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AB120124

2-APB, Ca2+ release modulator

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(21 Publications)

MW 225.1 Da, Purity >98%. Cell-permeable, allosteric inhibitor of D-*myo*-inositol 1,4,5-trisphosphate (IP3) -induced Ca2+ release. Inhibits IP3-induced Ca2+ release without affecting IP3 receptor binding. Blocks store operated Ca2+ entry.
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Functional Studies - 2-APB, Ca2+ release modulator (AB120124)
  • FuncS

PubMed

Functional Studies - 2-APB, Ca2+ release modulator (AB120124)

Induction of mGluR1-mediated inward current requires activation of TRPC1 but not TRPC3 in MLIs.

Time courses of the effects of SKF96365 (black circles, 30 μM, n = 4) and 2-APB (gray circles, 100 μM, n = 5) on the DHPG-induced inward current. A black bar indicates the time of drug application.

(From Figure 2 B of Kubota et al).

Kubota et al PLoS One. 2014; 9(9): e106316. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

Chemical Structure - 2-APB, Ca2+ release modulator (AB120124)
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Lab

Chemical Structure - 2-APB, Ca2+ release modulator (AB120124)

2D chemical structure image of ab120124, 2-APB, Ca2+ release modulator

Key facts

CAS number

524-95-8

Purity

>98%

Form

Solid

form

Molecular weight

225.1 Da

Molecular formula

C<sub>1</sub><sub>4</sub>H<sub>1</sub><sub>6</sub>BNO

PubChem

1598

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 10 mM

Biochemical name

2-Aminoethyl diphenylborinate

Biological description

Cell-permeable, allosteric inhibitor of D-*myo*-inositol 1,4,5-trisphosphate (IP3) -induced Ca2+ release . Inhibits IP3-induced Ca2+ release without affecting IP3 receptor binding. Blocks store operated Ca2+ entry.

Canonical smiles

B(C1=CC=CC=C1)(C2=CC=CC=C2)OCCN

InChi

InChI=1S/C14H16BNO/c16-11-12-17-15(13-7-3-1-4-8-13)14-9-5-2-6-10-14/h1-10H,11-12,16H2

InChiKey

BLZVCIGGICSWIG-UHFFFAOYSA-N

IUPAC Name

2-diphenylboranyloxyethanamine

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

TRPV1 also known as the capsaicin or vanilloid receptor 1 is a protein that acts as an ion channel primarily allowing the passage of calcium ions. It has an approximate molecular mass of 95 kDa and is expressed in sensory neurons particularly in the dorsal root ganglia. TRPV1 is sensitive to heat acidic conditions and natural compounds like capsaicin and plays a role in the perception of pain and heat. The Vitamin D Receptor (VDR) is a nuclear receptor that binds vitamin D and its active form with a molecular mass of approximately 48 kDa and is expressed in various tissues including the intestine bone and kidney regulating calcium and phosphorus balance. TRPV2 similar to TRPV1 is also an ion channel protein involved in detecting noxious heat with a molecular mass of about 86 kDa. It is mainly expressed in the central and peripheral nervous systems. Cytochrome P450 3A4 (CYP3A4) is involved in the metabolism of various xenobiotics and drugs having a molecular weight of roughly 57 kDa and is prominently expressed in the liver.
Biological function summary

TRPV1 and TRPV2 are integral in pain modulation and detection of temperature changes contributing to the body's response to external stimuli and potentially influencing behavioral responses. TRPM2 another member of the transient receptor potential channel family functions as a cation channel activated by oxidative stress affecting Ca2+ release. The Vitamin D Receptor modulates gene transcription in numerous cells facilitating calcium absorption and immune system function. It works in tandem with proteins such as cytochrome P450 enzymes including CYP3A4 to regulate vitamin D3 metabolism. 15-Lipoxygenase-1 (15-LOX-1) metabolizes polyunsaturated fatty acids particularly arachidonic acid in inflammatory processes. All these proteins contribute significantly to maintaining cellular homeostasis and communication.

Pathways

TRPV1 is associated with the nociceptive pain pathway where it interacts with other proteins like TRPV2 to mediate thermal and inflammatory pain. VDR plays an important role in the vitamin D signaling pathway aiding in calcium homeostasis and bone health with interactions involving proteins like CYP3A4 in metabolic pathways. TDP1 a phosphodiesterase involved in DNA repair interacts with proteins within the DNA damage response pathway ultimately affecting cellular survival and response to genotoxic stress. Similarly 15-LOX-2 functions in pathways linked to lipid metabolism.

TRPV1 shows relevance to conditions such as chronic pain and inflammatory diseases where it is often overactive. It maintains connections with related receptors like TRPV3. The Vitamin D Receptor links to osteoporosis through its role in calcium regulation and bone density. Variants in the VDR gene may alter susceptibility to certain cancers due to disordered control of cellular proliferation. Cytochrome P450 enzymes including CYP3A4 relate to drug metabolism disorders and conditions resulting from exposure to toxic substances. Alterations in 15-Lipoxygenase-1 are associated with asthma involving the regulation of inflammatory mediators. These associations highlight the multifaceted roles of these targets in human health and disease.

Product protocols

Publications (21)

Recent publications for all applications. Explore the full list and refine your search

Bio-protocol 14:e4959 PubMed38841288

2024

Dissecting the Mechanical Control of Mitotic Entry Using a Cell Confinement Setup.

Applications

Unspecified application

Species

Unspecified reactive species

Margarida Dantas,Débora Vareiro,Jorge G Ferreira

Cell reports methods 3:100544 PubMed37671014

2023

Functional imaging-guided cell selection for evolving genetically encoded fluorescent indicators.

Applications

Unspecified application

Species

Unspecified reactive species

Chang Lin,Lihao Liu,Peng Zou

Molecular cancer therapeutics 22:844-858 PubMed37127876

2023

Tyrosine Kinase Inhibitors Diminish Renal Neoplasms in a Tuberous Sclerosis Model Via Induction of Apoptosis.

Applications

Unspecified application

Species

Unspecified reactive species

Uchenna Unachukwu,Jarrod Sonett,Denzel Woode,Takayuki Shiomi,Kiran Chada,Jeanine M D'Armiento

iScience 26:106328 PubMed36968068

2023

Mitochondria-associated membrane protein PACS2 maintains right cardiac function in hypobaric hypoxia.

Applications

Unspecified application

Species

Unspecified reactive species

Jie Yang,Mengjia Sun,Renzheng Chen,Xiaowei Ye,Boji Wu,Zhen Liu,Jihang Zhang,Xubin Gao,Ran Cheng,Chunyan He,Jingyu He,Xuhong Wang,Lan Huang

International journal of molecular sciences 23: PubMed36499188

2022

Detection of TRPM6 and TRPM7 Proteins in Normal and Diseased Cardiac Atrial Tissue and Isolated Cardiomyocytes.

Applications

Unspecified application

Species

Unspecified reactive species

Inga Andriulė,Dalia Pangonytė,Asfree Gwanyanya,Dainius Karčiauskas,Kanigula Mubagwa,Regina Mačianskienė

The Journal of cell biology 221: PubMed36222828

2022

Nuclear tension controls mitotic entry by regulating cyclin B1 nuclear translocation.

Applications

Unspecified application

Species

Unspecified reactive species

Margarida Dantas,Andreia Oliveira,Paulo Aguiar,Helder Maiato,Jorge G Ferreira

Frontiers in cell and developmental biology 10:896014 PubMed35874841

2022

PINK1-Dependent Mitophagy Reduced Endothelial Hyperpermeability and Cell Migration Capacity Under Simulated Microgravity.

Applications

Unspecified application

Species

Unspecified reactive species

Chengfei Li,Yikai Pan,Yingjun Tan,Yongchun Wang,Xiqing Sun

Neuron 109:3283-3297.e11 PubMed34672983

2021

A synaptic temperature sensor for body cooling.

Applications

Unspecified application

Species

Unspecified reactive species

Gretel B Kamm,Juan C Boffi,Kristina Zuza,Sara Nencini,Joaquin Campos,Katrin Schrenk-Siemens,Ivo Sonntag,Burçe Kabaoğlu,Muad Y Abd El Hay,Yvonne Schwarz,Anke Tappe-Theodor,Dieter Bruns,Claudio Acuna,Thomas Kuner,Jan Siemens

Scientific reports 11:15445 PubMed34326388

2021

Evidence for the expression of TRPM6 and TRPM7 in cardiomyocytes from all four chamber walls of the human heart.

Applications

Unspecified application

Species

Unspecified reactive species

Inga Andriulė,Dalia Pangonytė,Mantė Almanaitytė,Vaiva Patamsytė,Milda Kuprytė,Dainius Karčiauskas,Kanigula Mubagwa,Regina Mačianskienė

Biochemical and biophysical research communication 533:692-697 PubMed33153718

2020

TRPM7 modulates macrophage polarization by STAT1/STAT6 pathways in RAW264.7 cells.

Applications

Unspecified application

Species

Unspecified reactive species

Lingling Li,Can Wei,Shiyi Cai,Ling Fang
View all publications

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