655203

TX-1918

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.

• Synonyme(s) : TX-1918, 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
• Formule empirique (notation de Hill): C₁₄H₁₂O₃
• Numéro CAS: 503473-32-3
• Poids moléculaire : 228.24
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: light orange
• Solubilité: DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C14H12O3/c1-8-5-10(6-9(2)14(8)17)7-11-12(15)3-4-13(11)16/h3-7,17H,1-2H3
• Clé InChI: YHWRISYBKMXSGJ-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
eEF2-K

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 440 nM against eEF2-K

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Harmful (C)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable