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TX-1123

Names

[ CAS No. ]:
157397-06-3

[ Name ]:
TX-1123

[Synonym ]:
TX-1123

Biological Activity

[Description]:

TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC50 values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer[1][2].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Neuronal Signaling >> CaMK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Stem Cell/Wnt >> PKA
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src
Signaling Pathways >> Immunology/Inflammation >> COX
Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

COX-2:1.16 nM (IC50)

COX-1:15.7 μM (IC50)


[In Vitro]

TX-1123 (NIH3T3 细胞) 抑制 Src-K、eEF2-K、PKA、PKC、EGFR-k，IC50 值分别为 2.2、3.2、9.6、320 和 320 μM[1]。 TX-1123 (线粒体悬浮液) 具有较弱的线粒体毒性和 ATP 合成抑制活性，IC50 值为 5 μM[1]。 TX-1123 (0-1000 μM; 48 h) 具有抗肿瘤活性，对 HepG2、HCT116 和大鼠肝细胞的 IC50 值分别为 3.66、39 和 57 μM[1] 。 Cell Viability Assay[1] Cell Line: HepG2, HCT116, and Rat hepatocytes Concentration: 0-1000 μM Incubation Time: 48 hours Result: Inhibited tumor cell growth in a dose-dependent manner.

[References]

[1]. Hori H, et, al. TX-1123: an antitumor 2-hydroxyarylidene-4-cyclopentene-1,3-dione as a protein tyrosine kinase inhibitor having low mitochondrial toxicity. Bioorg Med Chem. 2002 Oct;10(10):3257-65.  

[2]. Ohkura K, et, al. Interactive Analysis of TX-1123 with Cyclo-oxygenase: Design of COX2 Selective TX Analogs. Anticancer Res. 2017 Jul;37(7):3849-3854.  

Chemical & Physical Properties

[ Molecular Formula ]:
C20H24O3

[ Molecular Weight ]:
312.40300

[ Exact Mass ]:
312.17300

[ PSA ]:
54.37000

[ LogP ]:
4.07860

Related Compounds