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655203 Millipore

TX-1918 - CAS 503473-32-3 - Calbiochem

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K, while it inhibits other kinases at much higher concentrations.

Synonym: 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, TX-1918 - CAS 503473-32-3 - Calbiochem

  • CAS Number 503473-32-3

  • Empirical Formula (Hill Notation) C14H12O3

  • Molecular Weight 228.24

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Properties

Related Categories Biochemicals and Reagents, D to K, Elongation factor-2 Kinase, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme,
Quality Level   100
assay   ≥95% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   light orange
solubility   DMSO: 10 mg/mL
shipped in   ambient

Description

General description

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment.

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM). Inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Reported to exhibit potent anti-tumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models.

Packaging

10 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
eEF2-K

Product does not compete with ATP.

Reversible: no

Target IC50: 440 nM against eEF2-K

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Hori, H., et al. 2002. Bioorg. Med. Chem.10, 3257.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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