Molecular structure of TX-1918, CAS Number: 503473-32-3
TX-1918 (CAS 503473-32-3)
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Alternate Names:
2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
Application:
TX-1918 is a potent inhibitor for eEF2K
CAS Number:
503473-32-3
Molecular Weight:
228.25
Molecular Formula:
C14H12O3
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
TX-1918 may be useful as a therapeutic agent for cancer treatment in animal models. A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eukaryotic elongation factor-2 kinase (eEF2K, IC50 = 440 nM). At higher concentrations, TX-1918 may act to inhibit other kinases, including proto-oncogene tyrosine-protein kinase Src (c-SRC, IC50 = 4.4 μM), protein kinase A and C (PKA and PKC, IC50 = 44 μM for each), and epidermal growth factor receptor kinase (EGFR-K, IC50 = 440 μM). Additionally, TX-1918 has been reported to exhibit potent anti-tumor activity in HepG2 (EC50 = 2.07) and HCT116 (EC50 = 230 muM) tumor cells, with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (sc-200568).
TX-1918 (CAS 503473-32-3) References
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- Synthetic lethal screening with small-molecule inhibitors provides a pathway to rational combination therapies for melanoma. | Roller, DG., et al. 2012. Mol Cancer Ther. 11: 2505-15. PMID: 22962324
- Combined deletion of Pten and p53 in mammary epithelium accelerates triple-negative breast cancer with dependency on eEF2K. | Liu, JC., et al. 2014. EMBO Mol Med. 6: 1542-60. PMID: 25330770
- Identifying a kinase network regulating FGF14:Nav1.6 complex assembly using split-luciferase complementation. | Hsu, WC., et al. 2015. PLoS One. 10: e0117246. PMID: 25659151
- Eukaryotic elongation factor 2 kinase as a drug target in cancer, and in cardiovascular and neurodegenerative diseases. | Liu, R. and Proud, CG. 2016. Acta Pharmacol Sin. 37: 285-94. PMID: 26806303
- 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
- New eremophilane and dichlororesorcinol derivatives produced by endophytes isolated from Ficus ampelas. | Shiono, Y., et al. 2017. J Antibiot (Tokyo). 70: 1133-1137. PMID: 29066796
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- Structure prediction of eukaryotic elongation factor-2 kinase and identification of the binding mechanisms of its inhibitors: homology modeling, molecular docking, and molecular dynamics simulation. | Tatar, G., et al. 2022. J Biomol Struct Dyn. 40: 13355-13365. PMID: 30880628
- A HTRF based competitive binding assay for screening specific inhibitors of HIV-1 capsid assembly targeting the C-Terminal domain of capsid. | Zhang, DW., et al. 2019. Antiviral Res. 169: 104544. PMID: 31254557
- Progress in the Development of Eukaryotic Elongation Factor 2 Kinase (eEF2K) Natural Product and Synthetic Small Molecule Inhibitors for Cancer Chemotherapy. | Zhang, B., et al. 2021. Int J Mol Sci. 22: PMID: 33673713
- Target-Driven Design of a Coumarinyl Chalcone Scaffold Based Novel EF2 Kinase Inhibitor Suppresses Breast Cancer Growth In Vivo. | Comert Onder, F., et al. 2021. ACS Pharmacol Transl Sci. 4: 926-940. PMID: 33860211
- Inhibiting Eukaryotic Elongation Factor 2 Kinase: An Update on Pharmacological Small-Molecule Compounds in Cancer. | Zhu, S., et al. 2021. J Med Chem. 64: 8870-8883. PMID: 34162208
- Novel inhibitors of eukaryotic elongation factor 2 kinase: In silico, synthesis and in vitro studies. | Onder, FC., et al. 2021. Bioorg Chem. 116: 105296. PMID: 34488125
Inhibitor of:
c-Src, and eEF2K.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TX-1918, 10 mg | sc-296676 | 10 mg | $226.00 | |||
TX-1918, 50 mg | sc-296676A | 50 mg | $728.00 | |||
TX-1918, 250 mg | sc-296676B | 250 mg | $1327.00 |