TX-1123A tyrphostin that acts as a kinase inhibitor for c-Src, eEF2-K, and PKA

TX-1123 (CAS 157397-06-3)

  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getAggregateRating, 70ms
  • REVIEWS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
Synonym: 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
Application: A tyrphostin that acts as a kinase inhibitor for c-Src, eEF2-K, and PKA
CAS Number: 157397-06-3
Molecular Weight: 312.4
Molecular Formula: C20H24O3
* Refer to Certificate of Analysis for lot specific data (including water content).

TX-1123 may be useful as a therapeutic agent for cancer treatment in animal models. A cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for proto-oncogene tyrosine-protein kinase Src (c-Src, IC50 = 2.2 μM), eukaryotic elongation factor-2 kinase (eEF2-K, IC50 = 3.2 μM), and protein kinase A (PKA, IC50 = 9.6 μM). TX-1123 has been shown to inhibit EGFR-K and PKC, but only at much higher concentrations (IC50 = 320 μM).

Additionally, TX-1123 has been reported to exhibit potent anti-tumor activity in HepG2(EC50 = 3.66) and HCT116 (EC50 = 39 μM) tumor cells, with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (sc-200568).


References

1. Hori, Hitoshi., et al., 2002. TX-1123: an antitumor 2-hydroxyarylidene-4-cyclopentene-1,3-dione as a protein tyrosine kinase inhibitor having low mitochondrial toxicity. Bioorganic & medicinal chemistry. 10(10): 3257-65. PMID: 12150871

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml).
Storage :
Store at 4° C
Boiling Point :
442.36° C at 760 mmHg (Predicted)
Density :
1.14 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
c-Src: IC50 = 2.2 µM; eEF2K: IC50 = 3.2 µM; PKA: IC50 = 9.6 µM; PKC: IC50 = 320 µM; EGFR: IC50 = 320 µM
pK Values :
pKa: 10.04 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
403661
MDL Number :
MFCD06411461
SMILES :
CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C=C2C(=O)C=CC2=O

Download SDS (MSDS)

Certificate of Analysis

Adobe Acrobat Reader is required to reliably view,
print and comment on PDF documents

  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getContent, 72ms
  • QUESTIONS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getReviews, 9ms
  • REVIEWS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;

Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.