Genistein

Catalog # Availability Size / Price Qty
1110/10
1110/50
Genistein | CAS No. 446-72-0 | EGF Receptor Inhibitors
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Description: EGFR kinase inhibitor. Also estrogen and PPARγ ligand

Chemical Name: 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one

Purity: ≥98%

Product Details
Citations (10)
Supplemental Products
Reviews

Biological Activity

Genistein is a phytoestrogen with a wide range of biological actions. Genistein inhibits protein tyrosine kinases including epidermal growth factor receptor kinase, binds to PPARγ and estrogen receptors and acts as an agonist at GPER. Genistein inhibits aggregation and fibrilization of Aβ42 and amylin37 (hiAPP). In Huntington's disease fibroblast cells, Genistein reduces intracellular mutant huntingtin (mHTT) aggregates and induces degradation of mHTT; in a cellular model of Huntington's disease, Genistein corrects the mutant phenotype through stimulation of autophagy.

Technical Data

M.Wt:
270.24
Formula:
C15H10O5
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at -20°C
CAS No:
446-72-0

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. 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.
  2. Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
    Tollefson and Taylor
    CNS Drug Reviews, 2000;6:303
  3. Genistein: A Dual Inhibitor of Both Amyloid β and Human Islet Amylin Peptides.
    Ren et al.
    ACS.Chem.Neurosci., 2018;9:1215
  4. Genistein, a specific inhibitor of tyrosine-specific protein kinases.
    Akiyama et al.
    J.Biol.Chem., 1987;262:5592
  5. Peroxisome proliferator-activated receptor γ (PPARγ) as a molecular target for the soy phytoestrogen genistein.
    Dang et al.
    J.Biol.Chem., 2003;278:962
  6. Mechanisms of action in NIH-3T3 cells of genistein, an inhibitor of EGF receptor tyrosine kinase activity.
    Linassier et al.
    Biochem.Pharmacol., 1990;39:187
  7. Prevention of anti-CD3 monoclonal antibody-induced thymic apoptosis by protein tyrosine kinase inhibitors.
    Migita et al.
    J.Immunol., 1994;153:3457
  8. Genistein induces degradation of mutant huntingtin in fibroblasts from Huntington's disease patients.
    Pierzynowska et al.
    Metab.Brain Dis., 2019;34

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Citations for Genistein

The citations listed below are publications that use Tocris products. Selected citations for Genistein include:

10 Citations: Showing 1 - 10

  1. Estrogen modulates serotonin effects on vasoconstriction through Src inhibition.
    Authors: Kim Et al.
    Exp Mol Med  2018;50:167
  2. The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors
    Authors: Olianas Et al.
    European Journal of Pharmacology  2016;794:135
  3. A dual role for NOTCH signaling in joint cartilage maintenance and osteoarthritis.
    Authors: Liu Et al.
    Sci Signal  2015;8:ra71
  4. α6-Containing GABAA Receptors Are the Principal Mediators of Inhibitory Synapse Strengthening by Ins in Cerebellar Granule Cells.
    Authors: Accardi Et al.
    J Neurosci  2015;35:9676
  5. Soy promotes juvenile granulosa cell tumor development in mice and in the human granulosa cell tumor-derived COV434 cell line.
    Authors: Mansouri-Attia Et al.
    Biol Reprod  2014;91:100
  6. 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization.
    Authors: Bigford Et al.
    J Biol Chem  2012;287:11049
  7. Synergistic activation of DA D1 and TrkB receptors mediate gain control of synaptic plasticity in the basolateral amygdala.
    Authors: Li Et al.
    PLoS One  2011;6:e26065
  8. Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors.
    Authors: Melis Et al.
    J Neurosci  2008;28:13985
  9. Protein kinase C dependent inhibition of the heteromeric Kir4.1-Kir5.1 channel.
    Authors: Rojas Et al.
    Biochim Biophys Acta  2007;1768:2030
  10. Role of glycogen synthase kinase 3 β (GSK3β) in mediating the cytotoxic effects of the histone deacetylase inhibitor trichostatin A (TSA) in MCF-7 breast cancer cells.
    Authors: Alao Et al.
    Neurotox Res  2006;5:40

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