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.

• Sinonimo/i: TX-1918, 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
• Formula empirica (notazione di Hill): C₁₄H₁₂O₃
• Numero CAS: 503473-32-3
• Peso molecolare: 228.24
• Numero MDL: MFCD06411462
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: light orange
• Solubilità: DMSO: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: Oc1c(cc(cc1C)C=C2C(=O)C=CC2=O)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; YHWRISYBKMXSGJ-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
eEF2-K

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 440 nM against eEF2-K

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Harmful (C)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable