryonic stem cell-derived cardiomyocytes during differentiation.
    Authors: Kim Et al.
    Front Physiol  2010;19:783
  33. Caffeine and 2-Aminoethoxydiphenyl Borate (2-APB) Have Different Ability to Inhibit Intracellular Calcium Mobilization in Pancreatic Acinar Cell.
    Authors: Choi Et al.
    J Neuroimmune Pharmacol  2010;14:105
  34. Mobilization of calcium from intracellular stores facilitates somatodendritic DA release.
    Authors: Patel Et al.
    J Neurosci  2009;29:6568
  35. Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation.
    Authors: Clark Et al.
    J Neurosci  2009;29:11237
  36. P2Y receptors mediate Ca2+ signaling in duodenocytes and contribute to duodenal mucosal bicarbonate secretion.
    Authors: Dong Et al.
    Am J Physiol Gastrointest Liver Physiol  2009;296:G424
  37. Estrogen attenuates glutamate-induced cell death by inhibiting Ca2+ influx through L-type voltage-gated Ca2+ channels.
    Authors: Sribnick Et al.
    Brain Res  2009;1276:159
  38. Regulated release of BDNF by cortical oligodendrocytes is mediated through metabotropic glutamate receptors and the PLC pathway.
    Authors: Bagayogo and Dreyfus
    ASN Neuro  2009;1
  39. Low concentrations of sphingosylphosphorylcholine enhance pulmonary artery vasoreactivity: the role of protein kinase C δ and Ca2+ entry.
    Authors: Snetkov Et al.
    Am J Physiol Cell Physiol  2008;51:239
  40. Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons.
    Authors: Kelm Et al.
    Stem Cells Dev  2007;323:356
  41. Contribution of both Ca2+ entry and Ca2+ sensitization to the alpha1-adrenergic vasoconstriction of rat penile small arteries.
    Authors: Villalba Et al.
    Am J Physiol Heart Circ Physiol  2007;292:H1157
  42. Nimodipine selectively stimulates beta-amyloid 1-42 secretion by a mechanism independent of calcium influx blockage.
    Authors: Facchinetti Et al.
    Neurobiol Aging  2006;27:218
  43. PI3K and PKC contribute to membrane depolarization mediated by alpha2-adrenoceptors in the canine isolated mesenteric vein.
    Authors: Yamboliev
    BMC Physiol  2005;5:9
  44. 2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels.
    Authors: Gu Et al.
    Am J Physiol Lung Cell Mol Physiol  2005;288:L932

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IP3R involved or not
By Anonymous on 04/13/2018

We used 2-APB to determine whether IP3R involved in the related calcium signaling

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