All Photos(1)

655203

Sigma-Aldrich

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(s):
TX-1918 - CAS 503473-32-3 - Calbiochem, 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
Empirical Formula (Hill Notation):
C14H12O3
CAS Number:
Molecular Weight:
228.24

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light orange

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

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.
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.

Packaging

10 mg in Plastic ampoule
Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes
Target IC50: 440 nM against eEF2-K
Product does not compete with ATP.
Reversible: no
Primary Target
eEF2-K

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

Certificate of Origin

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service