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EB-3D

Catalog No. T7955   CAS 1839150-63-8

EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor(IC50 : 1 μM).with anti-cancer activity.

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EB-3D Chemical Structure
EB-3D, CAS 1839150-63-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 93.00
2 mg In stock $ 133.00
5 mg In stock $ 197.00
10 mg In stock $ 289.00
25 mg In stock $ 498.00
50 mg In stock $ 725.00
100 mg In stock $ 987.00
1 mL * 10 mM (in DMSO) In stock $ 292.00
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Purity: 98.75%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor(IC50 : 1 μM).with anti-cancer activity.
Targets&IC50 ChoKα1:1 μM
In vitro EB-3D?exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines and primary cultures of pediatric patients.?Moreover, the drug strongly induces apoptosis and more importantly it enhanced T-leukemia cell sensitivity to chemotherapeutic agents, such as dexamethasone and l-asparaginase.?In addition, the compound induces an early activation of AMPK, the main regulator of cellular energy homeostasis, by its phosphorylation at residue T712 of catalytic subunit α, and thus repressing mTORC1 pathway, as shown by mTOR S2448 dephosphorylation.?The inhibition of mTOR in turn affects the activity of several known downstream targets, such as 4E-BP1, p70S6K, S6 Ribosomal Protein and GSK3 that ultimately may lead to a reduction of protein synthesis and cell death[1].
Cell Research Cell Line:JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells. Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM.Incubation Time:72 hours
Molecular Weight 644.4
Formula C30H36Br2N4O2
CAS No. 1839150-63-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (77.59 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Elena M , Roberta B , Ilaria V , et al. EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR Pathway and apoptosis in leukemia T-cells[J]. Biochemical Pharmacology, 2018:S0006295218302727-. 2. Schiaffino-Ortega S , Baglioni E , Mariotto E , et al. Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human Choline Kinase α1 (ChoKα1)[J]. Scientific Reports, 2016, 6:23793.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library Membrane Protein-targeted Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Anti-Aging Compound Library Reprogramming Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max Anti-Lung Cancer Compound Library

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Keywords

EB-3D 1839150-63-8 Apoptosis Chromatin/Epigenetic Neuroscience PI3K/Akt/mTOR signaling AChR AMPK lipid inhibit lymphoblastic AMP-activated protein kinase EB3D acute tumorigenesis homeostasis dephosphorylation Inhibitor EB 3D leukemia HepG2 inhibitor

 

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