Molecular structure of TX-1123, CAS Number: 157397-06-3
TX-1123 (CAS 157397-06-3)
Alternate Names:
2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
Application:
TX-1123 is 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
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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 Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively). Has been shown to inhibits EGFR-K and PKC, but only at much higher concentrations (IC50 = 320 µM). Reported to exhibit potent anti-tumor activity (EC50 = 3.66 and 39 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (sc-200568 and sc-200568A).
TX-1123 (CAS 157397-06-3) References
- TX-1123: an antitumor 2-hydroxyarylidene-4-cyclopentene-1,3-dione as a protein tyrosine kinase inhibitor having low mitochondrial toxicity. | Hori, H., et al. 2002. Bioorg Med Chem. 10: 3257-65. PMID: 12150871
- A shikonin derivative, beta-hydroxyisovalerylshikonin, is an ATP-non-competitive inhibitor of protein tyrosine kinases. | Nakaya, K. and Miyasaka, T. 2003. Anticancer Drugs. 14: 683-93. PMID: 14551501
- Angiogenesis inhibitor TX-1898: syntheses of the enantiomers of sterically diverse haloacetylcarbamoyl-2-nitroimidazole hypoxic cell radiosensitizers. | Jin, CZ., et al. 2004. Bioorg Med Chem. 12: 4917-27. PMID: 15336271
- Effect of molecular chirality and side chain bulkiness on angiogenesis of haloacetylcarbamoyl-2-nitroimidazole compounds. | Ohkura, K., et al. 2007. Anticancer Res. 27: 3693-700. PMID: 17970030
- Design of antiangiogenic hypoxic cell radiosensitizers: 2-nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety. | Uto, Y., et al. 2008. Bioorg Med Chem. 16: 6042-53. PMID: 18474428
- Chemical properties and biological activities of cyclopentenediones: a review. | Sevcíková, Z., et al. 2014. Mini Rev Med Chem. 14: 322-31. PMID: 24605879
- The chemerin receptor CMKLR1 is a functional receptor for amyloid-β peptide. | Peng, L., et al. 2015. J Alzheimers Dis. 43: 227-42. PMID: 25079809
- A comprehensive LC/MS analysis of novel cyclopentenedione library. | Papouskova, B., et al. 2016. J Pharm Biomed Anal. 128: 342-351. PMID: 27328361
- An Antitumor 2-Hydroxyarylidene-4-cyclopentene-1,3-Dione as a Protein Tyrosine Kinase Inhibitor: Interaction Between TX-1123 Derivatives and Src Kinase. | Ohkura, K., et al. 2016. Anticancer Res. 36: 3645-9. PMID: 27354635
- Interactive Analysis of TX-1123 with Cyclo-oxygenase: Design of COX2 Selective TX Analogs. | Ohkura, K., et al. 2017. Anticancer Res. 37: 3849-3854. PMID: 28668885
Inhibitor of:
c-Src, eEF2K, PKA, and Ser/Thr Protein Kinase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TX-1123, 10 mg | sc-296675 | 10 mg | $185.00 |